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Wróblewska-Łuczka P, Kulenty L, Załuska-Ogryzek K, Góralczyk A, Łuszczki JJ. Screening of the Antimelanoma Activity of Monoterpenes-In Vitro Experiments on Four Human Melanoma Lines. Curr Issues Mol Biol 2025; 47:97. [PMID: 39996818 PMCID: PMC11854273 DOI: 10.3390/cimb47020097] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/14/2025] [Revised: 01/28/2025] [Accepted: 02/01/2025] [Indexed: 02/26/2025] Open
Abstract
(1) Malignant melanoma is the most aggressive type of malignant tumor caused by a dysfunction of melanocytes. Despite progress in the treatment of melanoma, further research and search for new potential drugs are necessary to optimize the therapy. (2) The aim of this study was to evaluate the antiproliferative activity of eight selected monoterpenes by MTT and LDH assays on four malignant melanoma cell lines. (3) Myrcene, rhodinol and nerol did not show any significant anticancer effect on melanoma cell lines, but citral, carvacrol, citronellol, thymol and geraniol showed a significant anti-viability effect. Our studies have shown that the most effective terpene among those tested in inhibiting melanoma cell viability was carvacrol, with the lowest IC50 in the range of 0.05 ± 0.00 to 0.06 ± 0.01 mM. Moreover, it did not negatively affect normal human keratinocyte cells. (4) Metastatic melanoma is very difficult to treat, and some terpenes have the ability to sensitize cells to other chemicals; so, it is worth investigating their antimelanoma potential, as terpenes could become an adjuvant to traditional treatment.
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Affiliation(s)
- Paula Wróblewska-Łuczka
- Department of Occupational Medicine, Medical University of Lublin, 20-090 Lublin, Poland (K.Z.-O.); (A.G.); (J.J.Ł.)
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Maharajan N, Kim KH, Vijayakumar KA, Cho GW. Unlocking Therapeutic Potential: Camphorquinone's Role in Alleviating Non-Alcoholic Fatty Liver Disease via SIRT1/LKB1/AMPK Pathway Activation. Tissue Eng Regen Med 2025; 22:129-144. [PMID: 39680356 PMCID: PMC11712022 DOI: 10.1007/s13770-024-00684-8] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/26/2024] [Revised: 10/16/2024] [Accepted: 11/06/2024] [Indexed: 12/17/2024] Open
Abstract
BACKGROUND Non-alcoholic fatty liver disease (NAFLD) is a pathological condition that increase the risk of simple steatosis to hepatocellular carcinoma. This study aimed to investigate the biological effects of camphorquinone (CQ) in a high-fat diet (HFD)-fed and low dose streptozotocin (STZ)-induced mouse model, widely used to mimic the concurrent development of NAFLD pathological conditions in vivo, and a free fatty acid-induced hepatic steatosis cell model in vitro. METHODS CQ (10 or 30 mg/kg/day; i.p.) was injected for three weeks, and fasting blood glucose levels, glucose tolerance, and liver lipid metabolism were assessed. RESULTS CQ administration alleviated the increase in body and liver weights and improved glucose tolerance in NAFLD mice model. CQ also reduced the gene expression levels of lipid biosynthesis and inflammation markers, while increasing the levels of fatty acid oxidation markers in liver tissues and HepG2 cells. These beneficial effects of CQ were mediated via activation of the sirtuin 1 (SIRT1)/adenosine monophosphate-activated protein kinase (AMPK) signalling pathway in vitro and in vivo. CONCLUSION Collectively, our data suggest that CQ improves liver lipid metabolism and reduces blood glucose levels via activation of the SIRT1/serine/threonine kinase 11 (STK11/LKB1)/AMPK axis.
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Affiliation(s)
- Nagarajan Maharajan
- Department of Otorhinolaryngology, Head and Neck Surgery, University of Maryland School of Medicine, Baltimore, MD, 21201, USA
| | - Kil Hwan Kim
- Veterans Health Service Medical Center, Veterans Medical Research Institute, Seoul, 05368, Korea
| | - Karthikeyan A Vijayakumar
- Department of Biological Science, College of Natural Sciences, Chosun University, 309 Pilmun-Daero, Dong-Gu, Gwangju, 501-759, Korea
- The Basic Science Institute of Chosun University, Chosun University, Gwangju, 61452, Korea
| | - Gwang-Won Cho
- Department of Biological Science, College of Natural Sciences, Chosun University, 309 Pilmun-Daero, Dong-Gu, Gwangju, 501-759, Korea.
- The Basic Science Institute of Chosun University, Chosun University, Gwangju, 61452, Korea.
- Department of Integrative Biological Science, BK21 FOUR Education Research Group for Age-Associated Disorder Control Technology, Chosun University, Gwangju, 61452, Korea.
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Ribeiro T, Reis M, Vasconcelos V, Urbatzka R. Phenotypic screening in zebrafish larvae identifies promising cyanobacterial strains and pheophorbide a as insulin mimetics. Sci Rep 2024; 14:32142. [PMID: 39739113 PMCID: PMC11685485 DOI: 10.1038/s41598-024-83986-0] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/26/2024] [Accepted: 12/18/2024] [Indexed: 01/02/2025] Open
Abstract
Diabetes is a pandemic disease that causes the loss of control of glucose regulation in the organism, in consequence of dysfunction of insulin production or functionality. In this work, the antidiabetic bioactivity of 182 fractions from 19 cyanobacteria strains derived from the LEGE Culture Collection were analysed using the 2-NBDG assay in zebrafish larvae. From this initial screening, two fractions (57 (06104_D) and 107 (03283_B)) were identified as promising insulin mimetics. These were further characterized by measuring glucose levels in whole larvae, the expression of glucose transporters (GLUT 1-3) using western blot, and the mRNA expression levels of the glut2, pepck, and insa genes using real-time qPCR. Both fractions showed a decrease in free glucose levels. Furthermore, exposure to fraction 06104_D decreased GLUT1 and increased insa mRNA levels. The chemical composition of these fractions was determined using LC-HRESIMS/MS and compared to inactive fractions of the same polarity in order to identify the unique bioactive molecules. The molecular networks constructed using the GNPS platform revealed that fraction 06104_D contained mass clusters primarily composed of chlorins, lipids, and terpenoids, while fraction 03283_B contained xanthophylls, peptides, and terpenoids. To correlate the observed activity with the chemical composition of fraction 06104_D, pheophorbide a was chosen as a representative of chlorophyll derivatives. Exposure to zebrafish larvae at 10 and 20 µM confirmed the increased glucose uptake on the 2-NBDG assay. These findings highlight the bioactivity of chlorophyll derivatives as insulin mimetic compounds, as well as cyanobacteria as a source of potential therapeutic diabetes applications.
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Affiliation(s)
- Tiago Ribeiro
- Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Avenida General Norton de Matos, s/n, Matosinhos, 4450-208, Portugal.
- Faculty of Sciences, University of Porto, Rua do Campo Alegre, Porto, 1021, 4169-007, Portugal.
| | - Mariana Reis
- Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Avenida General Norton de Matos, s/n, Matosinhos, 4450-208, Portugal
| | - Vitor Vasconcelos
- Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Avenida General Norton de Matos, s/n, Matosinhos, 4450-208, Portugal
- Faculty of Sciences, University of Porto, Rua do Campo Alegre, Porto, 1021, 4169-007, Portugal
| | - Ralph Urbatzka
- Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Avenida General Norton de Matos, s/n, Matosinhos, 4450-208, Portugal
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Wang D, Zhang W, Zhao Z, Li D, Fang Y, Wang Z, Lv J, Luan Y, Zhang W. Terpene mixtures and metabolic syndrome in the US general population: exploring the mediating role of insulin resistance. BMC Public Health 2024; 24:3587. [PMID: 39722019 DOI: 10.1186/s12889-024-20926-7] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/31/2024] [Accepted: 12/02/2024] [Indexed: 12/28/2024] Open
Abstract
BACKGROUND Terpenes have been shown to have an effect on metabolic status. However, it is unclear how they are associated with the metabolic syndrome (MetS) and whether insulin resistance (IR) mechanisms are involved. METHODS This cross-sectional study included data from the National Health and Nutrition Examination Survey (2013-2014). Serum terpenes (α- pinene, β- pinene, and limonene) were quantified by gas chromatography-tandem mass spectrometry. MetS was diagnosed by lipid, glucose, blood pressure, and waist circumference criteria. IR status was assessed using the homeostasis model assessment of insulin resistance (HOMA-IR) model and triglyceride-glucose index. Regression analysis models, mixed-effects models (weighted quantile sum regression models, quantile g-computation and Bayesian Kernel machine regression models), and mediation analysis were used for analysis. RESULTS Among 1563 U.S. general population (mean age 39.0 years), 447 (28.6%) had a diagnosis of MetS, and the median concentration was 0.08 ng/mL for α- pinene, 0.08 ng/mL for β- pinene, and 1.18 ng/mL for limonene. The terpene mixture showed positive joint association with MetS (OR = 1.454, 95%CI = 1.153, 1.833) and HOMA-IR (β = 0.569, 95%CI = 0.196, 0.942), with limonene contributing relatively large weights in both MetS (41.1%) and HOMA-IR (68.9%). Furthermore, HOMA-IR was positively associated with MetS (OR = 2.299, 95%CI = 1.888, 2.817) and its diagnostic components. When identified as a mediator, HOMA-IR accounted for approximately 15.8%, 20.0%, and 14.3% of the indirect effects between terpenes (α- pinene, β- pinene, and limonene) and MetS, respectively. The results were consistent when the IR biomarker was replaced by triglyceride-glucose index. CONCLUSION Serum terpenes were positively associated with MetS, which might be partially mediated by the mechanism of IR.
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Affiliation(s)
- Dan'an Wang
- Department of Cardiology, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, 3 East Qingchun Road, Hangzhou, Zhejiang, 310000, People's Republic of China
- Key Laboratory of Cardiovascular Intervention and Regenerative Medicine of Zhejiang Province, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Wei Zhang
- Department of Cardiology, Lishui People's Hospital, The Six Affiliated Hospital of Wenzhou Medical University, Zhejiang Province, Lishui, Zhejiang, 323000, People's Republic of China
| | - Zhenni Zhao
- Nursing Department, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Duanbin Li
- Department of Cardiology, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, 3 East Qingchun Road, Hangzhou, Zhejiang, 310000, People's Republic of China
- Key Laboratory of Cardiovascular Intervention and Regenerative Medicine of Zhejiang Province, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Yuan Fang
- School of Medicine, Zhejiang University, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Zijie Wang
- School of Medicine, Zhejiang University, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Jingyi Lv
- School of Medicine, Zhejiang University, Hangzhou, Zhejiang, 310000, People's Republic of China
| | - Yi Luan
- Department of Cardiology, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, 3 East Qingchun Road, Hangzhou, Zhejiang, 310000, People's Republic of China.
- Key Laboratory of Cardiovascular Intervention and Regenerative Medicine of Zhejiang Province, Hangzhou, Zhejiang, 310000, People's Republic of China.
| | - Wenbin Zhang
- Department of Cardiology, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, 3 East Qingchun Road, Hangzhou, Zhejiang, 310000, People's Republic of China.
- Key Laboratory of Cardiovascular Intervention and Regenerative Medicine of Zhejiang Province, Hangzhou, Zhejiang, 310000, People's Republic of China.
- Shaoxing University, Shaoxing, Zhejiang, 312000, People's Republic of China.
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Faivre C, Imtiyaz FD, Buyck JM, Marchand S, Marcotte M, Henry T, Anton N, Collot M, Tewes F. (E, E)-farnesol and myristic acid-loaded lipid nanoparticles overcome colistin resistance in Acinetobacter baumannii. Int J Pharm 2024; 667:124907. [PMID: 39500471 DOI: 10.1016/j.ijpharm.2024.124907] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/24/2024] [Revised: 10/09/2024] [Accepted: 11/01/2024] [Indexed: 11/08/2024]
Abstract
The rise of colistin-resistant Acinetobacter baumannii has severely limited treatment options for infections caused by this pathogen. While terpene alcohols and fatty acids have shown potential to enhance colistin's efficacy, but their high lipophilicity limits their clinical application. To address this, we developed water-dispersible lipid nanoparticles (LNPs) in two sizes (40 nm and 130 nm), loaded with these compounds to act as colistin adjuvants. Among eleven LNP formulations, six significantly reduced colistin's minimum inhibitory concentration (MIC) by 16- to 64-fold. The most effective, featuring (E,E)-farnesol and myristic acid, were further examined for bactericidal activity, membrane disruption, cytotoxicity, and in vivo efficacy in Galleria mellonella larvae. Time-kill studies demonstrated that at an adjuvant concentration of 60 mg/L, these LNPs eradicated bacteria when combined with 4 mg/L free colistin for resistant isolates (MIC = 128 mg/L) and 0.06 mg/L for susceptible isolates (MIC = 0.5 mg/L), without regrowth. Myristic acid-loaded LNPs combined with free colistin at 1/8 MIC resulted in a 4.2-fold higher mortality rate than the combination with (E,E)-farnesol-loaded LNPs in resistant strains. This result was correlated with a 45-fold faster increase in inner membrane permeability, measured by propidium iodide (PI) uptake, in the presence of myristic acid-loaded LNPs compared with a 13-fold faster increase with (E,E)-farnesol-loaded LNPs. DiSC3(5) assays revealed that LNPs alone depolarised the bacterial inner membrane, with enhanced effects when combined with colistin at 1/8 MIC, a result not observed with colistin alone at this concentration. As with PI uptake, this inner membrane depolarising effect was more pronounced with myristic acid-loaded LNPs than with (E,E)-farnesol-loaded LNPs in resistant strains, suggesting that the colistin adjuvant effect of these lipophilic compounds is due to their ability to help colistin destabilise the bacterial inner membrane. Cytotoxicity assays demonstrated no adverse effects on bone marrow macrophages after 6 h of exposure, although some toxicity was observed after 24 h. No mortality was observed in Galleria mellonella larvae over 7 days following three consecutive days of treatment with colistin and LNPs. Notably, the combination of (E,E)-farnesol-loaded LNPs and colistin significantly improved the survival of Galleria infected with A.baumannii. These results suggest that lipophilic-adjuvant-loaded LNPs may offer a promising strategy to enhance colistin efficacy and combat antibiotic-resistant A. baumannii infections.
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Affiliation(s)
- Carla Faivre
- Laboratoire de Bioimagerie et Pathologies, UMR 7021, CNRS/Université de Strasbourg, 74 route du Rhin, 67401 Illkirch-Graffenstaden, France; INSERM UMR 1260, Regenerative Nanomedicine (RNM), FMTS, Université de Strasbourg, F-67000 Strasbourg, France
| | | | - Julien M Buyck
- Université de Poitiers, PHAR2, INSERM U1070, Poitiers, France
| | - Sandrine Marchand
- Université de Poitiers, PHAR2, INSERM U1070, Poitiers, France; CHU de Poitiers, Laboratoire de Toxicologie et de Pharmacocinétique, Poitiers, France
| | - Melissa Marcotte
- CIRI, Centre International de Recherche en Infectiologie, Inserm U1111, Université Claude Bernard Lyon 1, CNRS, UMR5308, ENS de Lyon, Univ. Lyon, Lyon, France
| | - Thomas Henry
- CIRI, Centre International de Recherche en Infectiologie, Inserm U1111, Université Claude Bernard Lyon 1, CNRS, UMR5308, ENS de Lyon, Univ. Lyon, Lyon, France
| | - Nicolas Anton
- INSERM UMR 1260, Regenerative Nanomedicine (RNM), FMTS, Université de Strasbourg, F-67000 Strasbourg, France
| | - Mayeul Collot
- Laboratoire de Bioimagerie et Pathologies, UMR 7021, CNRS/Université de Strasbourg, 74 route du Rhin, 67401 Illkirch-Graffenstaden, France.
| | - Frédéric Tewes
- Université de Poitiers, PHAR2, INSERM U1070, Poitiers, France.
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Iudanov K, Nechmad NB, Poater A, Lemcoff NG. Selective Cross-Metathesis Versus Ring-Closing Metathesis of Terpenes, Taking the Path Less Travelled. Angew Chem Int Ed Engl 2024; 63:e202412430. [PMID: 39305156 DOI: 10.1002/anie.202412430] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/02/2024] [Indexed: 11/01/2024]
Abstract
A diiodo ruthenium olefin metathesis pre-catalyst was employed to achieve remarkably selective cross-metathesis reactions of prenylated 1,6-dienes, effectively overcoming the entropically favored intramolecular ring-closing metathesis. This reaction was investigated using Density Functional Theory (DFT) computations and fine-tuned through the application of a Design of Experiments (DoE) approach. The potential of this innovative process was demonstrated through the unprecedented functionalization of various terpene natural products via cross-metathesis, resulting in the synthesis of new derivatives in a single step.
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Affiliation(s)
- Keren Iudanov
- Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva, 84105, Israel
| | - Noy B Nechmad
- Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva, 84105, Israel
| | - Albert Poater
- Institut de Química Computacional i Catàlisi and Departament de Química, Universitat de Girona, c/ Maria Aurèlia Capmany 69, 17003, Girona, Catalonia, Spain
| | - N Gabriel Lemcoff
- Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva, 84105, Israel
- Ilse Katz Institute for Nanotechnology Science, Ben-Gurion University of the Negev, Beer-Sheva, 84105, Israel
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Ramírez-Santos J, Calzada F, García-Hernández N, Barbosa E, Velázquez C, Valdes M. Caryophyllene Oxide, a Bicyclic Terpenoid Isolated from Annona macroprophyllata with Antitumor Activity: In Vivo, In Vitro, and In Silico Studies. Int J Mol Sci 2024; 25:13355. [PMID: 39769118 PMCID: PMC11676109 DOI: 10.3390/ijms252413355] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/08/2024] [Revised: 11/30/2024] [Accepted: 12/03/2024] [Indexed: 01/11/2025] Open
Abstract
The Annona genus contains some species used in Mexican traditional medicine for the treatment cancer, including Annona macroprophyllata (A. macroprophyllata). The present study aimed to investigate the anticancer activity of caryophyllene oxide (CO) isolated from A. macroprophyllata using in vivo, in vitro, and in silico approaches. The identification of CO was performed using gas chromatography-mass spectroscopy and NMR methods. Antilymphoma activity was evaluated in male and female Balb/c mice inoculated with U-937 cells. Cytotoxic activity was evaluated using the WST method and flow cytometry was used to determine the type of cell death. Acute oral toxicity was determined, and a molecular docking study was performed using target proteins associated with cancer, including, HMG-CoA, Bcl-2, Mcl-1, and VEGFR-2. Results showed that CO exhibited significant antilymphoma and cytotoxic activities, and its effects were comparable to MTX. In addition, flow cytometry showed that the anticancer activity of CO could be mediated by the induction of late apoptosis and necrosis. The result for the acute oral toxicity of CO was classified in category 4, suggesting it is low risk. Finally, molecular coupling studies showed that CO had more affinity for the enzymes HMG-CoA reductase and Bcl-2. Our study provides evidences that CO is a potential anticancer agent for the treatment of histiocytic lymphoma.
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Affiliation(s)
- Jesica Ramírez-Santos
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Mexico City CP 06720, Mexico;
| | - Fernando Calzada
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Mexico City CP 06720, Mexico;
| | - Normand García-Hernández
- Unidad de Investigación Médica en Genética Humana, UMAE Hospital Pediatría, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Mexico City CP 06725, Mexico;
| | - Elizabeth Barbosa
- Escuela Superior de Medicina, Instituto Politécnico Nacional, Mexico City CP 11340, Mexico;
| | - Claudia Velázquez
- Área Académica de Farmacia, Instituto de Ciencias de la Salud, Universidad Autonoma del Estado de Hidalgo, San Agustin Tlaxiaca CP 42076, Mexico;
| | - Miguel Valdes
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Mexico City CP 06720, Mexico;
- Laboratorio de Biofísica y Biocatálisis, Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Mexico City CP 11340, Mexico
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Fan X, Liu X, Yan Y, Hua D, Luo K, Hao S, Zhu D, Zhou D, Liu H. Widely targeted metabolomics analysis reveals the effect of soybean hull polysaccharides on nonvolatile components of plant-based yogurt and its metabolic pattern. Int J Biol Macromol 2024; 279:135144. [PMID: 39208892 DOI: 10.1016/j.ijbiomac.2024.135144] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/23/2024] [Revised: 08/09/2024] [Accepted: 08/26/2024] [Indexed: 09/04/2024]
Abstract
Soybean hull polysaccharides (SHPS) enhance the physicochemical properties of plant-based yogurt. However, their effects on the nutritional profile and biochemical mechanisms remain unclear. This study aimed to assess the impact of SHPS addition on the nonvolatile components of plant-based yogurt and its underlying mechanisms through widely targeted metabolomics analysis. The results demonstrated that the addition of SHPS (0.2 %-1.0 % w/v) enhanced the levels of free amino acids, sugars, and organic acids, with the addition of 0.6 % w/v being particularly effective in improving yogurt quality. Widely targeted metabolomics analysis revealed 278 differential metabolites between yogurt supplemented with 0.6 % SHPS (SPY) and the control sample. SHPS increased the content of various metabolites, including amino acids and derivatives, saccharides, organic acids, and flavonoids, among others. Key metabolic pathways affected by SHPS included pantothenate and CoA biosynthesis; valine, leucine, and isoleucine biosynthesis; and benzoate degradation. As the primary component of SHPS, galacturonic acid affected the metabolic products in yogurt by participating in the pentose and glucuronate interconversions and ascorbate and aldarate metabolism pathways. These findings elucidate the role of SHPS in modulating the nutritional composition of plant-based yogurt, offering valuable insights into its functional mechanisms in food processing.
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Affiliation(s)
- Xiangrong Fan
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Xiaoqing Liu
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Yaxin Yan
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Dong Hua
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Ke Luo
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Sijia Hao
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Danshi Zhu
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China
| | - Dayu Zhou
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China.
| | - He Liu
- College of Food Science and Technology, Bohai University, Jinzhou 121013, China.
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Ciumărnean L, Sârb OF, Drăghici NC, Sălăgean O, Milaciu MV, Orășan OH, Vlad CV, Vlad IM, Alexescu T, Para I, Țărmure SF, Hirișcău EI, Dogaru GB. Obesity Control and Supplementary Nutraceuticals as Cofactors of Brain Plasticity in Multiple Sclerosis Populations. Int J Mol Sci 2024; 25:10909. [PMID: 39456690 PMCID: PMC11507128 DOI: 10.3390/ijms252010909] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/04/2024] [Revised: 09/26/2024] [Accepted: 10/07/2024] [Indexed: 10/28/2024] Open
Abstract
Multiple sclerosis (MS) is an immune-mediated disease characterized by inflammation, demyelination, and neurodegeneration within the central nervous system. Brain plasticity, the brain's ability to adapt its structure and function, plays a crucial role in mitigating MS's impact. This paper explores the potential benefits of lifestyle changes and nutraceuticals on brain plasticity in the MS population. Lifestyle modifications, including physical activity and dietary adjustments, can enhance brain plasticity by upregulating neurotrophic factors, promoting synaptogenesis, and reducing oxidative stress. Nutraceuticals, such as vitamin D, omega-3 fatty acids, and antioxidants like alpha lipoic acid, have shown promise in supporting brain health through anti-inflammatory and neuroprotective mechanisms. Regular physical activity has been linked to increased levels of brain-derived neurotrophic factor and improved cognitive function. Dietary interventions, including caloric restriction and the intake of polyphenols, can also positively influence brain plasticity. Integrating these lifestyle changes and nutraceuticals into the management of MS can provide a complementary approach to traditional therapies, potentially improving neurological outcomes and enhancing the quality of life for the MS population.
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Affiliation(s)
- Lorena Ciumărnean
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Oliviu-Florențiu Sârb
- Department of Clinical Neurosciences, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania (I.-M.V.)
| | - Nicu-Cătălin Drăghici
- Department of Clinical Neurosciences, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania (I.-M.V.)
- “IMOGEN” Institute, Centre of Advanced Research Studies, Emergency Clinical County Hospital Cluj, 400347 Cluj-Napoca, Romania
| | - Octavia Sălăgean
- Department of Nursing, Faculty of Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania; (O.S.); (E.-I.H.)
| | - Mircea-Vasile Milaciu
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Olga-Hilda Orășan
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Călin-Vasile Vlad
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Irina-Maria Vlad
- Department of Clinical Neurosciences, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania (I.-M.V.)
| | - Teodora Alexescu
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Ioana Para
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Simina-Felicia Țărmure
- Department of Internal Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400015 Cluj-Napoca, Romania; (L.C.); (M.-V.M.); (O.-H.O.); (C.-V.V.); (T.A.); (I.P.); (S.-F.Ț.)
| | - Elisabeta-Ioana Hirișcău
- Department of Nursing, Faculty of Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania; (O.S.); (E.-I.H.)
| | - Gabriela-Bombonica Dogaru
- Department of Medical Rehabilitation, “Iuliu Hațieganu” University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania
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10
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Saxena S, Dufossé L, Deshmukh SK, Chhipa H, Gupta MK. Endophytic Fungi: A Treasure Trove of Antifungal Metabolites. Microorganisms 2024; 12:1903. [PMID: 39338577 PMCID: PMC11433805 DOI: 10.3390/microorganisms12091903] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/11/2024] [Revised: 09/10/2024] [Accepted: 09/12/2024] [Indexed: 09/30/2024] Open
Abstract
Emerging and reemerging fungal infections are very common in nosocomial and non-nosocomial settings in people having poor immunogenic profiles either due to hematopoietic stem cell transplants or are using immunomodulators to treat chronic inflammatory disease or autoimmune disorders, undergoing cancer therapy or suffering from an immune weakening disease like HIV. The refractory behavior of opportunistic fungi has necessitated the discovery of unconventional antifungals. The emergence of black fungus infection during COVID-19 also triggered the antifungal discovery program. Natural products are one of the alternative sources of antifungals. Endophytic fungi reside and co-evolve within their host plants and, therefore, offer a unique bioresource of novel chemical scaffolds with an array of bioactivities. Hence, immense possibilities exist that these unique chemical scaffolds expressed by the endophytic fungi may play a crucial role in overcoming the burgeoning antimicrobial resistance. These chemical scaffolds so expressed by these endophytic fungi comprise an array of chemical classes beginning from cyclic peptides, sesquiterpenoids, phenols, anthraquinones, coumarins, etc. In this study, endophytic fungi reported in the last six years (2018-2023) have been explored to document the antifungal entities they produce. Approximately 244 antifungal metabolites have been documented in this period by different groups of fungi existing as endophytes. Various aspects of these antifungal metabolites, such as antifungal potential and their chemical structures, have been presented. Yet another unique aspect of this review is the exploration of volatile antifungal compounds produced by these endophytic fungi. Further strategies like epigenetic modifications by chemical as well as biological methods and OSMAC to induce the silent gene clusters have also been presented to generate unprecedented bioactive compounds from these endophytic fungi.
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Affiliation(s)
- Sanjai Saxena
- Department of Biotechnology, Thapar Institute of Engineering and Technology, Patiala 147004, Punjab, India;
- Agpharm Bioinnovations LLP, Incubatee: Science and Technology Entrepreneurs Park (STEP), Thapar Institute of Engineering and Technology, Patiala 147004, Punjab, India
| | - Laurent Dufossé
- Chimie et Biotechnologie des Produits Naturels (ChemBioPro Lab) & ESIROI Agroalimentaire, Université de la Réunion, 15 Avenue René Cassin, CS 92003, F-97744 Saint-Denis, France
| | - Sunil K. Deshmukh
- Agpharm Bioinnovations LLP, Incubatee: Science and Technology Entrepreneurs Park (STEP), Thapar Institute of Engineering and Technology, Patiala 147004, Punjab, India
- R&D Division, Greenvention Biotech Pvt. Ltd., Uruli Kanchan 412202, Maharashtra, India
| | - Hemraj Chhipa
- College of Horticulture and Forestry, Agriculture University Kota, Jhalawar 322360, Rajasthan, India;
| | - Manish Kumar Gupta
- SGT College of Pharmacy, SGT University, Gurugram 122505, Haryana, India;
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11
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De Gregorio MA, Zhang L, Mahomoodally MF, Zengin G, Jugreet S, Yildiztugay E, Fiorini A, Lucini L. Metabolomic Profiles and Biopharmaceutical Properties of Petrosimonia brachiata and P. nigdeensis from Turkey. PLANTS (BASEL, SWITZERLAND) 2024; 13:2073. [PMID: 39124192 PMCID: PMC11314340 DOI: 10.3390/plants13152073] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Subscribe] [Scholar Register] [Received: 06/14/2024] [Revised: 07/16/2024] [Accepted: 07/25/2024] [Indexed: 08/12/2024]
Abstract
Halophytic plants possess a huge range of active constituents and medicinal benefits. In this study, extracts (water, ethanol, ethyl acetate, dichloromethane, and n-hexane) of two halophytes of the genus Petrosimonia (P. brachiata and P. nigdeensis) were investigated for their phytochemical profiles and pharmacological properties. The phytochemical profiles of both species were investigated using an untargeted metabolomics approach based on high-resolution mass spectrometry. The two species show different polyphenolic profiles and these are influenced by the different extraction solvents used. The same extracts were used for different bioactivity assays. The results show that all extracts yielded total flavonoid and phenolic contents of 11.14-24.22 mg GAE/g and 3.15-22.03 mg RE/g, respectively. While extracts of both species demonstrated a radical scavenging ability in the ABTS assay (16.12-98.02 mg TE/g), only the polar and moderately polar extracts (water, ethanol, and ethyl acetate) showed scavenging potential in the DPPH assay (4.74-16.55 mg TE/g). A reducing potential was also displayed by all extracts in the CUPRAC and FRAP assays (26.02-80.35 mg TE/g and 31.70-67.69 mg TE/g, respectively). The total antioxidant capacity of the extracts ranged from 0.24 to 2.17 mmol TE/g, and the metal chelating activity ranged from 14.74 to 33.80 mg EDTAE/g. The water extracts possessed a higher metal chelating power than the other extracts. All extracts acted as inhibitors of acetylcholinesterase (0.16-3.85 mg GALAE/g) and amylase (0.11-1.28 mmol ACAE/g). Moreover, apart from the water extracts, the other extracts also showed anti-butyrylcholinesterase activity (0.73-2.86 mg GALAE/g), as well as anti-tyrosinase (36.74-61.40 mg KAE/g) and anti-glucosidase (2.37-2.73 mmol ACAE/g) potential. In general, the water extracts were found to be weak inhibitors of the tested enzymes, while the ethanol extracts mostly showed an inhibitory effect. The obtained findings revealed the antioxidant and enzyme inhibitory properties of these two species and demonstrated that the solvent type used affected the pharmacological properties of the extracts and hence, can be useful to further investigate the active constituents yielded in the extracts and understand the mechanisms involved.
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Affiliation(s)
- Marco A. De Gregorio
- Department of Sustainable Food Process, Università Cattolica del Sacro Cuore, 29122 Piacenza, Italy; (M.A.D.G.); (L.L.)
| | - Leilei Zhang
- Department of Sustainable Food Process, Università Cattolica del Sacro Cuore, 29122 Piacenza, Italy; (M.A.D.G.); (L.L.)
| | - Mohamad Fawzi Mahomoodally
- Institute of Research and Development, Duy Tan University, Da Nang 550000, Vietnam;
- School of Engineering & Technology, Duy Tan University, Da Nang 550000, Vietnam
| | - Gokhan Zengin
- Department of Biology, Science Faculty, Selcuk University, Konya 42130, Turkey
| | - Sharmeen Jugreet
- Department of Health Sciences, Faculty of Medicine and Health Sciences, University of Mauritius, Réduit 80837, Mauritius;
| | - Evren Yildiztugay
- Department of Biotechnology, Science Faculty, Selcuk University, Konya 42130, Turkey;
| | - Andrea Fiorini
- Department of Sustainable Crop Production, Università Cattolica del Sacro Cuore, 84, 29122 Piacenza, Italy;
| | - Luigi Lucini
- Department of Sustainable Food Process, Università Cattolica del Sacro Cuore, 29122 Piacenza, Italy; (M.A.D.G.); (L.L.)
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12
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Idrissi KE, Abdoul-Hakim M, Saleh N, Garmes H, Syed A, Ríos-Gutiérrez M, Paray BA, Verma M, Zeroual A, Domingo LR. MEDT analysis of mechanism and selectivities in non-catalyzed and lewis acid-catalyzed diels-alder reactions between R-carvone and isoprene. Sci Rep 2024; 14:16827. [PMID: 39039149 PMCID: PMC11263594 DOI: 10.1038/s41598-024-67351-9] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/26/2024] [Accepted: 07/10/2024] [Indexed: 07/24/2024] Open
Abstract
Within the context of Molecular Electronic Density Theory (MEDT), this study investigates the Diels-Alder reaction among isoprene (2) and R-carvone (1R) applying DFT simulations, with and without Lewis acid (LA) catalysis. The results show that carvone (1R) acts as an electrophile and isoprene (2) as a nucleophile in a polar process. LA catalysis increases the electrophilicity of carvone, thereby improving the reactivity and selectivity of the reaction by reducing the activation Gibbs free energy. Parr functions reveal that the C5=C6 double bond is more reactive than the C9=C10 double bond, indicating chemoselectivity. The examination of the Electron Localization Function (ELF) reveals high regio- and stereoselectivity, indicating an asynchronous mechanism for the LA-catalyzed DA reaction. Furthermore, it is suggested that cycloadduct 3 has great anti-HIV potential because it exhibits lower binding energies than azidothymidine (AZT) in the docking studies of cycloadducts 3 and 4 amongst a primary HIV-1protein (1A8O plus 5W4Q).
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Affiliation(s)
- Khadija El Idrissi
- Molecular Modelling and Spectroscopy Research Team, Faculty of Science, Chouaïb Doukkali University, P.O. Box 20, 24000, El Jadida, Morocco
- Analytical Chemistry and Environmental Sciences Team, Department of Chemistry, Faculty of Science, University Chouaib Doukkali, El Jadida, Morocco
| | - Mohamed Abdoul-Hakim
- Molecular Modelling and Spectroscopy Research Team, Faculty of Science, Chouaïb Doukkali University, P.O. Box 20, 24000, El Jadida, Morocco
- Analytical Chemistry and Environmental Sciences Team, Department of Chemistry, Faculty of Science, University Chouaib Doukkali, El Jadida, Morocco
| | - Na'il Saleh
- Department of Chemistry, College of Science, United Arab Emirates University, P.O. Box 15551, Al Ain, United Arab Emirates.
| | - Hocine Garmes
- Analytical Chemistry and Environmental Sciences Team, Department of Chemistry, Faculty of Science, University Chouaib Doukkali, El Jadida, Morocco
| | - Asad Syed
- Department of Botany and Microbiology, College of Science, King Saud University, P.O. Box 2455, 11451, Riyadh, Saudi Arabia
| | - Mar Ríos-Gutiérrez
- Department of Organic Chemistry, University of Valencia, Dr. Moliner 50, 46100, Burjassot, Valencia, Spain
| | - Bilal Ahamad Paray
- Department of Zoology, College of Science, King Saud University, PO Box 2455, 11451, Riyadh, Saudi Arabia
| | - Meenakshi Verma
- University Centre for Research & Development, Department of Chemistry, Chandigarh University, Gharuan, Mohali, India
| | - Abdellah Zeroual
- Molecular Modelling and Spectroscopy Research Team, Faculty of Science, Chouaïb Doukkali University, P.O. Box 20, 24000, El Jadida, Morocco.
| | - Luis R Domingo
- Department of Organic Chemistry, University of Valencia, Dr. Moliner 50, 46100, Burjassot, Valencia, Spain
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Tan RY, Ilham Z, Wan-Mohtar WAAQI, Abdul Halim-Lim S, Ahmad Usuldin SR, Ahmad R, Adlim M. Mushroom oils: A review of their production, composition, and potential applications. Heliyon 2024; 10:e31594. [PMID: 38845934 PMCID: PMC11153096 DOI: 10.1016/j.heliyon.2024.e31594] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/23/2024] [Revised: 05/05/2024] [Accepted: 05/20/2024] [Indexed: 06/09/2024] Open
Abstract
This review delves into the world of mushroom oils, highlighting their production, composition, and versatile applications. Despite mushrooms' overall low lipid content, their fatty acid composition, rich in essential fatty acids like linoleic acid and oleic acid, proves nutritionally significant. Variations in fatty acid profiles across mushroom species and the prevalence of unsaturated fats contribute to their cardiovascular health benefits. The exploration extends to mushroom essential oils, revealing diverse volatile compounds through extraction methods like hydrodistillation and solvent-assisted flavor evaporation (SAFE). The identification of 1-octen-3-ol as a key contributor to the distinct "mushroom flavor" adds a nuanced perspective. The focus broadens to applications, encompassing culinary and industrial uses with techniques like cold pressing and supercritical fluid extraction (SFE). Mushroom oils, with their unique nutritional and flavor profiles, enhance gastronomic experiences. Non-food applications in cosmetics and biofuels underscore the oils' versatility. The nutritional composition, enriched with essential fatty acids, bioactive compositions, and trace elements, is explored for potential health benefits. Bioactive compounds such as phenolic compounds and terpenes contribute to antioxidant and anti-inflammatory properties, positioning mushroom oils as nutritional powerhouses. In short, this concise review synthesizes the intricate world of mushroom oils, emphasizing their nutritional significance, extraction methodologies, and potential health benefits. The comprehensive overview underscores mushroom oils as a promising area for further exploration and utilization. The characteristics of mushroom biomass oil for the use in various industries are influenced by the mushroom species, chemical composition, biochemical synthesis of mushroom, and downstream processes including extraction, purification and characterization. Therefore, further research and exploration need to be done to achieve a circular bioeconomy with the integration of SDGs, waste reduction, and economic stimulation, to fully utilize the benefits of mushroom, a valuable gift of nature.
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Affiliation(s)
- Rui Yeong Tan
- Biomass Energy Laboratory, Faculty of Science, Institute of Biological Sciences, Universiti Malaya, Kuala Lumpur, Malaysia
- Functional Omics and Bioprocess Development Laboratory, Faculty of Science, Institute of Biological Sciences, Universiti Malaya, Kuala Lumpur, Malaysia
| | - Zul Ilham
- Biomass Energy Laboratory, Faculty of Science, Institute of Biological Sciences, Universiti Malaya, Kuala Lumpur, Malaysia
| | - Wan Abd Al Qadr Imad Wan-Mohtar
- Functional Omics and Bioprocess Development Laboratory, Faculty of Science, Institute of Biological Sciences, Universiti Malaya, Kuala Lumpur, Malaysia
| | - Sarina Abdul Halim-Lim
- Faculty of Food Science and Technology, Universiti Putra Malaysia, 43400, Seri Kembangan, Selangor Darul Ehsan, Malaysia
| | - Siti Rokhiyah Ahmad Usuldin
- Agro-Biotechnology Institute, Malaysia (ABI), National Institutes of Biotechnology Malaysia (NIMB), HQ MARDI, 43400, Serdang, Selangor, Malaysia
| | - Rahayu Ahmad
- Halal Action Laboratory, Kolej GENIUS Insan, Universiti Sains Islam Malaysia, 71800, Nilai, Negeri Sembilan, Malaysia
| | - Muhammad Adlim
- Chemistry Department, FKIP, Universitas Syiah Kuala, Darussalam Banda Aceh, 23111, Indonesia
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14
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Vieira RV, Peiter GC, de Melo FF, Zarpelon-Schutz AC, Teixeira KN. In silico prospective analysis of the medicinal plants activity on the CagA oncoprotein from Helicobacter pylori. World J Clin Oncol 2024; 15:653-663. [PMID: 38835850 PMCID: PMC11145963 DOI: 10.5306/wjco.v15.i5.653] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 12/15/2023] [Revised: 04/01/2024] [Accepted: 04/18/2024] [Indexed: 05/21/2024] Open
Abstract
BACKGROUND Colonization with Helicobacter pylori (H. pylori) has a strong correlation with gastric cancer, and the virulence factor CagA is implicated in carcinogenesis. Studies have been conducted using medicinal plants with the aim of eliminating the pathogen; however, the possibility of blocking H. pylori-induced cell differentiation to prevent the onset and/or progression of tumors has not been addressed. This type of study is expensive and time-consuming, requiring in vitro and/or in vivo tests, which can be solved using bioinformatics. Therefore, prospective computational analyses were conducted to assess the feasibility of interaction between phenolic compounds from medicinal plants and the CagA oncoprotein. AIM To perform a computational prospecting of the interactions between phenolic compounds from medicinal plants and the CagA oncoprotein of H. pylori. METHODS In this in silico study, the structures of the phenolic compounds (ligands) kaempferol, myricetin, quercetin, ponciretin (flavonoids), and chlorogenic acid (phenolic acid) were selected from the PubChem database. These phenolic compounds were chosen based on previous studies that suggested medicinal plants as non-drug treatments to eliminate H. pylori infection. The three-dimensional structure model of the CagA oncoprotein of H. pylori (receptor) was obtained through molecular modeling using computational tools from the I-Tasser platform, employing the threading methodology. The primary sequence of CagA was sourced from GenBank (BAK52797.1). A screening was conducted to identify binding sites in the structure of the CagA oncoprotein that could potentially interact with the ligands, utilizing the GRaSP online platform. Both the ligands and receptor were prepared for molecular docking using AutoDock Tools 4 (ADT) software, and the simulations were carried out using a combination of ADT and AutoDock Vina v.1.2.0 software. Two sets of simulations were performed: One involving the central region of CagA with phenolic compounds, and another involving the carboxy-terminus region of CagA with phenolic compounds. The receptor-ligand complexes were then analyzed using PyMol and BIOVIA Discovery Studio software. RESULTS The structure model obtained for the CagA oncoprotein exhibited high quality (C-score = 0.09) and was validated using parameters from the MolProbity platform. The GRaSP online platform identified 24 residues (phenylalanine and leucine) as potential binding sites on the CagA oncoprotein. Molecular docking simulations were conducted with the three-dimensional model of the CagA oncoprotein. No complexes were observed in the simulations between the carboxy-terminus region of CagA and the phenolic compounds; however, all phenolic compounds interacted with the central region of the oncoprotein. Phenolic compounds and CagA exhibited significant affinity energy (-7.9 to -9.1 kcal/mol): CagA/kaempferol formed 28 chemical bonds, CagA/myricetin formed 18 chemical bonds, CagA/quercetin formed 16 chemical bonds, CagA/ponciretin formed 13 chemical bonds, and CagA/chlorogenic acid formed 17 chemical bonds. Although none of the phenolic compounds directly bound to the amino acid residues of the K-Xn-R-X-R membrane binding motif, all of them bound to residues, mostly positively or negatively charged, located near this region. CONCLUSION In silico, the tested phenolic compounds formed stable complexes with CagA. Therefore, they could be tested in vitro and/or in vivo to validate the findings, and to assess interference in CagA/cellular target interactions and in the oncogenic differentiation of gastric cells.
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Affiliation(s)
| | | | - Fabrício Freire de Melo
- Universidade Federal da Bahia, Instituto Multidisciplinar em Saúde-Campus Anísio Teixeira, Vitória da Conquista 45029-094, Brazil
| | - Ana Carla Zarpelon-Schutz
- Universidade Federal do Paraná, Campus Toledo, Toledo 85919-899, Brazil
- Universidade Federal do Paraná-Setor Palotina, Programa de Pós-graduação em Biotecnologia, Palotina 85950-000, Brazil
| | - Kádima Nayara Teixeira
- Universidade Federal do Paraná, Campus Toledo, Toledo 85919-899, Brazil
- Universidade Federal do Paraná-Setor Palotina, Programa de Pós-graduação em Biotecnologia, Palotina 85950-000, Brazil
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15
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Samadd MA, Hossain MJ, Zahan MS, Islam MM, Rashid MA. A comprehensive account on ethnobotany, phytochemistry and pharmacological insights of genus Celtis. Heliyon 2024; 10:e29707. [PMID: 38726115 PMCID: PMC11078770 DOI: 10.1016/j.heliyon.2024.e29707] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/21/2022] [Revised: 10/19/2023] [Accepted: 04/14/2024] [Indexed: 05/12/2024] Open
Abstract
The plants of Celtis L. genus have been traditionally used to cure aches, sore throats, fevers, cancer, sexually transmitted diseases, sexual weakness, diarrhea, stomach problems, amenorrhea, menstrual disorders, kidney stones, and pain. The review aims to give a comprehensive account of the current state of ethnopharmacology, phytochemistry, and biological activities of the Celtis genus, as well as to describe the potential area of future avenues. Information on the Celtis genus was obtained from internet sources such as Google Scholar, Web of Science, PubMed, ScienceDirect, and so on by using appropriate keywords, including ethnobotanical, pharmacological, pharmaceutical, bioactivity, phytochemistry, and botanical features of the Celtis genus. This review identified 14 species in the genus Celtis that have a phytopharmacological investigation, including C.africana Burm. f., C. australis L., C. occidentalis L., C. sinensis Pers., C. philippensis Blanco., C. tetrandra Roxb., C. tessmannii Rendle., C. jessoensis Koidz., C. adolfi-friderici Engl., C. iguanaea (Jacq.) Sarg., C. laevigata Wild., C. pallida Torr., C. zenkeri Engl., and C. tournefortii Lam. This genus contains many classified phytoconstituents, such as terpenoids, organic acids, flavonoids, and volatile compounds. Their extracts and pure substances have been shown to have the same anticancer, antibacterial, anti-inflammatory, antioxidant, hepatoprotective, cardioprotective, urease-inhibiting, and antidiarrheal properties as their traditional uses. In terms of current information on ethnopharmacology, phytochemicals, and pharmacological uses, the data acquired in this review could be beneficial and needed for future research. Some phytoconstituents (for instance, kaempferol, myricetin, quercetin, and eugenol) and extracts (for example, leaves, seeds, and ripe fruits extracts of C. australis) showed tremendous results in preliminary testing with promising antimicrobial, anticancer, and urease inhibitory effects. Further research and clinical investigations are needed to develop them as lead compounds and neutraceuticals, which may provide an advance over traditional medicinal systems.
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Affiliation(s)
- Md Abdus Samadd
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka, 1000, Bangladesh
- Department of Pharmacy, School of Pharmaceutical Sciences, State University of Bangladesh, South Purbachal, Dhaka, 1461, Bangladesh
| | - Md. Jamal Hossain
- Department of Pharmacy, School of Pharmaceutical Sciences, State University of Bangladesh, South Purbachal, Dhaka, 1461, Bangladesh
| | - Miss Sharmin Zahan
- Department of Pharmacy, School of Pharmaceutical Sciences, State University of Bangladesh, South Purbachal, Dhaka, 1461, Bangladesh
| | - Md. Monirul Islam
- Department of Pharmacy, School of Pharmaceutical Sciences, State University of Bangladesh, South Purbachal, Dhaka, 1461, Bangladesh
| | - Mohammad A. Rashid
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka, 1000, Bangladesh
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16
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Tripathi S, Rani K, Raj VS, Ambasta RK. Drug repurposing: A multi targetted approach to treat cardiac disease from existing classical drugs to modern drug discovery. PROGRESS IN MOLECULAR BIOLOGY AND TRANSLATIONAL SCIENCE 2024; 207:151-192. [PMID: 38942536 DOI: 10.1016/bs.pmbts.2024.02.001] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 06/30/2024]
Abstract
Cardiovascular diseases (CVDs) are characterized by abnormalities in the heart, blood vessels, and blood flow. CVDs comprise a diverse set of health issues. There are several types of CVDs like stroke, endothelial dysfunction, thrombosis, atherosclerosis, plaque instability and heart failure. Identification of a new drug for heart disease takes longer duration and its safety efficacy test takes even longer duration of research and approval. This chapter explores drug repurposing, nano-therapy, and plant-based treatments for managing CVDs from existing drugs which saves time and safety issues with testing new drugs. Existing drugs like statins, ACE inhibitor, warfarin, beta blockers, aspirin and metformin have been found to be useful in treating cardiac disease. For better drug delivery, nano therapy is opening new avenues for cardiac research by targeting interleukin (IL), TNF and other proteins by proteome interactome analysis. Nanoparticles enable precise delivery to atherosclerotic plaques, inflammation areas, and damaged cardiac tissues. Advancements in nano therapeutic agents, such as drug-eluting stents and drug-loaded nanoparticles are transforming CVDs management. Plant-based treatments, containing phytochemicals from Botanical sources, have potential cardiovascular benefits. These phytochemicals can mitigate risk factors associated with CVDs. The integration of these strategies opens new avenues for personalized, effective, and minimally invasive cardiovascular care. Altogether, traditional drugs, phytochemicals along with nanoparticles can revolutionize the future cardiac health care by identifying their signaling pathway, mechanism and interactome analysis.
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Affiliation(s)
- Shyam Tripathi
- Centre for Drug Design Discovery and Development (C4D), Department of Biotechnology and Microbiology, SRM University, Delhi-NCR, Rajiv Gandhi Education City, Sonepat, Haryana, India
| | - Kusum Rani
- Centre for Drug Design Discovery and Development (C4D), Department of Biotechnology and Microbiology, SRM University, Delhi-NCR, Rajiv Gandhi Education City, Sonepat, Haryana, India
| | - V Samuel Raj
- Centre for Drug Design Discovery and Development (C4D), Department of Biotechnology and Microbiology, SRM University, Delhi-NCR, Rajiv Gandhi Education City, Sonepat, Haryana, India.
| | - Rashmi K Ambasta
- Centre for Drug Design Discovery and Development (C4D), Department of Biotechnology and Microbiology, SRM University, Delhi-NCR, Rajiv Gandhi Education City, Sonepat, Haryana, India.
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17
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Slama M, Slougui N, Benaissa A, Nekkaa A, Sellam F, Canabady-Rochelle L. Borago Officinalis L.: A Review Oon Extraction, Phytochemical, and Pharmacological Activities. Chem Biodivers 2024; 21:e202301822. [PMID: 38426739 DOI: 10.1002/cbdv.202301822] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/05/2023] [Revised: 02/29/2024] [Accepted: 03/01/2024] [Indexed: 03/02/2024]
Abstract
Borago officinalis L., an annual herb belonging to the Boraginaceae family, is used in the traditional medical practices of various countries and for multiple treatments, including respiratory disorders, colds, influenza, diarrhea, cramps, inflammation, palpitation, hypertension menopause, and post-menopausal symptoms. Its pharmacological properties and biological activities - among them antioxidant, antimicrobial, anticancer, anti-inflammatory, insecticidal, antigenotoxic, and anti-obesity activity - were demonstrated in vitro and in vivo and are related to its rich content of bioactive compounds (mainly phenolic acids, flavonoids, anthocyanins, alkaloids, and terpenes) extracted from various parts of B. officinalis including leaves, flowers, seeds, and roots. This review summarizes all updated information on applied extraction processes, phytochemistry, pharmacology, and toxicity of B. officinalis.
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Affiliation(s)
- Meriem Slama
- Laboratoire de Génie des Procédés pour le Développement Durable et Les Produits de Santé, Ecole Nationale Polytechnique de Constantine, Constantine, 25016, Algeria
| | - Nabila Slougui
- Laboratoire de Bio Géochimie des Milieux Désertiques, Université Kasdi Merbah Ouargla, Route de Ghardaia, Ouargla, 30000, Algeria
- Ecole Nationale Polytechnique de Constantine, Ville Universitaire Ali Mendjeli, BP 75 A RP Ali Mendjeli, Constantine, 25016, Algeria
| | - Akila Benaissa
- Pharmaceutical Research and Sustainable Development Laboratory (ReMeDD), Department of Pharmaceutical Engineering, Faculty of Process Engineering, Constantine 3 University, Constantine, 25000, Algeria
| | - Amine Nekkaa
- Université de Lorraine, CNRS, LRGP, F-54000, Nancy, France
| | - Feriel Sellam
- Genetic diagnosis and microscopy laboratory, Health and biotechnology division, National Research Center of Biotechnology, Constantine, Algeria
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Ramírez-Santos J, Calzada F, Ordoñez-Razo RM, Mendieta-Wejebe JE, Velázquez-Domínguez JA, Argüello-García R, Velázquez C, Barbosa E. In Vivo, In Vitro and In Silico Anticancer Activity of Ilama Leaves: An Edible and Medicinal Plant in Mexico. Molecules 2024; 29:1956. [PMID: 38731446 PMCID: PMC11085222 DOI: 10.3390/molecules29091956] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/22/2024] [Revised: 04/19/2024] [Accepted: 04/22/2024] [Indexed: 05/13/2024] Open
Abstract
Ilama leaves are an important source of secondary metabolites with promising anticancer properties. Cancer is a disease that affects a great number of people worldwide. This work aimed to investigate the in vivo, in vitro and in silico anticancer properties of three acyclic terpenoids (geranylgeraniol, phytol and farnesyl acetate) isolated from petroleum ether extract of ilama leaves. Their cytotoxic activity against U-937 cells was assessed using flow cytometry to determine the type of cell death and production of reactive oxygen species (ROS). Also, a morphological analysis of the lymph nodes and a molecular docking study using three proteins related with cancer as targets, namely, Bcl-2, Mcl-1 and VEGFR-2, were performed. The flow cytometry and histomorphological analysis revealed that geranylgeraniol, phytol and farnesyl acetate induced the death of U-937 cells by late apoptosis and necrosis. Geranylgeraniol and phytol induced a significant increase in ROS production. The molecular docking studies showed that geranylgeraniol had more affinity for Bcl-2 and VEGFR-2. In the case of farnesyl acetate, it showed the best affinity for Mcl-1. This study provides information that supports the anticancer potential of geranylgeraniol, phytol and farnesyl acetate as compounds for the treatment of cancer, particularly with the potential to treat non-Hodgkin's lymphoma.
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Affiliation(s)
- Jesica Ramírez-Santos
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico; (J.R.-S.); (J.E.M.-W.); (E.B.)
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades 2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06720, Mexico
| | - Fernando Calzada
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades 2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06720, Mexico
| | - Rosa María Ordoñez-Razo
- Unidad de Investigación Médica en Genética Humana, UMAE Hospital Pediatría, 2° Piso, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06725, Mexico;
| | - Jessica Elena Mendieta-Wejebe
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico; (J.R.-S.); (J.E.M.-W.); (E.B.)
| | - José Antonio Velázquez-Domínguez
- Instituto Politécnico Nacional, Escuela Nacional de Medicina y Homeopatía, Av. Guillermo Massieu Helguera 239, La Purísima Ticoman, Gustavo A. Madero, Mexico City 07320, Mexico;
| | - Raúl Argüello-García
- Departamento de Genética y Biología Molecular, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Av. Instituto Politécnico Nacional 2508, San Pedro Zacatenco, Gustavo A. Madero, Mexico City 07360, Mexico;
| | - Claudia Velázquez
- Área Académica de Farmacia, Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Km 4.5, Carretera Pachuca-Tulancingo, Unidad Universitaria, Pachuca 42076, Mexico;
| | - Elizabeth Barbosa
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico; (J.R.-S.); (J.E.M.-W.); (E.B.)
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Trepa M, Sułkowska-Ziaja K, Kała K, Muszyńska B. Therapeutic Potential of Fungal Terpenes and Terpenoids: Application in Skin Diseases. Molecules 2024; 29:1183. [PMID: 38474692 DOI: 10.3390/molecules29051183] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/23/2023] [Revised: 03/03/2024] [Accepted: 03/04/2024] [Indexed: 03/14/2024] Open
Abstract
Terpenes and their derivatives comprise a diverse group of natural compounds with versatile medicinal properties. This article elucidates the general characteristics of fungal terpenes and terpenoids, encompassing their structure and biogenesis. The focal point of this work involves a comprehensive overview of these compounds, highlighting their therapeutic properties, mechanisms of action, and potential applications in treating specific skin conditions. Numerous isolated terpenes and terpenoids have demonstrated noteworthy anti-inflammatory and anti-microbial effects, rivalling or surpassing the efficacy of currently employed treatments for inflammation or skin infections. Due to their well-documented antioxidant and anti-cancer attributes, these compounds exhibit promise in both preventing and treating skin cancer. Terpenes and terpenoids sourced from fungi display the capability to inhibit tyrosinase, suggesting potential applications in addressing skin pigmentation disorders and cancers linked to melanogenesis dysfunctions. This paper further disseminates the findings of clinical and in vivo research on fungal terpenes and terpenoids conducted thus far.
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Affiliation(s)
- Monika Trepa
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Collegium Medicum, Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland
- Doctoral School of Medical and Health Sciences, Collegium Medicum, Jagiellonian University, 16 Św. Łazarza St., 30-530 Kraków, Poland
| | - Katarzyna Sułkowska-Ziaja
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Collegium Medicum, Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland
| | - Katarzyna Kała
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Collegium Medicum, Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland
| | - Bożena Muszyńska
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Collegium Medicum, Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland
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20
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Yuan MM, Xu F, Zheng YB, Zhou LG, Deng Y, Zhou GP, Wu X, Ji TF. Diverse terpenoid glycosides with in vitro cytotoxicity from Glechoma longituba. PHYTOCHEMISTRY 2024; 217:113923. [PMID: 37963510 DOI: 10.1016/j.phytochem.2023.113923] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 08/16/2023] [Revised: 11/05/2023] [Accepted: 11/09/2023] [Indexed: 11/16/2023]
Abstract
Terpenoids are the largest class of all known natural products, possessing structural diversity and numerous biological activities. Ten previously undescribed terpenoid glycosides, glechlongsides A-J (1-10), were isolated from the ethanol extract of the whole plant of Glechoma longituba, including diterpenoid glycoside and pentacyclic triterpenoid saponin. The structures of these compounds were characterized by extensive analysis of 1D and 2D NMR as well as HRESIMS spectra. In addition, glechlongsides F-I (6-9) exhibited weak cytotoxicity against human cancer cell lines BGC-823, Be1, HCT-8, A2780, and A549 with IC50 values ranging from 3.77 to 30.95 μM, respectively.
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Affiliation(s)
- Ming-Ming Yuan
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China
| | - Fang Xu
- State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China
| | - Yang-Bing Zheng
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China
| | - Lei-Gang Zhou
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China
| | - Yu Deng
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China
| | - Guo-Ping Zhou
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China
| | - Xi Wu
- Jiangxi Institute for Drug Control, NMPA Key Laboratory of Quality Evaluation of Traditional Chinese Patent Medicine, Jiangxi Province Engineering Research Center of Drug and Medical Device Quality, Nanchang, 330029, China.
| | - Teng-Fei Ji
- State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China; Key Laboratory of Tibetan Medicine Research, Northwest Institute of Plateau Biology, Chinese Academy of Sciences, Xining, 810008, China.
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21
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Rajendran K, Ahmed U, Meunier AC, Shaikh MF, Siddiqui R, Anwar A. Natural Terpenes Inhibit the Cytopathogenicity of Naegleria fowleri Causing Primary Amoebic Meningoencephalitis in the Human Cell Line Model. ACS Chem Neurosci 2023; 14:4105-4114. [PMID: 37983556 DOI: 10.1021/acschemneuro.3c00258] [Citation(s) in RCA: 2] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/22/2023] Open
Abstract
Naegleria fowleri is one of the free-living amoebae and is a causative agent of a lethal and rare central nervous system infection called primary amoebic meningoencephalitis. Despite the advancement in antimicrobial chemotherapy, the fatality rate in the reported cases is more than 95%. Most of the treatment drugs used against N. fowleri infection are repurposed drugs. Therefore, a large number of compounds have been tested against N. fowleri in vitro, but most of the compounds showed high toxicity. To overcome this, we evaluated the effectiveness of naturally occurring terpene compounds against N. fowleri. In this study, we evaluated the antiamoebic potential of natural compounds including Thymol, Borneol, Andrographolide, and Forskolin againstN. fowleri. Thymol showed the highest amoebicidal activity with IC50/24 h at 153.601 ± 19.6 μM. Two combinations of compounds Forskolin + Thymol and Forskolin + Borneol showed a higher effect on the viability of trophozoites as compared to compounds alone and hence showed a synergistic effect. The IC50 reported for Forskolin + Thymol was 81.30 ± 6.86 μM. Borneol showed maximum cysticidal activity with IC50/24 h at 192.605 ± 3.01 μM. Importantly, lactate dehydrogenase release testing revealed that all compounds displayed minimal cytotoxicity to human HaCaT, HeLa, and SH-SY5Y cell lines. The cytopathogenicity assay showed that Thymol and Borneol also significantly reduced the host cell cytotoxicity of pretreated amoeba toward the human HaCaT cell line. So, these terpene compounds hold potential as therapeutic agents against infections caused by N. fowleri and are potentially a step forward in drug development against this deadly pathogen as these compounds have also been reported to cross the blood-brain barrier. Therefore, an in vivo study using animal models is necessary to assess the efficacy of these compounds and the need for further research into the intranasal route of delivery for the treatment of these life-threatening infections.
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Affiliation(s)
- Kavitha Rajendran
- School of American Education (SAE), Sunway University, Subang Jaya, Selangor 47500, Malaysia
| | - Usman Ahmed
- Department of Biological Sciences, School of Medical and Life Sciences, Sunway University, Subang Jaya, Selangor 47500, Malaysia
| | - Alexia Chloe Meunier
- Department of Biological Sciences, School of Medical and Life Sciences, Sunway University, Subang Jaya, Selangor 47500, Malaysia
| | - Mohd Farooq Shaikh
- Neuropharmacology Research Laboratory, Jeffrey Cheah School of Medicine and Health Sciences, Monash University Malaysia, Bandar Sunway 47500, Malaysia
- School of Dentistry and Medical Sciences, Charles Sturt University, Orange New South Wales, 2800, Australia
| | - Ruqaiyyah Siddiqui
- Department of Microbiota Research Centre, Istinye University, Istanbul 34010, Turkey
| | - Ayaz Anwar
- Department of Biological Sciences, School of Medical and Life Sciences, Sunway University, Subang Jaya, Selangor 47500, Malaysia
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22
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Malczak I, Gajda A. Interactions of naturally occurring compounds with antimicrobials. J Pharm Anal 2023; 13:1452-1470. [PMID: 38223447 PMCID: PMC10785267 DOI: 10.1016/j.jpha.2023.09.014] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/23/2023] [Revised: 09/12/2023] [Accepted: 09/19/2023] [Indexed: 01/16/2024] Open
Abstract
Antibiotics are among the most often used medications in human healthcare and agriculture. Overusing these substances can lead to complications such as increasing antibiotic resistance in bacteria or a toxic effect when administering large amounts. To solve these problems, new solutions in antibacterial therapy are needed. The use of natural products in medicine has been known for centuries. Some of them have antibacterial activity, hence the idea to combine their activity with commercial antibiotics to reduce the latter's use. This review presents collected information on natural compounds (terpenes, alkaloids, flavonoids, tannins, sulfoxides, and mycotoxins), of which various drug interactions have been observed. Many of the indicated compounds show synergistic or additive interactions with antibiotics, which suggests their potential for use in antibacterial therapy, reducing the toxicity of the antibiotics used and the risk of further development of bacterial resistance. Unfortunately, there are also compounds which interact antagonistically, potentially hindering the therapy of bacterial infection. Depending on its mechanism of action, each compound can behave differently in combination with different antibiotics and when acting against various bacterial strains.
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Affiliation(s)
- Izabela Malczak
- Department of Pharmacology and Toxicology, National Veterinary Research Institute, Partyzantów 57, 24-100, Poland
| | - Anna Gajda
- Department of Pharmacology and Toxicology, National Veterinary Research Institute, Partyzantów 57, 24-100, Poland
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23
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Okey SA, Waddell JT, Shah RV, Kennedy GM, Frangos MP, Corbin WR. An Ecological Examination of Indica Versus Sativa and Primary Terpenes on the Subjective Effects of Smoked Cannabis: A Preliminary Investigation. Cannabis Cannabinoid Res 2023; 8:857-866. [PMID: 36648357 DOI: 10.1089/can.2022.0213] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/18/2023] Open
Abstract
Background: The legal cannabis landscape has greatly outpaced scientific knowledge. Many popular cannabis claims, such as cultivar (colloquially referred to as strain) classification and terpene content producing different subjective effects, are unsubstantiated. This study examined, for the first time, whether cultivar classification (sativa/indica) and terpene content (caryophyllene, limonene, myrcene, pinene, and terpinolene) were associated with subjective cannabis effects (i.e., pain levels, low-arousal ["indica-like"] effects, high-arousal ["sativa-like"] effects, and negative effects). Methods: Regular cannabis users (n=101) took part in a 2-week long ecological momentary assessment study in which they responded to questions about their cannabis use, stated their preference for sativa versus indica, and reported their in-the-moment subjective effects within 30 min of smoking cannabis. Cultivars were coded for sativa versus indica classification and primary terpene content using Leafly, a popular search engine. Linear mixed-effect models then examined subjective response by sativa/indica and primary terpene. Covariates included demographics (age, sex, race, income), cannabis use (medical use, cannabis use frequency, stated preference for sativa/indica, global expected cannabis effects), morning pain ratings, and specific smoked cannabis occasions (hour of day, minutes since use, context, number of hits, and tetrahydrocannabinol). Results: The majority of participants (78.3%) had a preference for either sativa or indica and reported reasons for their preference that aligned with industry claims. After controlling for covariates, findings revealed that cultivars classified as indica dominant were associated with greater low-arousal (e.g., sluggish, slow) effects relative to the unweighted mean of all cannabis cultivars (b = 0.44, SE=0.16, p=0.01). Cultivars with primary caryophyllene were associated with greater pain ratings (b = 0.53, SE=0.24, p=0.03) and negative effects (b = 0.22, SE=0.08, p=0.01) relative to the mean of all other terpene types. Cultivars with primary pinene were associated with less negative effects (b = -0.35, SE=0.18, p=0.04). Conclusions: Cultivars classified as indica dominant were associated with greater low-arousal effects in models that accounted for both within- and between-person variation, despite the scientific challenges distinguishing between sativa and indica. Preliminary findings also suggest terpenes may play a role in subjective effects. These results emphasize the need for further research, particularly controlled lab studies.
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Affiliation(s)
- Sarah A Okey
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
| | - Jack T Waddell
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
| | - Rishika V Shah
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
| | - Gillian M Kennedy
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
| | - Maria P Frangos
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
| | - William R Corbin
- Department of Psychology, Arizona State University, Tempe, Arizona, USA
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24
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Sheng T, Kang G, Zhuang Z, Chekshin N, Wang Z, Hu L, Yu JQ. Synthesis of β,γ-Unsaturated Aliphatic Acids via Ligand-Enabled Dehydrogenation. J Am Chem Soc 2023; 145:20951-20958. [PMID: 37698388 PMCID: PMC11152581 DOI: 10.1021/jacs.3c06423] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 09/13/2023]
Abstract
α,β-Dehydrogenation of aliphatic acids has been realized through both enolate and β-C-H metalation pathways. However, the synthesis of isolated β,γ-unsaturated aliphatic acids via dehydrogenation has not been achieved to date. Herein, we report the ligand-enabled β,γ-dehydrogenation of abundant and inexpensive free aliphatic acids, which provides a new synthetic disconnection as well as a versatile platform for the downstream functionalization of complex molecules at remote γ-sites. A variety of free aliphatic acids, including acyclic and cyclic systems with ring sizes from five-membered to macrocyclic, undergo efficient dehydrogenation. Notably, this protocol features good chemoselectivity in the presence of more accessible α-C-H bonds and excellent regioselectivity in fused bicyclic scaffolds. The utility of this protocol has been demonstrated by the late-stage functionalization of a series of bioactive terpene natural products at the γ-sites. Further functionalization of the β,γ-double bond allows for the installation of covalent warheads, including epoxides, aziridines, and β-lactones, into complex natural product scaffolds, which are valuable for targeted covalent drug discovery.
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Affiliation(s)
- Tao Sheng
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Guowei Kang
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Zhe Zhuang
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Nikita Chekshin
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Zhen Wang
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Liang Hu
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
| | - Jin-Quan Yu
- Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, United States
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Han W, Jiao Y, Mi S, Han S, Xu J, Li S, Liu Y, Guo L. Stevioside reduces inflammation in periodontitis by changing the oral bacterial composition and inhibiting P. gingivalis in mice. BMC Oral Health 2023; 23:550. [PMID: 37563632 PMCID: PMC10416424 DOI: 10.1186/s12903-023-03229-y] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/12/2023] [Accepted: 07/14/2023] [Indexed: 08/12/2023] Open
Abstract
BACKGROUND Excessive sugar intake has become a major challenge in modern societies. Stevioside is a promising non-calorie sweetener with anti-inflammatory effects; however, its effects on the oral environment and periodontitis remain unclear. Therefore, this study explores the effect of stevioside on periodontitis in mice. METHODS Mice were divided into four groups, namely, control, treated with water, and periodontitis models, established using 5 - 0 silk sutures ligation around the second molar then infected the oral cavity with Porphyromonas gingivalis (P. gingivalis) viscous suspension, divided into three groups treated with 0.1% stevioside (P + S), 10% glucose (P + G), or water (P). Micro-CT scanning was used to assess alveolar bone resorption, while RT-PCR was used to evaluate the inflammatory factors expression and P. gingivalis invasion in the gingiva. The composition of the oral bacteria was analysed using 16 S rRNA sequence in the saliva. In addition, P. gingivalis was co-cultured with stevioside at different concentrations in vitro, and bacterial activity was detected via optical density values and live/dead staining. The virulence was detected using RT-PCR, while biofilm formation was detected using scanning electron microscopy. RESULTS Compared with 10% glucose, treatment with 0.1% stevioside reduced alveolar bone absorption and osteoclasts while decreasing IL-6, TNF-α, IL-1β, and P. gingivalis in the gingiva of periodontitis mice. The CEJ-ABC distance in the P + S group was significantly lower than that in the P and P + G groups (P < 0.05). Moreover, the composition of the oral bacteria in the P + S group was similar to that of the control. In vitro stevioside treatment also reduced the bacterial activity and toxicity of P. gingivalis in a dose-dependent manner and affected its biofilm composition. CONCLUSION Our results indicate that, compared with 10% glucose, 0.1% stevioside intake can reduce alveolar bone resorption and inflammation in periodontal tissues in mice; the bacterial composition following 0.1% stevioside intake was similar to that of a healthy environment. In vitro, high concentrations of stevioside reduced P. gingivalis activity, biofilm formation, and virulence expression. Therefore, stevioside is a potential alternative to glucose for patients with periodontitis.
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Affiliation(s)
- Wenrui Han
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China
| | - Yao Jiao
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China
| | - Sicong Mi
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China
| | - Shu Han
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China
| | - Junji Xu
- Laboratory of Tissue Regeneration and Immunology and Department of Periodontics, Beijing Key Laboratory of Tooth Regeneration and Function Reconstruction, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China
| | - Song Li
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China.
| | - Yi Liu
- Laboratory of Tissue Regeneration and Immunology and Department of Periodontics, Beijing Key Laboratory of Tooth Regeneration and Function Reconstruction, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China.
| | - Lijia Guo
- Department of Orthodontics, School of Stomatology, Capital Medical University, Tian Tan Xi Li No.4, Beijing, 100050, People's Republic of China.
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Ashraf MV, Pant S, Khan MAH, Shah AA, Siddiqui S, Jeridi M, Alhamdi HWS, Ahmad S. Phytochemicals as Antimicrobials: Prospecting Himalayan Medicinal Plants as Source of Alternate Medicine to Combat Antimicrobial Resistance. Pharmaceuticals (Basel) 2023; 16:881. [PMID: 37375828 DOI: 10.3390/ph16060881] [Citation(s) in RCA: 15] [Impact Index Per Article: 7.5] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/14/2023] [Revised: 06/10/2023] [Accepted: 06/12/2023] [Indexed: 06/29/2023] Open
Abstract
Among all available antimicrobials, antibiotics hold a prime position in the treatment of infectious diseases. However, the emergence of antimicrobial resistance (AMR) has posed a serious threat to the effectiveness of antibiotics, resulting in increased morbidity, mortality, and escalation in healthcare costs causing a global health crisis. The overuse and misuse of antibiotics in global healthcare setups have accelerated the development and spread of AMR, leading to the emergence of multidrug-resistant (MDR) pathogens, which further limits treatment options. This creates a critical need to explore alternative approaches to combat bacterial infections. Phytochemicals have gained attention as a potential source of alternative medicine to address the challenge of AMR. Phytochemicals are structurally and functionally diverse and have multitarget antimicrobial effects, disrupting essential cellular activities. Given the promising results of plant-based antimicrobials, coupled with the slow discovery of novel antibiotics, it has become highly imperative to explore the vast repository of phytocompounds to overcome the looming catastrophe of AMR. This review summarizes the emergence of AMR towards existing antibiotics and potent phytochemicals having antimicrobial activities, along with a comprehensive overview of 123 Himalayan medicinal plants reported to possess antimicrobial phytocompounds, thus compiling the existing information that will help researchers in the exploration of phytochemicals to combat AMR.
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Affiliation(s)
- Mohammad Vikas Ashraf
- Department of Biotechnology, School of Biosciences and Biotechnology, Baba Ghulam Shah Badshah University, Rajouri 185 234, India
| | - Shreekar Pant
- Centre for Biodiversity Studies, School of Biosciences and Biotechnology, Baba Ghulam Shah Badshah University, Rajouri 185 234, India
| | - M A Hannan Khan
- Department of Zoology, School of Biosciences and Biotechnology, Baba Ghulam Shah Badshah University, Rajouri 185 234, India
| | - Ali Asghar Shah
- Department of Zoology, School of Biosciences and Biotechnology, Baba Ghulam Shah Badshah University, Rajouri 185 234, India
| | - Sazada Siddiqui
- Department of Biology, College of Science, King Khalid University, Abha 61413, Saudi Arabia
| | - Mouna Jeridi
- Department of Biology, College of Science, King Khalid University, Abha 61413, Saudi Arabia
| | | | - Shoeb Ahmad
- Department of Biotechnology, School of Biosciences and Biotechnology, Baba Ghulam Shah Badshah University, Rajouri 185 234, India
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Jasmins G, Perestrelo R, Coïsson JD, Sousa P, Teixeira JA, Bordiga M, Câmara JS. Tracing the Volatilomic Fingerprint of the Most Popular Italian Fortified Wines. Foods 2023; 12:foods12102058. [PMID: 37238876 DOI: 10.3390/foods12102058] [Citation(s) in RCA: 2] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/21/2023] [Revised: 04/14/2023] [Accepted: 05/11/2023] [Indexed: 05/28/2023] Open
Abstract
The aim of the current study was to provide a useful platform to identify characteristic molecular markers related to the authenticity of Italian fortified wines. For this purpose, the volatilomic fingerprint of the most popular Italian fortified wines was established using headspace solid-phase microextraction combined with gas chromatography-mass spectrometry (HS-SPME/GC-MS). Several volatile organic compounds (VOCs), belonging with distinct chemical groups, were identified, ten of which are common to all the analyzed fortified Italian wines. Terpenoids were the most abundant chemical group in Campari bitter wines due to limonene's high contribution to the total volatilomic fingerprint, whereas for Marsala wines, alcohols and esters were the most predominant chemical groups. The fortified Italian wines VOCs network demonstrated that the furanic compounds 2-furfural, ethyl furoate, and 5-methyl-2-furfural, constitute potential molecular markers of Marsala wines, while the terpenoids nerol, α-terpeniol, limonene, and menthone isomers, are characteristic of Vermouth wines. In addition, butanediol was detected only in Barolo wines, and β-phellandrene and β-myrcene only in Campari wines. The obtained data reveal an adequate tool to establish the authenticity and genuineness of Italian fortified wines, and at the same time constitute a valuable contribution to identify potential cases of fraud or adulteration to which they are subject, due to the high commercial value associated with these wines. In addition, they contribute to the deepening of scientific knowledge that supports its valorization and guarantee of quality and safety for consumers.
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Affiliation(s)
- Gonçalo Jasmins
- CQM-Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
| | - Rosa Perestrelo
- CQM-Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
| | - Jean Daniel Coïsson
- Department of Pharmaceutical Sciences, Università degli Studi del Piemonte Orientale "A. Avogadro", Largo Donegani 2, 28100 Novara, Italy
| | - Patrícia Sousa
- CQM-Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
| | - José A Teixeira
- CEB-Centre of Biological Engineering, University of Minho, Campus Gualtar, 4710-057 Braga, Portugal
- LABBELS-Associate Laboratory, University of Minho, Campus Gualtar, 4710-057 Braga, Portugal
| | - Matteo Bordiga
- Department of Pharmaceutical Sciences, Università degli Studi del Piemonte Orientale "A. Avogadro", Largo Donegani 2, 28100 Novara, Italy
| | - José S Câmara
- CQM-Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
- Departamento de Química, Faculdade de Ciências Exatas e Engenharia, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
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28
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Capitain CC, Zischka M, Sirkeci C, Weller P. Evaluation of IMS drift tube temperature on the peak shape of high boiling fragrance compounds towards allergen detection in complex cosmetic products and essential oils. Talanta 2023; 257:124397. [PMID: 36858010 DOI: 10.1016/j.talanta.2023.124397] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/30/2022] [Revised: 02/22/2023] [Accepted: 02/23/2023] [Indexed: 02/26/2023]
Abstract
Gas chromatography-ion mobility spectrometry (GC-IMS) has recently gained increasing attention for the analysis of volatile compounds due to its high sensitivity, selectivity, and robust design. Peak shape distortion, including peak tailing or broadening, are well known challenges in chromatographic analysis that result in peak asymmetry and decreased resolution. However, in IMS analysis peak tailing, which is independent on the column separation technique, have also been observed. As high boiling substances, such as monoterpenes, are mainly affected by enlarged peak tailing in GC-IMS, we propose that condensation or adsorption effects within the "cold" IMS cell, which is commonly operated at 45 °C-90 °C, are the root cause. To avoid condensation and to decrease peak tailing, we used a prototypic high temperature ion mobility spectrometry (HTIMS) in this work, which allows an increase of the IMS drift tube temperature up to 180 °C. This HTIMS was coupled to a GC column separation and used to analyse the peak shape of homologues series of ketones, alcohols, aldehydes, as well as high boiling fragrance compounds, such as monoterpenes and phenylpropanoids. While we were able to show that an increased IMS drift tube temperatures correlates well with improved peak shapes, the GC parameters of the HS-GC-HTIMS method, however, were found to have little effect on the peak shapes in IMS spectra. In particular monoterpenes, which display intense peak tailing at lower IMS drift tube temperatures, show significant improvement of the peak shape at higher IMS drift tube temperatures. This leads to the assumption that high boiling substances indeed undergo condensation effects within the IMS cell at low drift tube temperatures. For many separation tasks, such as the separation of the phenylpropanoids eugenol and isoeugenol, comparably low IMS temperatures of 120 °C are already sufficient to achieve a resolution above 1.5. However, the optimal drift tube temperature is dependent on the substance class. While the aspect ratio increases steadily for most monoterpenes, phenylpropanoids and aldehyde monomer peaks investigated, an optimal aspect ratio was found for ketones between 140 °C and 160 °C and alcohols between 120 °C and 140 °C. Lastly, the change of the reduced mobility K0 with the increase of drift tube temperature was analysed. Compounds with similar chemical structure, such as the alcoholic monoterpenes citronellol and geraniol or the phenylpropanoids eugenol and isoeugenol show similar shifts of the K0 value. Substances which differ in their chemical structure, such as the aldehyde monoterpenes citral and cinnamal have substantially different shifts of the K0 value. With a future large substance database, the temperature dependant slope of the K0 value of a substance could be used to identify the substance groups of unknown molecules. Furthermore, substances with the same drift time but different chemical composition could be separable through a change in drift tube temperature.
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Affiliation(s)
- Charlotte C Capitain
- Institute for Instrumental Analytics and Bioanalytics, Mannheim University of Applied Sciences, 68163 Mannheim, Germany
| | - Martin Zischka
- Institute for Instrumental Analytics and Bioanalytics, Mannheim University of Applied Sciences, 68163 Mannheim, Germany
| | - Cengiz Sirkeci
- G.A.S. Gesellschaft für Analytische Sensorsysteme mbH, 44227 Dortmund, Germany
| | - Philipp Weller
- Institute for Instrumental Analytics and Bioanalytics, Mannheim University of Applied Sciences, 68163 Mannheim, Germany.
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Abdul Ghani MA, Ugusman A, Latip J, Zainalabidin S. Role of Terpenophenolics in Modulating Inflammation and Apoptosis in Cardiovascular Diseases: A Review. Int J Mol Sci 2023; 24:ijms24065339. [PMID: 36982410 PMCID: PMC10049039 DOI: 10.3390/ijms24065339] [Citation(s) in RCA: 22] [Impact Index Per Article: 11.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/30/2022] [Revised: 02/17/2023] [Accepted: 02/18/2023] [Indexed: 03/14/2023] Open
Abstract
One in every three deaths worldwide is caused by cardiovascular diseases (CVDs), estimating a total of 17.9 million deaths annually. By 2030, it is expected that more than 24 million people will die from CVDs related complications. The most common CVDs are coronary heart disease, myocardial infarction, stroke, and hypertension. A plethora of studies has shown inflammation causing both short-term and long-term damage to the tissues in many organ systems, including the cardiovascular system. In parallel to inflammation processes, it has been discovered that apoptosis, a mode of programmed cell death, may also contribute to CVD development due to the loss of cardiomyocytes. Terpenophenolic compounds are comprised of terpenes and natural phenols as secondary metabolites by plants and are commonly found in the genus Humulus and Cannabis. A growing body of evidence has shown that terpenophenolic compounds exhibit protective properties against inflammation and apoptosis within the cardiovascular system. This review highlights the current evidence elucidating the molecular actions of terpenophenolic compounds in protecting the cardiovascular system, i.e., bakuchiol, ferruginol, carnosic acid, carnosol, carvacrol, thymol and hinokitiol. The potential of these compounds is discussed as the new nutraceutical drugs that may help to decrease the burden of cardiovascular disorders.
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Affiliation(s)
- Muhamad Adib Abdul Ghani
- Programme of Biomedical Sciences, Centre of Toxicology and Health Risk Study, Faculty of Health Sciences, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, Malaysia
| | - Azizah Ugusman
- Department of Physiology, Faculty of Medicine, Universiti Kebangsaan Malaysia, Kuala Lumpur 56000, Malaysia
| | - Jalifah Latip
- Department of Chemical Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia, Bangi 43600, Malaysia
- Correspondence: (J.L.); (S.Z.); Tel.: +60-38921-1875 (J.L.); +60-39289-7684 (S.Z.)
| | - Satirah Zainalabidin
- Programme of Biomedical Sciences, Centre of Toxicology and Health Risk Study, Faculty of Health Sciences, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, Malaysia
- Correspondence: (J.L.); (S.Z.); Tel.: +60-38921-1875 (J.L.); +60-39289-7684 (S.Z.)
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30
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de Oliveira LMG, Carreira RB, de Oliveira JVR, do Nascimento RP, Dos Santos Souza C, Trias E, da Silva VDA, Costa SL. Impact of Plant-Derived Compounds on Amyotrophic Lateral Sclerosis. Neurotox Res 2023; 41:288-309. [PMID: 36800114 DOI: 10.1007/s12640-022-00632-1] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/23/2022] [Revised: 09/23/2022] [Accepted: 12/29/2022] [Indexed: 02/18/2023]
Abstract
Amyotrophic lateral sclerosis (ALS) is a fatal illness characterized by progressive motor neuron degeneration. Conventional therapies for ALS are based on treatment of symptoms, and the disease remains incurable. Molecular mechanisms are unclear, but studies have been pointing to involvement of glia, neuroinflammation, oxidative stress, and glutamate excitotoxicity as a key factor. Nowadays, we have few treatments for this disease that only delays death, but also does not stop the neurodegenerative process. These treatments are based on glutamate blockage (riluzole), tyrosine kinase inhibition (masitinib), and antioxidant activity (edaravone). In the past few years, plant-derived compounds have been studied for neurodegenerative disorder therapies based on neuroprotection and glial cell response. In this review, we describe mechanisms of action of natural compounds associated with neuroprotective effects, and the possibilities for new therapeutic strategies in ALS.
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Affiliation(s)
- Lucas Matheus Gonçalves de Oliveira
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil
| | - Rodrigo Barreto Carreira
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil
| | - Juciele Valeria Ribeiro de Oliveira
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil
| | - Ravena Pereira do Nascimento
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil
| | - Cleide Dos Santos Souza
- Sheffield Institute for Translational Neuroscience (SITraN), University of Sheffield, Sheffield, UK
| | | | - Victor Diogenes Amaral da Silva
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil.
| | - Silvia Lima Costa
- Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, Federal University of Bahia, Salvador, Bahia, 40110-100, Brazil.
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31
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Cuzzucoli Crucitti V, Ilchev A, Moore JC, Fowler HR, Dubern JF, Sanni O, Xue X, Husband BK, Dundas AA, Smith S, Wildman JL, Taresco V, Williams P, Alexander MR, Howdle SM, Wildman RD, Stockman RA, Irvine DJ. Predictive Molecular Design and Structure-Property Validation of Novel Terpene-Based, Sustainably Sourced Bacterial Biofilm-Resistant Materials. Biomacromolecules 2023; 24:576-591. [PMID: 36599074 PMCID: PMC9930090 DOI: 10.1021/acs.biomac.2c00721] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/06/2023]
Abstract
Presented in this work is the use of a molecular descriptor, termed the α parameter, to aid in the design of a series of novel, terpene-based, and sustainable polymers that were resistant to biofilm formation by the model bacterial pathogen Pseudomonas aeruginosa. To achieve this, the potential of a range of recently reported, terpene-derived monomers to deliver biofilm resistance when polymerized was both predicted and ranked by the application of the α parameter to key features in their molecular structures. These monomers were derived from commercially available terpenes (i.e., α-pinene, β-pinene, and carvone), and the prediction of the biofilm resistance properties of the resultant novel (meth)acrylate polymers was confirmed using a combination of high-throughput polymerization screening (in a microarray format) and in vitro testing. Furthermore, monomers, which both exhibited the highest predicted biofilm anti-biofilm behavior and required less than two synthetic stages to be generated, were scaled-up and successfully printed using an inkjet "valve-based" 3D printer. Also, these materials were used to produce polymeric surfactants that were successfully used in microfluidic processing to create microparticles that possessed bio-instructive surfaces. As part of the up-scaling process, a novel rearrangement was observed in a proposed single-step synthesis of α-terpinyl methacrylate via methacryloxylation, which resulted in isolation of an isobornyl-bornyl methacrylate monomer mixture, and the resultant copolymer was also shown to be bacterial attachment-resistant. As there has been great interest in the current literature upon the adoption of these novel terpene-based polymers as green replacements for petrochemical-derived plastics, these observations have significant potential to produce new bio-resistant coatings, packaging materials, fibers, medical devices, etc.
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Affiliation(s)
- Valentina Cuzzucoli Crucitti
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Aleksandar Ilchev
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Jonathan C Moore
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Harriet R Fowler
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Jean-Frédéric Dubern
- National Biofilms Innovation Centre, Biodiscovery Institute and School of Life Sciences, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Olutoba Sanni
- Advanced Materials and Healthcare Technologies, School of Pharmacy, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Xuan Xue
- Advanced Materials and Healthcare Technologies, School of Pharmacy, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Bethany K Husband
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Adam A Dundas
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Sean Smith
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Joni L Wildman
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Vincenzo Taresco
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Paul Williams
- National Biofilms Innovation Centre, Biodiscovery Institute and School of Life Sciences, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Morgan R Alexander
- Advanced Materials and Healthcare Technologies, School of Pharmacy, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Steven M Howdle
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Ricky D Wildman
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Robert A Stockman
- School of Chemistry, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
| | - Derek J Irvine
- Centre of Additive Manufacturing, Department of Chemical and Environmental Engineering, University of Nottingham, University Park, NottinghamNG7 2RD, U.K
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32
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Prakash J. Secondary Metabolites From Plants for Cardiovascular Disease. ADVANCES IN MEDICAL DIAGNOSIS, TREATMENT, AND CARE 2023:155-171. [DOI: 10.4018/978-1-6684-6737-4.ch010] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 01/06/2025]
Abstract
One of the leading causes of mortality worldwide is cardiac vascular disease. According to the WHO report, CVDs affect 17.9 million people each year and will affect 22.2 million people by 2030. The plants include flavonoids, polyphenols, plant Sulphur compounds, and terpenoids, which are all active phytochemicals. Recent research has revealed that flavonoids are substances with strong biological effects that may help prevent chronic illnesses including cardiovascular disease. The prevention of low-density lipoprotein oxidation, which encourages vasodilatation, is a common flavonoid mode of action. Due to the rising frequency of CVD, numerous plants have been identified to contain a number of physiologically active chemicals with known biological effects; however, proper CVD preventive and treatment approaches are still needed. This study aims to emphasize the cardiovascular risk factors, in addition to explaining the processes through which naturally occurring bioactive chemicals exhibit their cardiovascular preventive effects.
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Affiliation(s)
- Jose Prakash
- B.S. Abdur Rahman Crescent Insititute of Science and Technology, India
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33
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Singh A, Prakash A, Choudhary R. Bioactive Components Having Antimicrobial and Anticancerous Properties: A Review. BIOACTIVE COMPONENTS 2023:271-299. [DOI: 10.1007/978-981-19-2366-1_17] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 01/04/2025]
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34
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Liu Z, Gao H, Zhao Z, Huang M, Wang S, Zhan J. Status of research on natural protein tyrosine phosphatase 1B inhibitors as potential antidiabetic agents: Update. Biomed Pharmacother 2023; 157:113990. [PMID: 36459712 DOI: 10.1016/j.biopha.2022.113990] [Citation(s) in RCA: 18] [Impact Index Per Article: 9.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/10/2022] [Revised: 10/29/2022] [Accepted: 11/07/2022] [Indexed: 12/02/2022] Open
Abstract
Protein tyrosine phosphatase 1B (PTP1B) is a crucial therapeutic target for multiple human diseases comprising type 2 diabetes (T2DM) and obesity because it is a seminal part of a negative regulator in both insulin and leptin signaling pathways. PTP1B inhibitors increase insulin receptor sensitivity and have the ability to cure insulin resistance-related diseases. However, the few PTP1B inhibitors that entered the clinic (Ertiprotafib, ISIS-113715, Trodusquemine, and JTT-551) were discontinued due to side effects or low selectivity. Molecules with broad chemical diversity extracted from natural products have been reported to be potent PTP1B inhibitors with few side effects. This article summarizes the recent PTP1B inhibitors extracted from natural products, clarifying the current research progress, and providing new options for designing new and effective PTP1B inhibitors.
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Affiliation(s)
- Zhenyang Liu
- School of Life Science, Ludong University, Yantai, Shandong 264025, China
| | - Hongwei Gao
- School of Life Science, Ludong University, Yantai, Shandong 264025, China.
| | - Ziyu Zhao
- School of Life Science, Ludong University, Yantai, Shandong 264025, China
| | - Mengrui Huang
- School of Life Science, Ludong University, Yantai, Shandong 264025, China
| | - Shengnan Wang
- School of Life Science, Ludong University, Yantai, Shandong 264025, China
| | - Jiuyu Zhan
- School of Life Science, Ludong University, Yantai, Shandong 264025, China.
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35
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Oliveira RC, Bandeira PN, Lemos TLG, Dos Santos HS, Scherf JR, Rocha JE, Pereira RLS, Freitas TS, Freitas PR, Pereira-Junior FN, Marinho MM, Marinho EM, Marinho ES, Nogueira CES, Coutinho HDM, Teixeira AMR. In silico and in vitro evaluation of efflux pumps inhibition of α,β-amyrin. J Biomol Struct Dyn 2022; 40:12785-12799. [PMID: 34528866 DOI: 10.1080/07391102.2021.1976277] [Citation(s) in RCA: 11] [Impact Index Per Article: 3.7] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/27/2022]
Abstract
The use of the bacterial efflux pump mechanism to reduce the concentrations of antibiotics in the intracellular to the extracellular region is one of the main mechanisms by which bacteria acquire resistance to antibiotics. The present study aims to evaluate the antibacterial activity of the α,β-amyrin mixture isolated from Protium heptaphyllum against the multidrug-resistant strains of Escherichia coli 06 and Staphylococcus aureus 10, and to verify the inhibition of the efflux resistance mechanisms against the strains of S. aureus 1199B and K2068, carrying the NorA and MepA efflux pumps, respectively. The α,β-amyrin did not show clinically relevant direct bacterial activity. However, the α,β-amyrin when associated with the gentamicin antibiotic presented synergistic effect against the multidrug-resistant bacterial strain of S. aureus 10. In strains with efflux pumps, α,β-amyrin was able to inhibit the action of the efflux protein NorA against Ethidium Bromide. However, this inhibitory effect was not observed in the MepA efflux pump. In addition, when evaluating the effect of standard efflux pump inhibitors, clorptomazine and CCCP, α,β-amyrin showed a decrease in MIC, demonstrating the presence of the efflux mechanism through synergism. Docking studies indicate that α, β-amyrin have a higher affinity energy to MepA, and NorA than ciprofloxacin and norfloxacin. Also, α, β-amyrin bind to the same region of the binding site as these antibiotics. It was concluded that the α, β-amyrin has the potential to increase antibacterial activity with the association of antibiotics, together with the ability to be a strong candidate for an efflux pump inhibitor.Communicated by Ramaswamy H. Sarma.
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Affiliation(s)
- Raíssa C Oliveira
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Paulo N Bandeira
- Science and Technology Centre, Course of Chemistry, State University Vale do Acaraú, Sobral, CE, Brazil
| | - Telma L G Lemos
- Department of Organic and Inorganic Chemistry, Federal University of Ceará, Fortaleza, CE, Brazil
| | - Hélcio S Dos Santos
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil.,Science and Technology Centre, Course of Chemistry, State University Vale do Acaraú, Sobral, CE, Brazil
| | - Jackelyne R Scherf
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Janaina E Rocha
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Raimundo L S Pereira
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Thiago S Freitas
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Priscila R Freitas
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Francisco N Pereira-Junior
- Center of Agricultural Sciences and of the Biodiversity, Federal University of Cariri, Juazeiro do Norte, CE, Brazil
| | - Márcia M Marinho
- Faculty of Education, Sciences and Letters of Iguatu, State University of Ceará, Campus FECLI, Iguatu, CE, Brazil
| | - Emanuelle M Marinho
- Department of Analytical Chemistry and Physical Chemistry, Federal University of Ceará, Fortaleza, CE, Brazil
| | - Emmanuel S Marinho
- Group of Theoretical Chemistry and Electrochemistry, State University of Ceará, Campus FAFIDAM, Limoeiro do Norte, CE, Brazil
| | - Carlos E S Nogueira
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil.,Department of Physics, Regional University of Cariri, Juazeiro do Norte, CE, Brazil
| | - Henrique D M Coutinho
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil
| | - Alexandre M R Teixeira
- Graduate Program in Biological Chemistry, Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil.,Department of Physics, Regional University of Cariri, Juazeiro do Norte, CE, Brazil
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36
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Carr S, Buan NR. Insights into the biotechnology potential of Methanosarcina. Front Microbiol 2022; 13:1034674. [PMID: 36590411 PMCID: PMC9797515 DOI: 10.3389/fmicb.2022.1034674] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/01/2022] [Accepted: 10/28/2022] [Indexed: 12/23/2022] Open
Abstract
Methanogens are anaerobic archaea which conserve energy by producing methane. Found in nearly every anaerobic environment on earth, methanogens serve important roles in ecology as key organisms of the global carbon cycle, and in industry as a source of renewable biofuels. Environmentally, methanogenic archaea play an essential role in the reintroducing unavailable carbon to the carbon cycle by anaerobically converting low-energy, terminal metabolic degradation products such as one and two-carbon molecules into methane which then returns to the aerobic portion of the carbon cycle. In industry, methanogens are commonly used as an inexpensive source of renewable biofuels as well as serving as a vital component in the treatment of wastewater though this is only the tip of the iceberg with respect to their metabolic potential. In this review we will discuss how the efficient central metabolism of methanoarchaea could be harnessed for future biotechnology applications.
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Affiliation(s)
| | - Nicole R. Buan
- Department of Biochemistry, University of Nebraska-Lincoln, Lincoln, NE, United States
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37
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Insight for the photochemical reaction of 4-aryl-4H-pyran: Experimental and theoretical studies. Tetrahedron 2022. [DOI: 10.1016/j.tet.2022.133212] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/15/2022]
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38
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Doğan C, Doğan N, Gungor M, Eticha AK, Akgul Y. Novel active food packaging based on centrifugally spun nanofibers containing lavender essential oil: Rapid fabrication, characterization, and application to preserve of minced lamb meat. Food Packag Shelf Life 2022. [DOI: 10.1016/j.fpsl.2022.100942] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/15/2022]
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39
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Correddu D, Helmy Aly S, Di Nardo G, Catucci G, Prandi C, Blangetti M, Bellomo C, Bonometti E, Viscardi G, Gilardi G. Enhanced and specific epoxidation activity of P450 BM3 mutants for the production of high value terpene derivatives. RSC Adv 2022; 12:33964-33969. [PMID: 36505709 PMCID: PMC9703296 DOI: 10.1039/d2ra06029a] [Citation(s) in RCA: 9] [Impact Index Per Article: 3.0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/24/2022] [Accepted: 11/23/2022] [Indexed: 11/29/2022] Open
Abstract
Terpenes are natural molecules of valuable interest for different industrial applications. Cytochromes P450 enzymes can functionalize terpenoids to form high value oxidized derivatives in a green and sustainable manner, representing a valid alternative to chemical catalysis. In this work, an enhanced and specific epoxidation activity of cytochrome P450 BM3 mutants was found for the terpenes geraniol and linalool. This is the first report showing the epoxidation of linalool by P450 BM3 and its mutant A2 (Asp251Gly/Gln307His) with the formation of valuable oxide derivatives, highlighting the relevance of this enzymes for industrial applications.
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Affiliation(s)
- Danilo Correddu
- Department of Life Sciences and Systems Biology, University of TorinoVia Accademia Albertina 1310123TorinoItaly
| | - Sabrina Helmy Aly
- Department of Life Sciences and Systems Biology, University of TorinoVia Accademia Albertina 1310123TorinoItaly
| | - Giovanna Di Nardo
- Department of Life Sciences and Systems Biology, University of TorinoVia Accademia Albertina 1310123TorinoItaly
| | - Gianluca Catucci
- Department of Life Sciences and Systems Biology, University of TorinoVia Accademia Albertina 1310123TorinoItaly
| | - Cristina Prandi
- Department of Chemistry, University of TorinoVia P. Giuria 710125TorinoItaly
| | - Marco Blangetti
- Department of Chemistry, University of TorinoVia P. Giuria 710125TorinoItaly
| | - Chiara Bellomo
- Department of Chemistry, University of TorinoVia P. Giuria 710125TorinoItaly
| | | | - Guido Viscardi
- Department of Chemistry, University of TorinoVia P. Giuria 710125TorinoItaly
| | - Gianfranco Gilardi
- Department of Life Sciences and Systems Biology, University of TorinoVia Accademia Albertina 1310123TorinoItaly
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Izcara S, Perestrelo R, Morante-Zarcero S, Sierra I, Câmara JS. Volatilomic fingerprinting from edible flowers. Unravelling some impact compounds behind its attractiveness. FOOD BIOSCI 2022. [DOI: 10.1016/j.fbio.2022.102188] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/13/2022]
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Ramírez-Santos J, Calzada F, Mendieta-Wejebe JE, Ordoñez-Razo RM, Martinez-Casares RM, Valdes M. Understanding the Antilymphoma Activity of Annona macroprophyllata Donn and Its Acyclic Terpenoids: In Vivo, In Vitro, and In Silico Studies. Molecules 2022; 27:7123. [PMID: 36296714 PMCID: PMC9607537 DOI: 10.3390/molecules27207123] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/26/2022] [Revised: 10/07/2022] [Accepted: 10/13/2022] [Indexed: 11/24/2022] Open
Abstract
Annona macroprophyllata Donn (A. macroprophyllata) is used in traditional Mexican medicine for the treatment of cancer, diabetes, inflammation, and pain. In this work, we evaluated the antitumor activity of three acyclic terpenoids obtained from A. macroprophyllata to assess their potential as antilymphoma agents. We identified the terpenoids farnesyl acetate (FA), phytol (PT) and geranylgeraniol (Gg) using gas chromatography-mass spectroscopy (GC-MS) and spectroscopic (1H, and 13C NMR) methods applied to petroleum ether extract of leaves from A. macroprophyllata (PEAm). We investigated antitumor potential in Balb/c mice inoculated with U-937 cells by assessing brine shrimp lethality (BSL), and cytotoxic activity in these cells. In addition, to assess the potential toxicity of PEAm, FA, PT and Gg in humans, we tested their acute oral toxicity in mice. Our results showed that the three terpenoids exhibited considerable antilymphoma and cytotoxic activity. In terms of lethality, we determined a median lethal dose (LD50) for thirteen isolated products of PEAm. Gg, PT and AF all exhibited a higher lethality with values of 1.41 ± 0.42, 3.03 ± 0.33 and 5.82 ± 0.58 µg mL-1, respectively. To assess cytotoxic activity against U-937 cells, we calculated the mean cytotoxic concentration (CC50) and found that FA and PT were closer in respect to the control drug methotrexate (MTX, 0.243 ± 0.007 µM). In terms of antilymphoma activity, we found that FA, PT and Gg considerably inhibited lymph node growth, with median effective doses (ED50) of 5.89 ± 0.39, 6.71 ± 0.31 and 7.22 ± 0.51 mg kg-1 in females and 5.09 ± 0.66, 5.83 ± 0.50 and 6.98 ± 0.57mg kg -1 in males, respectively. Regarding acute oral toxicity, we classified all three terpenoids as category IV, indicating a high safety margin for human administration. Finally, in a molecular docking study of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, we found binding of terpenoids to some amino acids of the catalytic site, suggesting an effect upon activity with a resulting decrease in the synthesis of intermediates involved in the prenylation of proteins involved in cancer progression. Our findings suggest that the acyclic terpenoids FA, PT, and Gg may serve as scaffolds for the development of new treatments for non-Hodgkin's lymphoma.
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Affiliation(s)
- Jesica Ramírez-Santos
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades 2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06720, Mexico
| | - Fernando Calzada
- Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades 2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06720, Mexico
| | - Jessica Elena Mendieta-Wejebe
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico
| | - Rosa María Ordoñez-Razo
- Unidad de Investigación Médica en Genética Humana, UMAE Hospital Pediatría, 2° Piso, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06725, Mexico
| | - Rubria Marlen Martinez-Casares
- Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana, Calzada del Hueso 1100, Mexico City 04960, Mexico
| | - Miguel Valdes
- Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico
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Arip M, Selvaraja M, R M, Tan LF, Leong MY, Tan PL, Yap VL, Chinnapan S, Tat NC, Abdullah M, K D, Jubair N. Review on Plant-Based Management in Combating Antimicrobial Resistance - Mechanistic Perspective. Front Pharmacol 2022; 13:879495. [PMID: 36249774 PMCID: PMC9557208 DOI: 10.3389/fphar.2022.879495] [Citation(s) in RCA: 16] [Impact Index Per Article: 5.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/01/2022] [Accepted: 08/01/2022] [Indexed: 11/13/2022] Open
Abstract
Antimicrobial resistance (AMR) occurs when microbes no longer respond to any pharmacological agents, rendering the conventional antimicrobial agents ineffective. AMR has been classified as one of the top 10 life-threatening global health problems needed multilevel attention and global cooperation to attain the Sustainable Development Goals (SDGs) according to the World Health Organization (WHO), making the discovery of a new and effective antimicrobial agent a priority. The recommended treatments for drug-resistant microbes are available but limited. Furthermore, the transformation of microbes over time increases the risk of developing drug resistance. Hence, plant metabolites such as terpenes, phenolic compounds and alkaloids are widely studied due to their antibacterial, antiviral, antifungal and antiparasitic effects. Plant-derived antimicrobials are preferred due to their desirable efficacy and safety profile. Plant metabolites work by targeting microbial cell membranes, interfering with the synthesis of microbial DNA/RNA/enzymes and disrupting quorum sensing and efflux pump expression. They also work synergistically with conventional antibiotics to enhance antimicrobial effects. Accordingly, this review aims to identify currently available pharmacological therapies against microbes and AMR, as well as to discuss the importance of plant and secondary metabolites as a possible solution for AMR together with their mechanisms of action. All the information was obtained from government databases, WHO websites, PubMed, Springer, Google Scholar and Science Direct. Based on the information obtained, AMR is regarded as a significant warning to global healthcare. Plant derivatives such as secondary metabolites may be considered as potential therapeutic targets to mitigate the non-ending AMR.
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Affiliation(s)
- Masita Arip
- Allergy and Immunology Research Centre, Institute for Medical Research, Ministry of Health Malaysia, Setia Alam, Malaysia
| | - Malarvili Selvaraja
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Mogana R
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Lee Fang Tan
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Mun Yee Leong
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Puay Luan Tan
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Vi Lien Yap
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Sasikala Chinnapan
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
| | - Ng Chin Tat
- Immunology Unit, Department of Pathology, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia
| | - Maha Abdullah
- Immunology Unit, Department of Pathology, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia
| | - Dharmendra K
- Narayan Institute of Pharmacy, Gopal Narayan Singh University, Jamuhar, India
| | - Najwan Jubair
- Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, UCSI University, Cheras, Malaysia
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Spices Volatilomic Fingerprinting—A Comprehensive Approach to Explore Its Authentication and Bioactive Properties. Molecules 2022; 27:molecules27196403. [PMID: 36234940 PMCID: PMC9570555 DOI: 10.3390/molecules27196403] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/12/2022] [Revised: 09/23/2022] [Accepted: 09/26/2022] [Indexed: 11/17/2022] Open
Abstract
Volatile organic metabolites (VOMs) present in different spices can provide distinct analytical biosignatures related to organoleptic properties and health benefits. This study aimed to establish the volatilomic fingerprint of six of the most consumed spices all over the world (saffron (Crocus sativus L.), cinnamon (Cinnamomum verum), cumin (Cuminum cyminum L.), black pepper, (Piper nigrum L.), sweet paprika (Capsicum annuum L.), and curry (a mix of different herbs and spices)). Based on headspace solid phase microextraction (HS-SPME) followed by gas chromatography-mass spectrometry (GC-MS) analysis, this is a powerful strategy to explore and establish the spice’s volatile pattern and unravel the potential health benefits related to the most important VOMs identified in each spice. This comprehensive knowledge will help in the definition of their authenticity, while simultaneously protecting against potential frauds and adulterations. A total of 162 VOMs were identified. Semi-quantitative assessments revealed that terpenoids and sesquiterpenoids amounted to the major volatile class in the investigated spices, except for cinnamon, where carbonyl compounds are the major group. Most of the studied spices comprised key characteristics of aroma and health bioactive compounds, e.g., dihydrojuneol in saffron, cinnamaldehyde in cinnamon, cuminaldehyde in cumin and curry, and caryophyllene in black pepper. The principal component analysis (PCA) and partial least-squares discriminant analysis (PLS-DA) successfully discriminated the investigated spices, being α-cubebene, 3-methyl butanal, β-patchoulene and β-selinene, the most important VOMs (highest VIP’s) that contributed to its discrimination. Moreover, some VOMs have a high influence on the spice’s bioactive potential, helping to prevent certain diseases including cancer, inflammatory-related diseases, diabetes, and cardiovascular diseases.
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Gombos LG, Werner L, Schollmeyer D, Martínez-Huitle CA, Waldvogel SR. Selective Electrochemical Dibromination of Terpenes and Naturally Derived Olefins. European J Org Chem 2022. [DOI: 10.1002/ejoc.202200857] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/09/2022]
Affiliation(s)
- Lilla G. Gombos
- Johannes Gutenberg University: Johannes Gutenberg Universitat Mainz Chemistry GERMANY
| | - Leo Werner
- Johannes Gutenberg University: Johannes Gutenberg Universitat Mainz Chemistry GERMANY
| | - Dieter Schollmeyer
- Johannes Gutenberg Universität Mainz: Johannes Gutenberg Universitat Mainz Chemistry GERMANY
| | | | - Siegfried R Waldvogel
- Johannes Gutenberg-Universität Mainz Institut für Organische Chemie Duesbergweg 10-14 55128 Mainz GERMANY
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León-Gutiérrez G, Elste JE, Cabello-Gutiérrez C, Millán-Pacheco C, Martínez-Gómez MH, Mejía-Alvarez R, Tiwari V, Mejía A. A potent virucidal activity of functionalized TiO 2 nanoparticles adsorbed with flavonoids against SARS-CoV-2. Appl Microbiol Biotechnol 2022; 106:5987-6002. [PMID: 35951081 PMCID: PMC9366830 DOI: 10.1007/s00253-022-12112-9] [Citation(s) in RCA: 7] [Impact Index Per Article: 2.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/15/2022] [Revised: 07/22/2022] [Accepted: 07/27/2022] [Indexed: 12/24/2022]
Abstract
Abstract The coronavirus SARS-CoV-2 has caused a pandemic with > 550 millions of cases and > 6 millions of deaths worldwide. Medical management of COVID-19 relies on supportive care as no specific targeted therapies are available yet. Given its devastating effects on the economy and mental health, it is imperative to develop novel antivirals. An ideal candidate will be an agent that blocks the early events of viral attachment and cell entry, thereby preventing viral infection and spread. This work reports functionalized titanium dioxide (TiO2)-based nanoparticles adsorbed with flavonoids that block SARS-CoV-2 entry and fusion. Using molecular docking analysis, two flavonoids were chosen for their specific binding to critical regions of the SARS-CoV-2 spike glycoprotein that interacts with the host cell angiotensin-converting enzyme-2 (ACE-2) receptor. These flavonoids were adsorbed onto TiO2 functionalized nanoparticles (FTNP). This new nanoparticulate compound was assayed in vitro against two different coronaviruses; HCoV 229E and SARS-CoV-2, in both cases a clear antiviral effect was observed. Furthermore, using a reporter-based cell culture model, a potent antiviral activity is demonstrated. The adsorption of flavonoids to functionalized TiO2 nanoparticles induces a ~ threefold increase of that activity. These studies also indicate that FTNP interferes with the SARS-CoV-2 spike, impairing the cell fusion mechanism. Key points/Highlights • Unique TiO2nanoparticles displaying flavonoid showed potent anti-SARS-CoV-2 activity. • The nanoparticles precisely targeting SARS-CoV-2 were quantitatively verified by cell infectivity in vitro. • Flavonoids on nanoparticles impair the interactions between the spike glycoprotein and ACE-2 receptor. Graphical abstract ![]()
Supplementary Information The online version contains supplementary material available at 10.1007/s00253-022-12112-9.
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Affiliation(s)
- Gabriela León-Gutiérrez
- Departamento de Biotecnología, Universidad Autónoma Metropolitana-Iztapalapa, Ciudad de Mexico, Mexico
| | - James Edward Elste
- Department of Microbiology and Immunology, Midwestern University, Downers Grove, IL, USA
| | - Carlos Cabello-Gutiérrez
- Departamento de Virología e Investigación en Micología, Instituto Nacional de Enfermedades Respiratorias, Ciudad de Mexico, Mexico
| | - Cesar Millán-Pacheco
- Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, Mexico
| | - Mario H Martínez-Gómez
- Departamento de Biotecnología, Universidad Autónoma Metropolitana-Iztapalapa, Ciudad de Mexico, Mexico
| | - Rafael Mejía-Alvarez
- Department of Physiology, College of Graduate Studies, Midwestern University, Downers Grove, IL, USA
| | - Vaibhav Tiwari
- Department of Microbiology and Immunology, Midwestern University, Downers Grove, IL, USA
| | - Armando Mejía
- Departamento de Biotecnología, Universidad Autónoma Metropolitana-Iztapalapa, Ciudad de Mexico, Mexico.
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Bachheti RK, Worku LA, Gonfa YH, Zebeaman M, Deepti, Pandey DP, Bachheti A. Prevention and Treatment of Cardiovascular Diseases with Plant Phytochemicals: A Review. EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE : ECAM 2022; 2022:5741198. [PMID: 35832515 PMCID: PMC9273387 DOI: 10.1155/2022/5741198] [Citation(s) in RCA: 20] [Impact Index Per Article: 6.7] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Received: 04/10/2022] [Revised: 05/27/2022] [Accepted: 06/02/2022] [Indexed: 12/19/2022]
Abstract
Cardiovascular diseases (CVDs) are the world's leading killers, accounting for 30% deaths. According to the WHO report, CVDs kill 17.9 million people per year, and there will be 22.2 million deaths from CVD in 2030. The death rates rise as people get older. Regarding gender, the death rate of women by CVD (51%) is higher than that of men (42%). To decrease and prevent CVD, most people rely on traditional medicine originating from the plant (phytochemicals) in addition to or in preference to commercially available drugs to recover from their illness. The CVD therapy efficacy of 92 plants, including 15 terrestrial plants, is examined. Some medicinal plants well known to treat CVD are, Daucus carota, Nerium oleander, Amaranthus Viridis, Ginkgo biloba, Terminalia arjuna, Picrorhiza kurroa, Salvia miltiorrhiza, Tinospora cordifolia, Mucuna pruriens, Hydrocotyle asiatica, Bombax ceiba, and Andrographis paniculate. The active phytochemicals found in these plants are flavonoids, polyphenols, plant sterol, plant sulphur compounds, and terpenoids. A general flavonoid mechanism of action is to prevent low-density lipoprotein oxidation, which promotes vasodilatation. Plant sterols prevent CVD by decreasing cholesterol absorption in the blood. Plant sulphur compound also prevent CVD by activation of nuclear factor-erythroid factor 2-related factor 2 (Nrf2) and inhibition of cholesterol synthesis. Quinone decreases the risk of CVD by increasing ATP production in mitochondria while terpenoids by decreasing atherosclerotic lesion in the aortic valve. Although several physiologically active compounds with recognized biological effects have been found in various plants because of the increased prevalence of CVD, appropriate CVD prevention and treatment measures are required. More research is needed to understand the mechanism and specific plants' phytochemicals responsible for treating CVD.
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Affiliation(s)
- Rakesh Kumar Bachheti
- Bioprocess and Biotechnology Center of Excellence, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
- Department of Industrial Chemistry, College of Applied Sciences, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
| | - Limenew Abate Worku
- Bioprocess and Biotechnology Center of Excellence, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
- Department of Industrial Chemistry, College of Applied Sciences, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
| | - Yilma Hunde Gonfa
- Bioprocess and Biotechnology Center of Excellence, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
- Department of Chemistry, Faculty of Natural and Computational Science, Ambo University, Ambo, Ethiopia
| | - Meseret Zebeaman
- Bioprocess and Biotechnology Center of Excellence, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
- Department of Industrial Chemistry, College of Applied Sciences, Addis Ababa Sciences and Technology University, P.O. Box 16417, Addis Ababa, Ethiopia
| | - Deepti
- Department of Environment Science, Graphic Era University, Dehradun-248002, Uttarakhand, India
| | - D. P. Pandey
- Department of Chemistry, Government P. G. College, Uttarkashi, India
| | - Archana Bachheti
- Department of Environment Science, Graphic Era University, Dehradun-248002, Uttarakhand, India
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Li YN, Zhang SB, Lv YY, Zhai HC, Cai JP, Hu YS. Linalool, the main volatile constituent from Zanthoxylum schinifolium pericarp, prevents growth of Aspergillus flavus in post-harvest grains. Food Control 2022. [DOI: 10.1016/j.foodcont.2022.108967] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/18/2022]
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Current Progress and Future Perspectives on the Use of Bacillus clausii. Microorganisms 2022; 10:microorganisms10061246. [PMID: 35744764 PMCID: PMC9230978 DOI: 10.3390/microorganisms10061246] [Citation(s) in RCA: 11] [Impact Index Per Article: 3.7] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/30/2022] [Revised: 05/30/2022] [Accepted: 05/31/2022] [Indexed: 12/12/2022] Open
Abstract
Bacillus clausii is a probiotic that benefits human health. Its key characteristics include the ability to form spores; the resulting tolerance to heat, acid, and salt ensures safe passage through the human gastrointestinal tract with no loss of cells. Although B. clausii has been widely used for many decades, the beneficial properties of other probiotics, such as Lactobacillus spp. and Bifidobacterium spp., are better disseminated in the literature. In this review, we summarize the physiological, antimicrobial, and immunomodulatory properties of probiotic B. clausii strains. We also describe findings from studies that have investigated B. clausii probiotics from the perspective of quality and safety. We highlight innovative properties based on biochemical investigations of non-probiotic strains of B. clausii, revealing that B. clausii may have further health benefits in other therapeutic areas.
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The Analysis of Correlations Between Terpene Transformations and Fermentation Type of Apple Musts. ACTA UNIVERSITATIS CIBINIENSIS. SERIES E: FOOD TECHNOLOGY 2022. [DOI: 10.2478/aucft-2022-0008] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/20/2022] Open
Abstract
Abstract
We measured the concentration of 13 terpenes in musts of 3 different apple cultivars fermented spontaneously, with Ethanol RED yeast (Saccharomyces cerevisiae) or Cider Yeast (Saccharomyces bayanus). Then we analysed obtained data with PCA with various packages in R to assess how different types of fermentation and apple cultivars affected terpene profile. The most informative results of PCA were obtained in ‘psych’ package and they indicated that there were groups of terpenes which concentrations increased simultaneously, while for some other groups the content of particular compounds was negatively correlated. This suggests that the first group of terpenes originated from different substrates while the latter group could be obtained from the same compound. Our findings indicated new possible pathways of terpene transformation, e.g. linalool, citral and geraniol could transform into one another. Moreover, the role of S. bayanus in those processes remains unclear and it requires further consideration.
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Identification of Potent Bioassay Guided Terpenoid and Glycoside Root Fractions of Astragalus candolleanus against Clinically Significant Bacterial Strains. Int J Microbiol 2022; 2022:4584799. [PMID: 35528313 PMCID: PMC9072053 DOI: 10.1155/2022/4584799] [Citation(s) in RCA: 3] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/10/2022] [Revised: 02/03/2022] [Accepted: 04/07/2022] [Indexed: 01/22/2023] Open
Abstract
Antibiotic resistance represents one of the biggest challenges, and there is an urgent need for plant-based antimicrobial agents that enable managing this crisis effectively. In this work, we aimed to investigate the antibacterial activity of Astragalus candolleanus (A. candolleanus) hydromethanolic root extract against Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Kocuria rhizophila) strains by the cup-plate method. The root was powdered and extracted with 70% methanol by cold maceration for 5 days. Preliminary phytochemical screening was performed with different solvents in the order of increasing polarity. Pure compounds were isolated by column chromatography and were characterized through liquid chromatography-mass spectrometry. Targeted predictions of the isolated compounds were also studied using Swiss Target prediction software and prediction of activity spectra for substances. The extract showed a broad zone of inhibition against pathogenic bacteria. Four pure compounds were isolated, of which a novel terpenoid compound has been identified as stemmadenine along with scillirosidin, cephalotaxine, and myxoxanthophyll. The structures of the isolated phytoconstituents were elucidated by spectral analysis. The four pure components isolated from the roots of A. candolleanus are suggested to be effective against tested pathogens. Overall results of drug design suggest that myxoxanthophyll is a promising bioactive compound endowed with antibacterial activity.
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