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Zhang X, Liu M, Zhang X, Ma L, Song S, Pan M, Huang S, Ren W, Ma W. Aster tataricus L. f.: a review on the botany, phytochemistry, ethnopharmacology, pharmacology, toxicology and comprehensive utilization. Front Pharmacol 2025; 16:1581505. [PMID: 40271061 PMCID: PMC12014666 DOI: 10.3389/fphar.2025.1581505] [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: 02/22/2025] [Accepted: 03/26/2025] [Indexed: 04/25/2025] Open
Abstract
Aster tataricus L.f. (A.tataricus), a perennial herb of the genus Aster in the Asteraceae (Compositae) family. It is associated with a spicy, bitter, and warm nature and belongs to the Lung Meridian. The medicinal parts of A.tataricus are flowers, leaves, roots, and rhizomes. A.tataricus was first recorded in Shuo Wen under the alias "Zi Wan" (). Traditionally, it is utilised to clear lung qi, promote fluid flow, calm adverse-rising energy, relieve cough, resolve sputum, and regulate secretions. However, it is worth noting that A.tataricus has certain hepatotoxicity. Modern pharmacology indicates that A.tataricus can be used to treat various diseases, including those of the respiratory and urinary systems. In this review, all available information on A.tataricus was collected via academic databases such as PubMed, SciFinder Scholar, CNKI, iPlant, Google Scholar, Web of Science, GBIF, and Masterpieces of Traditional Chinese Medicine. To date, more than 200 metabolites have been isolated and characterized from A.tataricus, including terpenoids, flavonoids, polypeptides, and others. These compounds demonstrate a wide range of pharmacological activities, such as anti-inflammatory effects, antitussive and bronchodilatory properties, anticancer activity, antioxidant effects, treatment of osteolytic disorders, management of urinary system diseases, alleviation of acute lung injury, and enhancement of memory. Meanwhile, the different polarity extracts of A.tataricus also exhibit some toxicological characteristics, the astin has a similar structure to that of cyclochloridine, the hepatotoxic metabolite of penicillin; its saponins also have hemolytic effects. However, there are currently few studies on the toxicology of A.tataricus. Further in-depth research is needed to explore the potential mechanisms underlying the toxicity of A.tataricus. The toxicity of A.tataricus can be reduced through compatibility and processing, but this aspect has received little discussion and further research on quality standardization is needed. To ensure the sustainable development of A.tataricus, we have also summarized its artificial cultivation techniques. Shionone and astin are the characteristic components of A.tataricus. Their pharmacological effects have been deeply studied, but the research on other metabolites is relatively scarce. Therefore, this article focuses on botany, artificial cultivation, phytochemistry, ethnopharmacology, pharmacology, toxicology, and comprehensive utilization of A.tataricus. Discuss the future research prospects and existing problems of A.tataricus, and provide references for further research on A.tataricus and the establishment of quality control standards.
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Affiliation(s)
| | | | | | | | | | | | | | - Weichao Ren
- College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, China
| | - Wei Ma
- College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, China
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Hendawy MS, Hashem MM, Zaki AA, Rabie MA, Sayed NSE, El Dine RS, El-Halawany AM. Efficacy of Aster chinensis aerial parts metabolites in BALB/c mice model of Imiquimod-induced psoriasis skin inflammation. Inflammopharmacology 2025; 33:1973-1996. [PMID: 40072672 PMCID: PMC11991947 DOI: 10.1007/s10787-025-01652-x] [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: 11/07/2024] [Accepted: 01/08/2025] [Indexed: 03/14/2025]
Abstract
Using a bioassay-guided fractionation approach, the most potent anti-psoriatic components of Aster squamatus herb, Aster chinensis stalks, and Aster chinensis flowers, cultivated in Egypt, were identified and evaluated against Imiquimod (IMQ)-induced psoriasis in female BALB/c mice and compared to standard drug, mometasone. The topical application of A. chinensis stalk methanolic extract exhibited the strongest anti-psoriatic effects against IMQ-induced psoriasis model, as evidenced by improvements in psoriasis area severity index (PASI) score, histopathological analysis, and spleen index. Further fractionation of A. chinensis stalk methanolic extract using petroleum ether, methylene chloride, ethyl acetate, and n-butanol revealed that the methylene chloride fraction (MCF) was the most potent. Indeed, MCF significantly reduced the PASI score, alleviated histopathological changes, and restored spleen index. Mechanistically, MCF exerted its anti-psoriatic effects by suppressing inflammation, evidenced by decreased TLR-4 gene expression and lower levels of HMGB1 and NFκBp65 protein contents. Additionally, MCF reduced serum levels of pro-inflammatory cytokines interleukin (IL)-1β, IL-6, IL-23, and IL-17 while mitigating oxidative stress through increased superoxide dismutase (SOD) activity and reduced malondialdehyde (MDA) content. Notably, the efficacy of MCF was comparable to that of mometasone, with no significant differences observed. In parallel, the chemical profile of the MCF was analyzed using UHPLC-MS/MS techniques in negative and positive ionization full scan modes. MCF of A. chinensis stalk could be used a potential therapeutic agent for psoriasis.
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Affiliation(s)
- Mai S Hendawy
- Department of Pharmacognosy, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt
| | - Mona M Hashem
- Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt
| | - Ahmed A Zaki
- Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt
| | - Mostafa A Rabie
- Department of Pharmacology & Toxicology, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt
| | - Nesrine S El Sayed
- Department of Pharmacology & Toxicology, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt
| | - Riham Salah El Dine
- Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt.
| | - Ali M El-Halawany
- Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt
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Fan XL, Qin ZP, Wen JH, Wang ZZ, Xiao W. An updated and comprehensive review of the morphology, ethnomedicinal uses, phytochemistry, and pharmacological activity of Aster tataricus L. f. Heliyon 2024; 10:e35267. [PMID: 39166058 PMCID: PMC11334675 DOI: 10.1016/j.heliyon.2024.e35267] [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: 02/09/2024] [Revised: 06/20/2024] [Accepted: 07/25/2024] [Indexed: 08/22/2024] Open
Abstract
Ethnopharmacological relevance Aster tataricus L.f., an extensively used herb in traditional Chinese medicine for more than 2000 years, is known as "Zi wan" or "Fan huncao". Its dried root and rhizome hold great promise in the treatment of cough, asthma, tumor, inflammation, etc.Aim of the study: This literature review summarizes the morphology characteristics, ethnopharmacological use, phytochemical properties, pharmacological effects, and potential applications of Aster tataricus. Furthermore, this review will discuss the future research trends and development prospects of this plant. Materials and methods Using "Aster tataricus L.f.", "Traditional medicinal usage", "Phytochemistry", "Pharmacological effects" as the keywords and gathered relevant data on Aster tataricus L.f. using electronic databases (Elsevier, PubMed, ACS, CNKI, Google Scholar, Baidu Scholar, Web of Science), relevant books, and classic literature about Chinese herb. Result A total of 186 compounds have been isolated and identified from Aster tataricus, including terpenes, organic acids, peptides, and flavonoids. And Aster tataricus has been widely used as a natural cough suppressant and has anti-oxidative, anti-inflammatory, anti-depressive, and anti-tumor effects. In addition, Aster tataricus has also been reported to have damaging effects on the liver as well as other toxicities were discussed in this review. Conclusions Aster tataricus is an ancient herbal medicine with a broad spectrum of pharmaco logical activities that has been used for thousands of years in China, and has shown remarkable effectiveness in the treatment of various diseases, especially cough, asthma, inflammation. Although its rich chemical constituents have various pharmacological activities, the underlying mechanisms, as well as its toxicity and safety, remains unclear and warrant further investigation.
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Affiliation(s)
- Xi-Ling Fan
- Henan University of Chinese Medicine, Zhengzhou, China
- National Key Laboratory on Technologies for Chinese Medicine Pharmaceutical Process Control and Intelligent Manufacture, China
| | | | - Jian-Hui Wen
- National Key Laboratory on Technologies for Chinese Medicine Pharmaceutical Process Control and Intelligent Manufacture, China
| | - Zhen-Zhong Wang
- National Key Laboratory on Technologies for Chinese Medicine Pharmaceutical Process Control and Intelligent Manufacture, China
| | - Wei Xiao
- National Key Laboratory on Technologies for Chinese Medicine Pharmaceutical Process Control and Intelligent Manufacture, China
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Wang G, Xie W, Deng L, Huang X, Sun M, Liu W, Tang S. Nrf2 mediates the effects of shionone on silica-induced pulmonary fibrosis. Chin Med 2024; 19:88. [PMID: 38898509 PMCID: PMC11188511 DOI: 10.1186/s13020-024-00947-5] [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: 11/29/2023] [Accepted: 05/19/2024] [Indexed: 06/21/2024] Open
Abstract
BACKGROUND Extended contact with silica particles can lead to Silicosis, a chronic lung condition lacking established treatment protocols or clear mechanisms of development. The urgency for innovative treatments arises from the unavailability of effective treatment methodologies. The origin of silica-induced pulmonary fibrosis includes essential processes such as macrophage activation and the conversion of fibroblasts into myofibroblasts, with oxidative stress playing a pivotal role. Shionone (SHI), a triterpenoid extracted from the Aster tataricus plant, is recognized for its extensive health benefits. This study explores the capability of SHI to alleviate the effects of silica-induced lung fibrosis in mice. METHODS This investigation explored the impact of SHI on lung inflammation and fibrosis at different stages (early and late) triggered by silica in mice, focusing specifically on the initial and more developed phases. It comprised an analysis of isolated peritoneal macrophages and fibroblasts extracted from mice to elucidate SHI's therapeutic potential and its underlying mechanism. The methodology employed encompassed quantitative PCR, immunofluorescence, flow cytometry, and western blotting to examine macrophage activity and their transition into myofibroblasts. The activation of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway by SHI was confirmed via immunofluorescence and western blot studies. SHI's antioxidative properties were evidenced by the measurement of reactive oxygen species (ROS) and mitochondrial ROS within both macrophages and fibroblasts, using 2', 7'-dichlorodihydrofluorescein diacetate and MitoSOX, respectively. The relevance of SHI was further underscored by applying ML385 and Nrf2 siRNA to gauge its effectiveness. RESULTS Starting SHI treatment early countered the harmful effects of lung inflammation and fibrosis caused by silica, while initiating SHI at a later phase decelerated the advancement of fibrosis. SHI's action was linked to the activation of the Nrf2 signaling pathway, a boost in antioxidant enzyme levels, and a decrease in oxidative stress and inflammation in macrophages affected by silica. Furthermore, SHI prevented the conversion of fibroblasts into myofibroblasts prompted by TGF-β, along with the resultant oxidative stress. The beneficial outcomes of SHI were negated when ML385 and Nrf2 siRNA were applied, highlighting the pivotal role of the Nrf2 pathway in SHI's efficacy. CONCLUSION SHI plays a significant role in stimulating the Nrf2 pathway, thereby defending against silica-induced oxidative stress and inflammatory reactions in macrophages, and inhibiting the conversion of fibroblasts to myofibroblasts due to TGF-β. This suggests that SHI is a viable option for treating lung inflammation and fibrosis in mice suffering from silicosis.
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Affiliation(s)
- Guiyun Wang
- Shandong Xiehe University, Jinan, Shandong, China
| | - Weixi Xie
- Xiangya Nursing School, Central South University, Changsha, Hunan, China
| | - Lang Deng
- Xiangya Nursing School, Central South University, Changsha, Hunan, China
| | - Xiaoting Huang
- Xiangya Nursing School, Central South University, Changsha, Hunan, China
| | - Mei Sun
- Xiangya Nursing School, Central South University, Changsha, Hunan, China
| | - Wei Liu
- Xiangya Nursing School, Central South University, Changsha, Hunan, China.
| | - Siyuan Tang
- Xiangya Nursing School, Central South University, Changsha, Hunan, China.
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Gao XY, Li XY, Zhang CY, Bai CY. Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity. Front Pharmacol 2024; 15:1268464. [PMID: 38464713 PMCID: PMC10923241 DOI: 10.3389/fphar.2024.1268464] [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: 07/28/2023] [Accepted: 01/24/2024] [Indexed: 03/12/2024] Open
Abstract
Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, pharmacokinetics, and toxicity of scopoletin is provided. In addition, the prospects and outlook for future studies are appraised. Scopoletin is indicated to have antimicrobial, anticancer, anti-inflammation, anti-angiogenesis, anti-oxidation, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties and immunomodulatory effects in both in vitro and in vivo experimental trials. In addition, it is an inhibitor of various enzymes, including choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies have demonstrated the low bioavailability, rapid absorption, and extensive metabolism of scopoletin. These properties may be associated with its poor solubility in aqueous media. In addition, toxicity research indicates the non-toxicity of scopoletin to most cell types tested to date, suggesting that scopoletin will neither induce treatment-associated mortality nor abnormal performance with the test dose. Considering its favorable pharmacological activities, scopoletin has the potential to act as a drug candidate in the treatment of cancer, liver disease, diabetes, neurodegenerative disease, and mental disorders. In view of its merits and limitations, scopoletin is a suitable lead compound for the development of new, efficient, and low-toxicity derivatives. Additional studies are needed to explore its molecular mechanisms and targets, verify its toxicity, and promote its oral bioavailability.
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Affiliation(s)
- Xiao-Yan Gao
- Basic Medicine College, Chifeng University, Chifeng, China
- Inner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, China
- Key Laboratory of Mechanism and Evaluation of Chinese and Mongolian Pharmacy at Chifeng University, Chifeng University, Chifeng, China
| | - Xu-Yang Li
- Basic Medicine College, Chifeng University, Chifeng, China
- Inner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, China
| | - Cong-Ying Zhang
- Basic Medicine College, Chifeng University, Chifeng, China
- Inner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, China
- Key Laboratory of Mechanism and Evaluation of Chinese and Mongolian Pharmacy at Chifeng University, Chifeng University, Chifeng, China
| | - Chun-Ying Bai
- Basic Medicine College, Chifeng University, Chifeng, China
- Inner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, China
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Jaiswal V, Lee HJ. Pharmacological Properties of Shionone: Potential Anti-Inflammatory Phytochemical against Different Diseases. Molecules 2023; 29:189. [PMID: 38202771 PMCID: PMC10780092 DOI: 10.3390/molecules29010189] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/15/2023] [Revised: 12/19/2023] [Accepted: 12/27/2023] [Indexed: 01/12/2024] Open
Abstract
Shionone is a triterpenoid that is the primary constituent of an important ancient Chinese medicine named Radix Asteris. It has emerged as an attractive candidate against different important diseases, including interstitial cystitis, colitis, cancer, Parkinson's disease, and urinary tract infections, and was found to have a protective effect on multiple organs, including the colon, kidneys, lungs, brain, and bladder. The anti-inflammation activity of shionone may be considered an important property that imparts the positive health outcomes of shionone. Important molecular targets and markers such as TNF-α, STAT3, NLRP3, and NF-κB were also found to be targeted by shionone and were verified in different diseases. This suggests the possible potential of shionone against other diseases associated with these targets. Pharmacokinetic studies also support the therapeutic potential of shionone and provide the initial track that may be pursued for its development. Yet, the compilation of the pharmacological activities of shionone and its important genes and pathway targets are absent in the existing literature, which would direct its development as a therapeutic and/or supplement. Hence, the present review provides a compilation of information concerning pharmacological activities, highlights the existing holes, and proposes a specific direction for the expansion of shionone as a therapeutic against different diseases and conditions.
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Affiliation(s)
- Varun Jaiswal
- Department of Food and Nutrition, College of BioNano Technology, Gachon University, Seongnam 13120, Republic of Korea;
| | - Hae-Jeung Lee
- Department of Food and Nutrition, College of BioNano Technology, Gachon University, Seongnam 13120, Republic of Korea;
- Institute for Aging and Clinical Nutrition Research, Gachon University, Seongnam 13120, Republic of Korea
- Department of Health Sciences and Technology, GAIHST, Gachon University, Incheon 21999, Republic of Korea
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Jia K, Zhang X, Meng Y, Liu S, Liu X, Yang T, Wen C, Liu L, Ge S. Metabolomics and transcriptomics provide insights into the flavonoid biosynthesis pathway in the roots of developing Aster tataricus. JOURNAL OF PLANT RESEARCH 2023; 136:139-156. [PMID: 36520245 PMCID: PMC9753034 DOI: 10.1007/s10265-022-01426-4] [Citation(s) in RCA: 6] [Impact Index Per Article: 3.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Figures] [Subscribe] [Scholar Register] [Received: 07/13/2022] [Accepted: 11/09/2022] [Indexed: 06/17/2023]
Abstract
Aster tataricus (L.) is an important medicinal plant in China. Its roots are rich in flavonoids, the main medicinal components. However, the molecular basis of flavonoid biosynthesis in the roots of A. tataricus remains unclear. In this study, the content of total flavonoid of A. tataricus roots at different developmental stages was measured first, and the results showed that the content of total flavonoid gradually decreased from September to November, which may be caused by the stagnation of A. tataricus growth due to the decrease in temperature after September. Then, an integrated analysis of transcriptome and metabolome was conducted on five developing stages of A. tataricus roots to identify flavonoid compositions and potential genes involved in flavonoid biosynthesis. A total of 80 flavonoid metabolites, of which 75% were flavonols and flavonoids, were identified in metabolomic analyses, among which isorhamnetin, kaempferol, quercetin, and myricetin were the main skeletons of these flavonoids. Cluster analysis divided these 80 flavonoids into 3 clusters. The compounds in cluster I mainly accumulated in S1, S3, and S5. In cluster II, the relative content of the flavonoid metabolites showed an upward trend from S2 to S4. In cluster III, the flavonoids decreased from S1 to S5. A total of 129 structural genes, including 43 PAL, 23 4CL, 9 C4H, 4 CHS, 18 CHI, 3 F3H, 5 F3'H, 1 F3'5'H, 21 FLS, and 2 FSII, and 65 transcription factors, including 22 AP2/ERF, 7 bHLH, 5 bZIP, 8 MYB, 11 NAC, and 12 WRKY, showed significant correlation with total flavonoid content. Eighteen genes (7 4CL, 5 C4H, 2 CHI, 1 F3H, and 3 FLS) and 30 genes (5 PAL, 9 4CL, 1 C4H, 2 CHI, 1 F3H, 1 DFR, 7 3AT, 1 BZ1, and 3 UGT79B1) were identified as key structural genes for kaempferol and anthocyanins biosynthesis, respectively. Our study provides valuable information for understanding the mechanism of flavonoid biosynthesis in A. tataricus root.
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Affiliation(s)
- Kaixuan Jia
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
| | - Xiaoling Zhang
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
| | - Yijiang Meng
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
- College of Life Science, Hebei Agricultural University, Baoding, 071000, China
| | - Shuqi Liu
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
| | - Xiaoqing Liu
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
| | - Taixin Yang
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China
| | - Chunxiu Wen
- Institute of Cash Crops, Medicinal Plant Research Center West of Hebei Academy of Agriculture and Forestry Sciences, Nongke Road, Xiyuan Street, Xinhua District, Shijiazhuang, 050000, Hebei, China
| | - Lingdi Liu
- Institute of Cash Crops, Medicinal Plant Research Center West of Hebei Academy of Agriculture and Forestry Sciences, Nongke Road, Xiyuan Street, Xinhua District, Shijiazhuang, 050000, Hebei, China.
| | - Shujun Ge
- College of Agronomy, West Campus of Hebei Agricultural University, Lianchi District, Baoding, 071000, Hebei, China.
- Key Laboratory of Crop Germplasm Resources Research and Utilization in North China, Ministry of Education, Baoding, 071000, China.
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Majid M, Farhan A, Baig MW, Khan MT, Kamal Y, Hassan SSU, Bungau S, Haq IU. Ameliorative Effect of Structurally Divergent Oleanane Triterpenoid, 3-Epifriedelinol from Ipomoea batatas against BPA-Induced Gonadotoxicity by Targeting PARP and NF-κB Signaling in Rats. Molecules 2022; 28:molecules28010290. [PMID: 36615482 PMCID: PMC9822353 DOI: 10.3390/molecules28010290] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.7] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/02/2022] [Revised: 12/19/2022] [Accepted: 12/24/2022] [Indexed: 12/31/2022] Open
Abstract
The pentacyclic triterpenoids (PTs) of plant origin are reputed to restrain prostate cancer (PCa) cell proliferation. This study aims to assess 3-epifriedelinol (EFD) isolated from aerial part of Ipomoea batatas against PCa and its potential mechanism, in vitro and in vivo. Molecular docking affirms good binding affinity of the compound with target proteins exhibiting binding energy of −7.9 Kcal/mol with BAX, −8.1 Kcal/mol (BCL-2), −1.9 Kcal/mol (NF-κB) and −8.5 Kcal/mol with P53. In the MTT assay, EFD treatment (3−50 µM) showed a significant (p < 0.05 and p < 0.01) dose and time dependent drop in the proliferative graph of DU145 and PC3, and an upsurge in apoptotic cell population. EFD displayed substantial IC50 against DU145 (32.32 ± 3.72 µM) and PC3 (35.22 ± 3.47 µM). According to Western blots, EFD administration significantly enhanced the cleavage of caspases and PARP, elevated BAX and P53 and decreased BCL-2 and NF-κB expression, thereby triggering apoptosis in PCa cells. When male Sprague Dawley rats were intoxicated with Bisphenol A (BPA), an apparent increase in prostate mass (0.478 ± 0.08 g) in comparison to control (0.385 ± 0.03 g) indicates prostatitis. Multidose treatment of EFD (10 mg/kg) significantly reduced prostate size (0.404 ± 0.05 g). EFD exhibited substantial curative potential in vivo, as hematological, hormonal and histopathological parameters have been significantly improved. Reduced peroxidation (TBARS), and suppression of inflammatory markers i.e., NO, IL-6 and TNF-α, signposts substantial antiinflammatory potential of the compound. Overall, EFD has shown better binding affinity with target molecules, acceptable ADMET profile, potent antiproliferative and apoptotic nature and significant reduction in inflamed prostate mass of rats. The present study demonstrates acceptable physicochemical and pharmacokinetic properties of the compound with excellent drugable nature, hence EFD in the form of standardized formulation can be developed as primary or adjuvant therapy against PCa and toxins-induced gonadotoxicity.
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Affiliation(s)
- Muhammad Majid
- Faculty of Pharmacy, Hamdard University, Islamabad 45550, Pakistan
| | - Anam Farhan
- Department of Biology, School of Science and Engineering, Lahore University of Management Sciences, Lahore 54792, Pakistan
| | - Muhammad Waleed Baig
- Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan
| | - Muhammad Tariq Khan
- Faculty of Pharmacy, Capital University of Science and Technology, Islamabad 44000, Pakistan
| | - Yousaf Kamal
- Faculty of Pharmacy, Hamdard University, Islamabad 45550, Pakistan
| | - Syed Shams ul Hassan
- Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China
- Correspondence: (S.S.u.H.); (S.B.); (I.-u.H.)
| | - Simona Bungau
- Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 410028 Oradea, Romania
- Correspondence: (S.S.u.H.); (S.B.); (I.-u.H.)
| | - Ihsan-ul Haq
- Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan
- Correspondence: (S.S.u.H.); (S.B.); (I.-u.H.)
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Li KJ, Liu YY, Wang D, Yan PZ, Lu DC, Zhao DS. Radix Asteris: Traditional Usage, Phytochemistry and Pharmacology of An Important Traditional Chinese Medicine. Molecules 2022; 27:molecules27175388. [PMID: 36080154 PMCID: PMC9458035 DOI: 10.3390/molecules27175388] [Citation(s) in RCA: 3] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/27/2022] [Revised: 08/15/2022] [Accepted: 08/22/2022] [Indexed: 12/04/2022] Open
Abstract
Radix Asteris (RA), also known as ‘Zi Wan’, is the dried root and rhizome of Aster tataricus L. f., which has been used to treat cough and asthma in many countries such as China, Japan, Korea and Vietnam. This article summarizes the available information on RA in ancient Chinese medicine books and modern research literature: its botanical properties, traditional uses, chemical composition, pharmacological activity, toxicity and quality control. Studies have shown that RA extracts contain terpenes, triterpenoid saponins, organic acids, peptides and flavonoids, and have various pharmacological activities such as anti-inflammatory, anti-tumor, anti-oxidation, and anti-depression. RA is considered to be a promising medicinal plant based on its traditional use, chemical constituents and pharmacological activities. However, there are few studies on its toxicity and the consistency of its components, which indicates the need for further in-depth studies on the toxicity and quality control of RA and its extracts.
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Affiliation(s)
- Ke-Jie Li
- Experimental Center, Shandong University of Traditional Chinese Medicine, Jinan 250355, China
| | - Yang-Yang Liu
- College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China
| | - Dong Wang
- Shandong Academy of Pharmaceutical Sciences, Jinan 250101, China
| | - Pei-Zheng Yan
- College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China
| | - De-Chao Lu
- International Education College, Shandong University of Traditional Chinese Medicine, Jinan 250355, China
| | - Dong-Sheng Zhao
- College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China
- Correspondence: ; Tel./Fax: +86-531-89628172
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Aurantiamide Acetate Ameliorates Lung Inflammation in Lipopolysaccharide-Induced Acute Lung Injury in Mice. BIOMED RESEARCH INTERNATIONAL 2022; 2022:3510423. [PMID: 36046440 PMCID: PMC9424011 DOI: 10.1155/2022/3510423] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Received: 05/05/2022] [Revised: 07/21/2022] [Accepted: 08/08/2022] [Indexed: 11/18/2022]
Abstract
Purpose Aurantiamide acetate (AA) is a dipeptide derivative with complex pharmacological activities and remarkable effects on preventing and treating various diseases. In the current study, we aimed to investigate whether AA can exert protective effects in a mouse model of ALI induced by LPS. Materials and Methods In this model, mice were given intranasal LPS for 3 days prior to receiving AA (2.5, 5, and 10 mg/kg) via oral gavage. An assessment of histopathological changes was performed by hematoxylin and eosin (HE). Proinflammatory cytokines were detected in bronchoalveolar lavage fluids (BALFs) by enzyme-linked immunosorbent assays (ELISAs). The effects of AA on protein expression of NF-κB and PI3K/AKT signaling pathways were determined by Western blot. In addition, lung wet/dry (W/D) weight ratio, myeloperoxidase (MPO) activity, cell counts, and protein content were also measured. Results According to results, AA pretreatment significantly reduced lung pathological changes, W/D ratio, MPO activity, and protein content. Additionally, AA resulted in a significant reduction in the number of total cells, neutrophils, and proinflammatory cytokines in the BALF after LPS stimulation. The subsequent study revealed that pretreatment with AA dose dependently suppressed LPS-induced activation of NF-κB as well as PI3K/AKT phosphorylation. Conclusion The results indicated that the AA had a protective effect on LPS-induced ALI in mice and could be a potential drug for ALI.
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11
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Chemical synthesis of the pentasaccharide related to the anti-inflammatory oleanane type saponins isolated from medicinal plant Aster tataricus L. f. Carbohydr Res 2022; 516:108563. [DOI: 10.1016/j.carres.2022.108563] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/23/2022] [Revised: 04/05/2022] [Accepted: 04/19/2022] [Indexed: 11/17/2022]
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12
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Zhang J, He Y, Zhou Y, Hong L, Jiang Z, Zhao Y, Pan Z. Epifriedelinol Ameliorates DMBA-induced Breast Cancer in Albino Rats by Regulating the PI3K/AKT Pathway. TOHOKU J EXP MED 2022; 257:283-289. [DOI: 10.1620/tjem.2022.j030] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/18/2022]
Affiliation(s)
- Jing Zhang
- Department of Integrative Oncology, Tian Jin Cancer Hospital Airport Hospital
| | - Yang He
- Department of Breast Medical Oncology, Tian Jin Cancer Hospital Airport Hospital
| | - Ying Zhou
- Department of Integrative Oncology, Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer; Key Laboratory of Cancer Prevention and Therapy; Tianjin's Clinical Research Center for Cancer; Key Laboratory of Cancer Immunology and Biotherapy
| | - Liping Hong
- Center for Precision Cancer Medicine & Translational Research, Tianjin Cancer Hospital Airport Hospital
| | - Zhansheng Jiang
- Department of Integrative Oncology, Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer; Key Laboratory of Cancer Prevention and Therapy; Tianjin's Clinical Research Center for Cancer; Key Laboratory of Cancer Immunology and Biotherapy
| | - Ying Zhao
- Department of Breast Cancer I, Tian Jin Medical University Cancer Institute & Hospital
| | - Zhanyu Pan
- Department of Integrative Oncology, Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer; Key Laboratory of Cancer Prevention and Therapy; Tianjin's Clinical Research Center for Cancer; Key Laboratory of Cancer Immunology and Biotherapy
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13
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Semwal RB, Semwal DK, Combrinck S, Viljoen A. Emodin - A natural anthraquinone derivative with diverse pharmacological activities. PHYTOCHEMISTRY 2021; 190:112854. [PMID: 34311280 DOI: 10.1016/j.phytochem.2021.112854] [Citation(s) in RCA: 88] [Impact Index Per Article: 22.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 05/17/2021] [Revised: 06/19/2021] [Accepted: 06/20/2021] [Indexed: 06/13/2023]
Abstract
Emodin (1,3,8-trihydroxy-6-methyl-anthraquinone) is a natural anthraquinone derivative that is present in numerous globally renowned herbal medicines. It is recognised as a protein tyrosine kinase inhibitor and as an anticancer drug, active against various tumour cells, including lung, breast, liver, and ovarian cancer cells. Recently, its role in combination chemotherapy with various allopathic medicines, to minimize their toxicity and to enhance their efficacy, has been studied. The use of emodin in these therapies is gaining popularity, due to fewer associated side effects compared with standard anticancer drugs. Emodin has a broad therapeutic window, and in addition to its antineoplastic activity, it displays anti-ulcer, anti-inflammatory, hepatoprotective, neuroprotective, antimicrobial, muscle relaxant, immunosuppressive and antifibrotic activities, in both in vitro and in vivo models. Although reviews on the anticancer activity of emodin have been published, none coherently unite all the pharmacological properties of emodin, particularly the anti-oxidant, antimicrobial, antidiabetic, immunosuppressive and hepatoprotective activities of the compound. Hence, in this review, all of the available data regarding the pharmacological properties of emodin are explored, with particular emphasis on the modes of action of the molecule. In addition, the manuscript details the occurrence, biosynthesis and chemical synthesis of the compound, as well as its toxic effects on biotic systems.
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Affiliation(s)
- Ruchi Badoni Semwal
- Department of Pharmaceutical Sciences, Faculty of Science, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa; Department of Chemistry, Pt. Lalit Mohan Sharma Govt. Post Graduate College, Rishikesh, 249201, India
| | - Deepak Kumar Semwal
- Department of Pharmaceutical Sciences, Faculty of Science, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa; Department of Phytochemistry, Faculty of Biomedical Sciences, Uttarakhand Ayurved University, Harrawala, Dehradun, 248001, India
| | - Sandra Combrinck
- Department of Pharmaceutical Sciences, Faculty of Science, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa
| | - Alvaro Viljoen
- Department of Pharmaceutical Sciences, Faculty of Science, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa; SAMRC Herbal Drugs Research Unit, Faculty of Science, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa.
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14
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Wang S, Xue Z, Huang X, Ma W, Yang D, Zhao L, Ouyang H, Chang Y, He J. Comparison of the chemical profile differences of Aster tataricus between raw and processed products by metabolomics coupled with chemometrics methods. J Sep Sci 2021; 44:3883-3897. [PMID: 34405960 DOI: 10.1002/jssc.202100315] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/18/2021] [Revised: 07/25/2021] [Accepted: 08/16/2021] [Indexed: 11/08/2022]
Abstract
Aster tataricus, a traditional Chinese herb, has been used to treat cough and asthma for many years. Its raw and processed products have different pharmacological effects in clinical applications. To explore the chemical profile differences of components in A. tataricus processed with different methods, metabolomics methods based on ultra-high-performance liquid chromatography coupled with quadrupole time of flight mass spectrometry and gas chromatography-mass spectrometry were developed. Chemometrics strategy was applied to filter and screen the candidate compounds. The accuracy of differential markers was validated by back propagation neural network. The established methods showed that raw A. tataricus, honey-processed A. tataricus, vinegar-processed A. tataricus, and steamed A. tataricus were clearly divided into four groups, suggesting that the components were closely related to the processing methods. A total of 64 nonvolatile and 43 volatile compounds were identified in A. tataricus, and 22 nonvolatile and 12 volatile differential constituents were selected to distinguish the raw and processed A. tataricus. This study demonstrated that the metabolomics methods coupled with chemometrics were a comprehensive strategy to analyze the chemical profile differences and provided a reliable reference for quality evaluation of A. tataricus.
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Affiliation(s)
- Songrui Wang
- First Teaching Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China.,National Clinical Research Center for Chinese Medicine Acupuncture and Moxibustion, Tianjin, P. R. China.,State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Zixiang Xue
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Xuhua Huang
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Wenjuan Ma
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Dongyue Yang
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Lulu Zhao
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Huizi Ouyang
- First Teaching Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China.,National Clinical Research Center for Chinese Medicine Acupuncture and Moxibustion, Tianjin, P. R. China.,State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Yanxu Chang
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
| | - Jun He
- State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China
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15
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Chen T, Yang P, Chen HJ, Huang B. A new biflavonoids from Aster tataricus induced non-apoptotic cell death in A549 cells. Nat Prod Res 2021; 36:1409-1415. [PMID: 33615932 DOI: 10.1080/14786419.2021.1882456] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/15/2023]
Abstract
A new biflavonoids, (2R,2''R)-7-O-methyl-2,3,2'',3''-tetrahydrorobustaflavone (1), along with five known flavonoids (2-6) were isolated from the MeOH extract of Aster tataricus. Among them, compounds 1-2 were the C-3'-C-6'' type biflavonoids obtained from the genus Aster for the first time. The structures and absolute configurations of compound 1 was confirmed based on extensive spectroscopic and circular dichroism analyses. Compound 1 exhibited moderate cytotoxicity against seven human cancer A549, HepG2, PC3, DU145, MCF-7, LOVO and NCI-H1975 cell lines. Compound 1 remarkably inhibited the proliferation of A549 cancer cells with IC50 value of 5.4 μM. Further preliminary pharmacological study, 1 induces A549 cell death by non-apoptotic forms through flow cytometry and cell scratch assay data.
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Affiliation(s)
- Ting Chen
- Department of Pharmacy, Guizhou Health Vocational College, Tongren, China
| | - Peng Yang
- Hunan Province Key Laboratory for Antibody-based Drug and Intelligent Delivery System, School of Pharmaceutical Sciences, Hunan University of Medicine, Huaihua, China
| | - Hai-Jun Chen
- Hunan Province Key Laboratory for Antibody-based Drug and Intelligent Delivery System, School of Pharmaceutical Sciences, Hunan University of Medicine, Huaihua, China
| | - Bin Huang
- Hunan Province Key Laboratory for Antibody-based Drug and Intelligent Delivery System, School of Pharmaceutical Sciences, Hunan University of Medicine, Huaihua, China
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16
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Tahir MS, Almezgagi M, Zhang Y, Bashir A, Abdullah HM, Gamah M, Wang X, Zhu Q, Shen X, Ma Q, Ali M, Solangi ZA, Malik WS, Zhang W. Mechanistic new insights of flavonols on neurodegenerative diseases. Biomed Pharmacother 2021; 137:111253. [PMID: 33545661 DOI: 10.1016/j.biopha.2021.111253] [Citation(s) in RCA: 23] [Impact Index Per Article: 5.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/28/2020] [Revised: 12/22/2020] [Accepted: 01/03/2021] [Indexed: 02/06/2023] Open
Abstract
With a large and increasing elderly population, neurodegenerative diseases such as Parkinson's disease (PD), Huntington disease (HD), Alzheimer's disease (AD), Amyotrophic lateral sclerosis (ALS) and Multiple sclerosis (MS) have become a major and growing health problem. During the past few decades, the elderly population has grown 2.5 % every year. Unfortunately, there are no specific therapeutic remedies available to slow the onset or development of these diseases. An aging brain causes many pathophysiological changes and is the major risk factor for most of the neurodegenerative disorders. Polyphenolic compounds such as flavonols have shown therapeutic potential and can contribute to the treatment of these diseases. In this review, evidence for the beneficial neuroprotective effect of multiple flavonols is discussed and their multifactorial cellular pathways for the progressions of age-associated brain changes are identified. Moreover, the animal models of these diseases support the neuroprotective effect and target the potential of flavonols in the treatment of neurodegenerative diseases.
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Affiliation(s)
- Muhammad Shoaib Tahir
- The Key Laboratory of High-Altitude Medical Application of Qinghai Province, Qinghai, Xining, 810001, China; Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Maged Almezgagi
- The Key Laboratory of High-Altitude Medical Application of Qinghai Province, Qinghai, Xining, 810001, China; Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Yu Zhang
- Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Adnan Bashir
- Department of Pharmacology, Fatima Memorial College of Medicine and Dentistry, Punjab Lahore, 54000, Pakistan
| | - Hasnat Mazhar Abdullah
- Department of Emergency Medicine, Milton Keynes University Hospital NHS Foundation Trust, Milton Keynes, MK6 5BY, United Kingdom
| | - Mohammed Gamah
- Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Xiaozhou Wang
- The Key Laboratory of High-Altitude Medical Application of Qinghai Province, Qinghai, Xining, 810001, China
| | - Qinfang Zhu
- The Key Laboratory of High-Altitude Medical Application of Qinghai Province, Qinghai, Xining, 810001, China
| | - Xiangqun Shen
- Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Qianqian Ma
- Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China
| | - Muhammad Ali
- Department of Hepatobiliary Surgery, Qinghai University Affiliated Hospital, Qinghai, Xining, 810001, China
| | - Zeeshan Ahmed Solangi
- Department of Crop Genetics and Breeding, Qinghai Academy of Agricultural and Forestry Sciences, Qinghai University, Xining, 810016, China
| | - Waseem Sami Malik
- Department of Hepatobiliary Surgery, Qinghai University Affiliated Hospital, Qinghai, Xining, 810001, China
| | - Wei Zhang
- The Key Laboratory of High-Altitude Medical Application of Qinghai Province, Qinghai, Xining, 810001, China; Department of Basic Medicine, Medical College of Qinghai University, Qinghai, Xining, 810001, China.
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17
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Boudreau A, Richard AJ, Harvey I, Stephens JM. Artemisia scoparia and Metabolic Health: Untapped Potential of an Ancient Remedy for Modern Use. Front Endocrinol (Lausanne) 2021; 12:727061. [PMID: 35211087 PMCID: PMC8861327 DOI: 10.3389/fendo.2021.727061] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 06/17/2021] [Accepted: 12/16/2021] [Indexed: 11/19/2022] Open
Abstract
Botanicals have a long history of medicinal use for a multitude of ailments, and many modern pharmaceuticals were originally isolated from plants or derived from phytochemicals. Among these, artemisinin, first isolated from Artemisia annua, is the foundation for standard anti-malarial therapies. Plants of the genus Artemisia are among the most common herbal remedies across Asia and Central Europe. The species Artemisia scoparia (SCOPA) is widely used in traditional folk medicine for various liver diseases and inflammatory conditions, as well as for infections, fever, pain, cancer, and diabetes. Modern in vivo and in vitro studies have now investigated SCOPA's effects on these pathologies and its ability to mitigate hepatotoxicity, oxidative stress, obesity, diabetes, and other disease states. This review focuses on the effects of SCOPA that are particularly relevant to metabolic health. Indeed, in recent years, an ethanolic extract of SCOPA has been shown to enhance differentiation of cultured adipocytes and to share some properties of thiazolidinediones (TZDs), a class of insulin-sensitizing agonists of the adipogenic transcription factor PPARγ. In a mouse model of diet-induced obesity, SCOPA diet supplementation lowered fasting insulin and glucose levels, while inducing metabolically favorable changes in adipose tissue and liver. These observations are consistent with many lines of evidence from various tissues and cell types known to contribute to metabolic homeostasis, including immune cells, hepatocytes, and pancreatic beta-cells. Compounds belonging to several classes of phytochemicals have been implicated in these effects, and we provide an overview of these bioactives. The ongoing global epidemics of obesity and metabolic disease clearly require novel therapeutic approaches. While the mechanisms involved in SCOPA's effects on metabolic, anti-inflammatory, and oxidative stress pathways are not fully characterized, current data support further investigation of this plant and its bioactives as potential therapeutic agents in obesity-related metabolic dysfunction and many other conditions.
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Affiliation(s)
- Anik Boudreau
- Adipocyte Biology Laboratory, Pennington Biomedical Research Center, Baton Rouge, LA, United States
| | - Allison J. Richard
- Adipocyte Biology Laboratory, Pennington Biomedical Research Center, Baton Rouge, LA, United States
| | - Innocence Harvey
- Adipocyte Biology Laboratory, Pennington Biomedical Research Center, Baton Rouge, LA, United States
| | - Jacqueline M. Stephens
- Adipocyte Biology Laboratory, Pennington Biomedical Research Center, Baton Rouge, LA, United States
- Department of Biological Sciences, Louisiana State University, Baton Rouge, LA, United States
- *Correspondence: Jacqueline M. Stephens,
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18
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Yang D, Wang S, Huang X, Ma W, Xue Z, Zhao L, Ouyang H, He J. Pharmacokinetic comparison of 15 active compositions in rat plasma after oral administration of raw and honey‐processed
Aster tataricus
extracts. J Sep Sci 2020; 44:908-921. [DOI: 10.1002/jssc.202001020] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/22/2020] [Revised: 11/19/2020] [Accepted: 11/27/2020] [Indexed: 01/18/2023]
Affiliation(s)
- Dongyue Yang
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Songrui Wang
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Xuhua Huang
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Wenjuan Ma
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Zixiang Xue
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Lulu Zhao
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Huizi Ouyang
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
| | - Jun He
- State Key Laboratory of Component‐based Chinese Medicine Tianjin University of Traditional Chinese Medicine Tianjin P.R. China
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19
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Wang X, Fan L, Yin H, Zhou Y, Tang X, Fei X, Tang H, Peng J, Ren X, Xue Y, Zhu C, Luo J, Jin Q, Jin Q. Protective effect of Aster tataricus extract on NLRP3-mediated pyroptosis of bladder urothelial cells. J Cell Mol Med 2020; 24:13336-13345. [PMID: 33030301 PMCID: PMC7701514 DOI: 10.1111/jcmm.15952] [Citation(s) in RCA: 20] [Impact Index Per Article: 4.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/17/2020] [Revised: 08/17/2020] [Accepted: 08/29/2020] [Indexed: 12/16/2022] Open
Abstract
Aster tataricus L.f. is a traditional Eastern Asian herbal medicine used for the relief of uroschesis‐related illnesses and has been demonstrated clinically to exert satisfied effects. However, the mechanism of its therapeutic action remains unclear. The present study aimed to evaluate the protective mechanism of Aster tataricus extract (ATE) on CYP or LPS + ATP‐induced interstitial cystitis (IC), we successfully constructed the induced IC Sprague‐Dawley (SD) rat model and IC human urothelium cell (SV‐HUC‐1) model. The main compounds of ATE were determined by LC‐MS. After intervention, the changes on the bladder wall morphology and inflammation were observed in each group. SV‐HUC1 cell viability was measured by MTT and double stained with Hoechst 33342 and propidium iodide (PI). The expression levels of NLRP3, Pro‐caspase‐1, Caspsae‐1 p20, GSDMD, GSDMD‐N and Cleave‐IL‐1β in vivo and in vitro in different groups were detected by Western blotting. ATE significantly alleviated oedema and haemorrhage and reduced the inflammation index and histopathological score in SD rat bladder. The results of cell revealed that ATE could improve cell viability and decrease pyroptosis ratio. The expression of NLRP3 and other pyroptosis‐related protein was remarkably decreased by ATE both in vivo and in vitro. ATE may be used as an inhibitor of NLRP3 in treating IC. The discovery of NLRP3/Caspase‐1/GSDMD‐N as a new protective pathway provides a new direction for protecting cell against IC.
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Affiliation(s)
- Xin Wang
- Department of Nephrology, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China.,Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Ling Fan
- Department of Pharmacy, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Hao Yin
- Department of Nephrology, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China.,Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Yiqun Zhou
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Xiaolong Tang
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Xiaojun Fei
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Hailin Tang
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Juan Peng
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Xiaoqin Ren
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Yi Xue
- Department of Nephrology, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Chunli Zhu
- Department of Nephrology, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Jianping Luo
- Department of Nephrology, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Qinglei Jin
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
| | - Qingjiang Jin
- Li Shicai School Inheritance Studio, Suzhou Hospital of Integrated Traditional Chinese and Western Medicine, Suzhou, China
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20
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Rho J, Seo CS, Park HS, Jeong HY, Moon OS, Seo YW, Son HY, Won YS, Kwun HJ. Asteris Radix et Rhizoma suppresses testosterone-induced benign prostatic hyperplasia in rats by regulating apoptosis and inflammation. JOURNAL OF ETHNOPHARMACOLOGY 2020; 255:112779. [PMID: 32209388 DOI: 10.1016/j.jep.2020.112779] [Citation(s) in RCA: 13] [Impact Index Per Article: 2.6] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 09/05/2019] [Revised: 03/17/2020] [Accepted: 03/18/2020] [Indexed: 06/10/2023]
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE Asteris Radix et Rhizoma (AR) refers to the roots and rhizomes of Aster tataricus L., which is widely distributed throughout East Asia. AR has been consumed as a traditional medicine in Korea, Japan and China for the treatment of urologic symptoms. To date, however, the therapeutic effect of AR on benign prostatic hyperplasia (BPH) has not been investigated. AIM OF THE STUDY The present study evaluated the therapeutic effects of AR on a testosterone-induced BPH rats. MATERIALS AND METHODS We induced BPH to rats by subcutaneous injections (s.c) of testosterone propionate (TP) daily for four weeks. Rats were also administered daily oral gavage of AR (150 mg/kg) or vehicle. After four weeks of induction, all animals were euthanized humanely and their prostate glands were removed, weighed and processed for further analysis, including histopathological examination, real-time PCR, terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay and Western blot analysis. RESULTS Administration of AR to TP-induced BPH rats considerably reduced prostate weight and concentrations of serum testosterone and prostate dihydrotestosterone (DHT). Epithelial thickness and expression of proliferating cell nuclear antigen (PCNA) were markedly suppressed by AR-treatment in the rats. Furthermore, the expression of the B-cell lymphoma 2 (Bcl-2) were reduced and expression of the Bcl-2-associated X protein (Bax) increased, resulting in significant reduction in Bcl-2/Bax ratio. In addition, AR decreased the level of pro-inflammatory cytokines, including interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). The expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) were reduced by AR treatment in a TP-induced BPH rat model. CONCLUSIONS AR alleviates BPH by promoting apoptosis and suppressing inflammation, indicating that AR may be used clinically to treat BPH accompanied by inflammation.
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Affiliation(s)
- Jinhyung Rho
- Department of Veterinary Pathology, College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
| | - Chang-Seob Seo
- Research Infrastructure Team, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
| | - Hee-Seon Park
- Department of Veterinary Pathology, College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
| | - Hye-Yun Jeong
- Department of Veterinary Pathology, College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
| | - Og-Sung Moon
- Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk, South Korea.
| | - Young-Won Seo
- Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk, South Korea.
| | - Hwa-Young Son
- Department of Veterinary Pathology, College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
| | - Young-Suk Won
- Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk, South Korea.
| | - Hyo-Jung Kwun
- Department of Veterinary Pathology, College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
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21
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Ma W, Yao G, Huang X, Jia Q, Shen J, Chang Y, Ouyang H, He J. Comparison of the active components of
Aster tataricus
from different regions and related processed products by ultra‐high performance liquid chromatography with tandem mass spectrometry. J Sep Sci 2020; 43:865-876. [DOI: 10.1002/jssc.201900814] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/07/2019] [Revised: 11/20/2019] [Accepted: 12/01/2019] [Indexed: 11/09/2022]
Affiliation(s)
- Wenjuan Ma
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Guangzhe Yao
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Xuhua Huang
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Qi Jia
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Jiayuan Shen
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Yanxu Chang
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Huizi Ouyang
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
- First Teaching Hospital of Tianjin University of Traditional Chinese Medicine Tianjin P. R. China
| | - Jun He
- Tianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese Medicine Tianjin P. R. China
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Jang JH, Park JE, Han JS. Scopoletin increases glucose uptake through activation of PI3K and AMPK signaling pathway and improves insulin sensitivity in 3T3-L1 cells. Nutr Res 2019; 74:52-61. [PMID: 31945607 DOI: 10.1016/j.nutres.2019.12.003] [Citation(s) in RCA: 28] [Impact Index Per Article: 4.7] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/23/2019] [Revised: 12/01/2019] [Accepted: 12/04/2019] [Indexed: 12/16/2022]
Abstract
Coumarins have been shown to reduce blood glucose levels and improve insulin sensitivity in other studies. The purpose of this study was to investigate the effects of scopoletin, which is a type of coumarin family, on glucose uptake in 3T3-L1 cells to test the hypothesis that scopoletin exerts an antidiabetic function on adipocytes. Scopoletin significantly increased glucose uptake, which was associated with increased expression of the plasma membrane glucose transporter type 4 (PM-GLUT4) in 3T3-L1 adipocytes. This increase in PM-GLUT4 expression was promoted by phosphorylation of protein kinase B, activation of phosphatidylinositol-3-kinase (PI3K), and enhanced intracellular glucose uptake. Scopoletin also promoted phosphorylation of adenosine monophosphate-activated protein kinase (AMPK) and enhanced PM-GLUT4 expression. Scopoletin-induced glucose uptake in 3T3-L1 adipocytes was inhibited by treatment with the PI3K inhibitor wortmannin and the AMPK inhibitor compound C. These results suggest that scopoletin has an antidiabetic effect by stimulating GLUT4 translocation to the PM through activation of the PI3K and AMPK pathways in 3T3-L1 adipocytes, thereby upregulating glucose uptake.
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Affiliation(s)
- June Hyuk Jang
- Department of Food Science and Nutrition, Pusan National University, Busan 46241, Republic of Korea; Department of Food Science and Nutrition and Kimchi Research Institute, Pusan National University, Busan 46241, Republic of Korea
| | - Jae Eun Park
- Department of Food Science and Nutrition, Pusan National University, Busan 46241, Republic of Korea; Department of Food Science and Nutrition and Kimchi Research Institute, Pusan National University, Busan 46241, Republic of Korea
| | - Ji Sook Han
- Department of Food Science and Nutrition, Pusan National University, Busan 46241, Republic of Korea; Department of Food Science and Nutrition and Kimchi Research Institute, Pusan National University, Busan 46241, Republic of Korea.
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23
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Antitumor astins originate from the fungal endophyte Cyanodermella asteris living within the medicinal plant Aster tataricus. Proc Natl Acad Sci U S A 2019; 116:26909-26917. [PMID: 31811021 DOI: 10.1073/pnas.1910527116] [Citation(s) in RCA: 38] [Impact Index Per Article: 6.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/18/2022] Open
Abstract
Medicinal plants are a prolific source of natural products with remarkable chemical and biological properties, many of which have considerable remedial benefits. Numerous medicinal plants are suffering from wildcrafting, and thus biotechnological production processes of their natural products are urgently needed. The plant Aster tataricus is widely used in traditional Chinese medicine and contains unique active ingredients named astins. These are macrocyclic peptides showing promising antitumor activities and usually containing the highly unusual moiety 3,4-dichloroproline. The biosynthetic origins of astins are unknown despite being studied for decades. Here we show that astins are produced by the recently discovered fungal endophyte Cyanodermella asteris We were able to produce astins in reasonable and reproducible amounts using axenic cultures of the endophyte. We identified the biosynthetic gene cluster responsible for astin biosynthesis in the genome of C. asteris and propose a production pathway that is based on a nonribosomal peptide synthetase. Striking differences in the production profiles of endophyte and host plant imply a symbiotic cross-species biosynthesis pathway for astin C derivatives, in which plant enzymes or plant signals are required to trigger the synthesis of plant-exclusive variants such as astin A. Our findings lay the foundation for the sustainable biotechnological production of astins independent from aster plants.
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24
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Hsueh CC, Wu CC, Chen BY. Polyphenolic compounds as electron shuttles for sustainable energy utilization. BIOTECHNOLOGY FOR BIOFUELS 2019; 12:271. [PMID: 31832094 PMCID: PMC6859638 DOI: 10.1186/s13068-019-1602-9] [Citation(s) in RCA: 23] [Impact Index Per Article: 3.8] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 07/20/2019] [Accepted: 10/25/2019] [Indexed: 05/05/2023]
Abstract
For renewable and sustainable bioenergy utilization with cost-effectiveness, electron-shuttles (ESs) (or redox mediators (RMs)) act as electrochemical "catalysts" to enhance rates of redox reactions, catalytically accelerating electron transport efficiency for abiotic and biotic electrochemical reactions. ESs are popularly used in cellular respiratory systems, metabolisms in organisms, and widely applied to support global lives. Apparently, they are applicable to increase power-generating capabilities for energy utilization and/or fuel storage (i.e., dye-sensitized solar cell, batteries, and microbial fuel cells (MFCs)). This first-attempt review specifically deciphers the chemical structure association with characteristics of ESs, and discloses redox-mediating potentials of polyphenolics-abundant ESs via MFC modules. Moreover, to effectively convert electron-shuttling capabilities from non-sustainable antioxidant activities, environmental conditions to induce electrochemical mediation apparently play critical roles of great significance for bioenergy stimulation. For example, pH levels would significantly affect electrochemical potentials to be exhibited (e.g., alkaline pHs are electrochemically favorable for expression of such electron-shuttling characteristics). Regarding chemical structure effect, chemicals with ortho- and para-dihydroxyl substituents-bearing aromatics own convertible characteristics of non-renewable antioxidants and electrochemically catalytic ESs; however, ES capabilities of meta-dihydroxyl substituents can be evidently repressed due to lack of resonance effect in the structure for intermediate radical(s) during redox reaction. Moreover, this review provides conclusive remarks to elucidate the promising feasibility to identify whether such characteristics are non-renewable antioxidants or reversible ESs from natural polyphenols via cyclic voltammetry and MFC evaluation. Evidently, considering sustainable development, such electrochemically convertible polyphenolic species in plant extracts can be reversibly expressed for bioenergy-stimulating capabilities in MFCs under electrochemically favorable conditions.
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Affiliation(s)
- Chung-Chuan Hsueh
- Department of Chemical and Materials Engineering, National I-Lan University, I-Lan, 26047 Taiwan
| | - Chia-Chyi Wu
- Department of Horticulture, National I-Lan University, I-Lan, 26047 Taiwan
| | - Bor-Yann Chen
- Department of Chemical and Materials Engineering, National I-Lan University, I-Lan, 26047 Taiwan
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25
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Su XD, Jang HJ, Li HX, Kim YH, Yang SY. Identification of potential inflammatory inhibitors from Aster tataricus. Bioorg Chem 2019; 92:103208. [PMID: 31473471 DOI: 10.1016/j.bioorg.2019.103208] [Citation(s) in RCA: 14] [Impact Index Per Article: 2.3] [Reference Citation Analysis] [Abstract] [Key Words] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/21/2019] [Revised: 07/25/2019] [Accepted: 08/15/2019] [Indexed: 12/12/2022]
Abstract
Aster tataricus L.f. is a traditional Eastern Asian herbal medicine used for the relief of cough-related illnesses. In this study, 32 known compounds and two novel monoterpene glycosides were isolated from the roots of A. tataricus. With the aid of reported data, elucidation of the root-extract components was carried out using a multitude of spectroscopic techniques. All isolates were investigated for their ability to inhibit nitric oxide (NO) secretion in lipopolysaccharide-activated RAW264.7 cells. Compound 7 remarkably suppressed NO production with an IC50 value of 8.5 µM. In addition, compound 7 exhibited significant inhibitory activity against the production of inflammatory cytokines (prostaglandin E2, interleukin-6, and interleukin-1 beta) and the expression of inflammatory enzymes (inducible nitric oxide synthase and cyclooxygenase-2) via inhibition of nuclear factor-kappa B activation. Moreover, compound 7 effectively prevented the downstream activation of the mitogen-activated protein kinase signaling pathway by inhibiting phosphorylation of c-Jun N-terminal kinases, extracellular signal-regulated kinases, and p38. These results outline compound 7 as a potential inhibitor for the broad treatment of inflammatory diseases, such as atopic dermatitis, asthma, and various allergies.
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Affiliation(s)
- Xiang Dong Su
- College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea
| | - Hyun-Jae Jang
- Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, 30 Cheongju, Chungbuk 28116, Republic of Korea
| | - Hong Xu Li
- College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea
| | - Young Ho Kim
- College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
| | - Seo Young Yang
- College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
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Su XD, Jang HJ, Wang CY, Lee SW, Rho MC, Kim YH, Yang SY. Anti-inflammatory Potential of Saponins from Aster tataricus via NF-κB/MAPK Activation. JOURNAL OF NATURAL PRODUCTS 2019; 82:1139-1148. [PMID: 30931559 DOI: 10.1021/acs.jnatprod.8b00856] [Citation(s) in RCA: 24] [Impact Index Per Article: 4.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 05/17/2023]
Abstract
Four new aster saponins (1-4) together with five known analogues (5-9) were isolated from Aster tataricus. The chemical structures of 1-4 were elucidated based on spectrometric and spectroscopic analysis and comparison with reported data. The potential anti-inflammatory activities of aster saponins 1-9 were evaluated subsequently by measuring lipopolysaccharide (LPS)-enhanced nitric oxide (NO) formation in murine macrophages. Among these, aster saponin B (6) exhibited the most potent inhibitory activity (IC50: 1.2 μM). Additionally, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein levels were dose-dependently suppressed by 6 in LPS-activated RAW 264.7 cells. Investigation of the anti-inflammatory mechanism indicated that 6 attenuated the phosphorylation and degradation of the inhibitor of NF-κB (IκB), which led to the blocking of NF-κB p65 translocation to the nucleus.
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Affiliation(s)
- Xiang-Dong Su
- College of Pharmacy , Chungnam National University , Daejeon 34134 , Korea
| | - Hyun-Jae Jang
- Immunoregulatory Material Research Center , Korea Research Institute of Bioscience and Biotechnology , 181 Ipsin-gil , Jeongeup, Jeonbuk 56212 , Korea
| | - Cai-Yi Wang
- College of Pharmacy , Chungnam National University , Daejeon 34134 , Korea
| | - Seung Woong Lee
- Immunoregulatory Material Research Center , Korea Research Institute of Bioscience and Biotechnology , 181 Ipsin-gil , Jeongeup, Jeonbuk 56212 , Korea
| | - Mun-Chual Rho
- Immunoregulatory Material Research Center , Korea Research Institute of Bioscience and Biotechnology , 181 Ipsin-gil , Jeongeup, Jeonbuk 56212 , Korea
| | - Young Ho Kim
- College of Pharmacy , Chungnam National University , Daejeon 34134 , Korea
| | - Seo Young Yang
- College of Pharmacy , Chungnam National University , Daejeon 34134 , Korea
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27
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Zhou H, Zhang YQ, Lai T, Liu XJ, Guo FY, Guo T, Ding W. Acaricidal Mechanism of Scopoletin Against Tetranychus cinnabarinus. Front Physiol 2019; 10:164. [PMID: 30894818 PMCID: PMC6414448 DOI: 10.3389/fphys.2019.00164] [Citation(s) in RCA: 15] [Impact Index Per Article: 2.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/17/2018] [Accepted: 02/11/2019] [Indexed: 01/10/2023] Open
Abstract
Scopoletin is a promising acaricidal botanical natural compound against Tetranychus cinnabarinus, and its acaricidal mechanism maybe involve calcium overload according to our previous study. To seek potential candidate target genes of calcium overload induced by scopoletin in T. cinnabarinus, RNA-seq was utilized to detect changes in transcription levels. 24 and 48 h after treatment, 70 and 102 differentially expressed genes were obtained, respectively. Target genes included 3 signal transduction genes, 4 cell apoptosis genes, 4 energy metabolism genes, and 2 transcription factor genes. The role of 3 calcium signaling pathway-related genes, namely, G-protein-coupled neuropeptide receptor, Bcl-2 protein and guanylate kinase (designated TcGPCR, TcBAG, and TcGUK, respectively) in the calcium overload were investigated in this study. RT-qPCR detection showed that scopoletin treatment upregulated the expression level of TcGPCR and downregulated the expression level of TcBAG and TcGUK. The result of RNAi indicated that downregulation of TcGPCR decreased susceptibility to scopoletin, and downregulation of TcBAG and TcGUK enhanced susceptibility to scopoletin. Functional expression in Chinese hamster ovary cells showed that scopoletin induced a significant increase in intracellular free calcium [Ca2+]i levels by activating TcGPCR. These results demonstrated that the acaricidal mechanism of scopoletin was via disrupting intracellular Ca2+ homeostasis and calcium signaling pathway mediated by GPCR, BAG, and GUK.
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Affiliation(s)
| | | | | | | | | | | | - Wei Ding
- Institute of Pesticide Science, College of Plant Protection, Southwest University, Chongqing, China
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28
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Antioxidant potential of essential oils from some Himalayan Asteraceae and Lamiaceae species. MEDICINE IN DRUG DISCOVERY 2019. [DOI: 10.1016/j.medidd.2019.100004] [Citation(s) in RCA: 12] [Impact Index Per Article: 2.0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/31/2023] Open
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Li S, Zhang Q, Li P. Protective Effects of Epifriedelinol in a Rat Model of Traumatic Brain Injury Assessed with Histological and Hematological Markers. Transl Neurosci 2018; 9:38-42. [PMID: 30425851 PMCID: PMC6227786 DOI: 10.1515/tnsci-2018-0008] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.4] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/17/2017] [Accepted: 02/20/2018] [Indexed: 11/20/2022] Open
Abstract
Background This study evaluated the protective effects of epifriedelinol (EFD) in a rat model of traumatic brain injury (TBI). Methodology TBI was induced by dropping a weight from a specific height. The animals were separated into control, TBI, and EFD 100 and 200 mg/kg groups. The latter received 100 and 200 mg/kg EFD, respectively, for 2 days beginning 30 min after inducing TBI. The neurological examination score, permeability of the blood–brain barrier (BBB), water content of the brain, cytokine levels, and oxidative stress parameters were measured in the rats. The effects of EFD on glial fibrillary acidic protein (GFAP)-positive cells were evaluated using immunohistochemistry. Result The EFD treatment significantly decreased the neurological score, permeability of the BBB, and water content of brain compared with the TBI group. The levels of interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and oxidative stress were significantly decreased in the EFD-treated groups. The number of GFAP-positive cells was also significantly reduced in the EFD-treated groups. Conclusion EFD attenuates the secondary injury in TBI rats by reducing the serum cytokine levels and oxidative stress.
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Affiliation(s)
- Shiping Li
- Urgent Care Centre, Lanzhou University Second Hospital, Lanzhou, Gansu province, 730030, P R China
| | - Qiaoying Zhang
- School of Life Sciences, Lanzhou University, Lanzhou, Gansu province, 730030, P R China
| | - Peiwu Li
- School of Life Sciences, Lanzhou University, Lanzhou, Gansu province, 730030, P R China
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30
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Luo J, Lai T, Guo T, Chen F, Zhang L, Ding W, Zhang Y. Synthesis and Acaricidal Activities of Scopoletin Phenolic Ether Derivatives: QSAR, Molecular Docking Study and in Silico ADME Predictions. Molecules 2018; 23:E995. [PMID: 29695088 PMCID: PMC6102537 DOI: 10.3390/molecules23050995] [Citation(s) in RCA: 19] [Impact Index Per Article: 2.7] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/03/2018] [Revised: 04/15/2018] [Accepted: 04/18/2018] [Indexed: 01/27/2023] Open
Abstract
Thirty phenolic ether derivatives of scopoletin modified at the 7-hydroxy position were synthesized, and their structures were confirmed by IR, ¹H-NMR, 13C-NMR, MS and elemental analysis. Preliminary acaricidal activities of these compounds against female adults of Tetranychus cinnabarinus (Boisduval) were evaluated using the slide-dip method. The results indicated that some of these compounds exhibit more pronounced acaricidal activity than scopoletin, especially compounds 32, 20, 28, 27 and 8 which exhibited about 8.41-, 7.32-, 7.23-, 6.76-, and 6.65-fold higher acaricidal potency. Compound 32 possessed the the most promising acaricidal activity and exhibited about 1.45-fold higher acaricidal potency against T. cinnabarinus than propargite. Statistically significant 2D-QSAR model supports the observed acaricidal activities and reveals that polarizability (HATS5p) was the most important parameter controlling bioactivity. 3D-QSAR (CoMFA: q² = 0.802, r² = 0.993; CoMSIA: q² = 0.735, r² = 0.965) results show that bulky substituents at R₄, R₁, R₂ and R₅ (C₆, C₃, C₄, and C₇) positions, electron positive groups at R₅ (C₇) position, hydrophobic groups at R₁ (C₃) and R₂ (C₄), H-bond donors groups at R₁ (C₃) and R₄ (C₆) will increase their acaricidal activity, which provide a good insight into the molecular features relevant to the acaricidal activity for further designing novel acaricidal agents. Molecular docking demonstrates that these selected derivatives display different bide modes with TcPMCA1 from lead compound and they interact with more key amino acid residues than scopoletin. In silico ADME properties of scopoletin and its phenolic ether derivatives were also analyzed and showed potential to develop as good acaricidal candidates.
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Affiliation(s)
- Jinxiang Luo
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Ting Lai
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Tao Guo
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Fei Chen
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Linli Zhang
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Wei Ding
- College of Plant Protection, Southwest University, Chongqing 400715, China.
| | - Yongqiang Zhang
- College of Plant Protection, Southwest University, Chongqing 400715, China.
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32
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Jahn L, Schafhauser T, Wibberg D, Rückert C, Winkler A, Kulik A, Weber T, Flor L, van Pée KH, Kalinowski J, Ludwig-Müller J, Wohlleben W. Linking secondary metabolites to biosynthesis genes in the fungal endophyte Cyanodermella asteris: The anti-cancer bisanthraquinone skyrin. J Biotechnol 2017. [PMID: 28647529 DOI: 10.1016/j.jbiotec.2017.06.410] [Citation(s) in RCA: 30] [Impact Index Per Article: 3.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/21/2022]
Abstract
Fungal aromatic polyketides display a very diverse and widespread group of natural products. Due to their excellent light absorption properties and widely studied biological activities, they offer numerous application for food, textile and pharmaceutical industry. The biosynthetic pathways of fungal aromatic polyketides usually involve a set of successive enzymes, in which a non-reductive polyketide synthase iteratively catalyzes the essential assembly of simple building blocks into (often polycyclic) aromatic compounds. However, only a limited number of such pathways have been described so far and further elucidation of the individual biosynthetic steps is needed to fully exploit the biotechnological and medicinal potential of these compounds. Here, we identified the bisanthraquinone skyrin as the main pigment of the fungus Cyanodermella asteris, an endophyte that has recently been isolated from the traditional Chinese medicinal plant Aster tataricus. The genome of C. asteris was sequenced, assembled and annotated, which enables first insights into a genome from a non-lichenized member of the class Lecanoromycetes. Genetic and in silico analyses led to the identification of a gene cluster of five genes suggested to encode the enzymatic pathway for skyrin. Our study is a starting point for rational pathway engineering in order to drive the production towards higher yields or more active derivatives. Moreover, our investigations revealed a large potential of secondary metabolite production in C. asteris as well as in all Lecanoromycetes of which genomes were available. These findings convincingly emphasize that Lecanoromycetes are prolific producers of secondary metabolites.
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Affiliation(s)
- Linda Jahn
- Institut für Botanik, Technische Universität Dresden, 01062 Dresden, Germany
| | - Thomas Schafhauser
- Mikrobiologie und Biotechnologie, Interfakultäres Institut für Mikrobiologie und Infektionsmedizin, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 28, 72076 Tübingen, Germany.
| | - Daniel Wibberg
- Centrum für Biotechnologie, CeBiTec, Universität Bielefeld, Universitätsstr. 27, 33615 Bielefeld, Germany
| | - Christian Rückert
- Centrum für Biotechnologie, CeBiTec, Universität Bielefeld, Universitätsstr. 27, 33615 Bielefeld, Germany
| | - Anika Winkler
- Centrum für Biotechnologie, CeBiTec, Universität Bielefeld, Universitätsstr. 27, 33615 Bielefeld, Germany
| | - Andreas Kulik
- Mikrobiologie und Biotechnologie, Interfakultäres Institut für Mikrobiologie und Infektionsmedizin, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 28, 72076 Tübingen, Germany
| | - Tilmann Weber
- Mikrobiologie und Biotechnologie, Interfakultäres Institut für Mikrobiologie und Infektionsmedizin, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 28, 72076 Tübingen, Germany; The Novo Nordisk Foundation Center for Biosustainability, Technical University of Denmark, Kemitorvet Bygning 220, 2800 Kgs. Lyngby, Denmark; German Centre for Infection Research (DZIF), Partner site Tübingen, IMIT, Auf der Morgenstelle 28, 72076 Tübingen, Germany
| | - Liane Flor
- Allgemeine Biochemie, Technische Universität Dresden, 01062 Dresden, Germany
| | - Karl-Heinz van Pée
- Allgemeine Biochemie, Technische Universität Dresden, 01062 Dresden, Germany
| | - Jörn Kalinowski
- Centrum für Biotechnologie, CeBiTec, Universität Bielefeld, Universitätsstr. 27, 33615 Bielefeld, Germany
| | - Jutta Ludwig-Müller
- Institut für Botanik, Technische Universität Dresden, 01062 Dresden, Germany.
| | - Wolfgang Wohlleben
- Mikrobiologie und Biotechnologie, Interfakultäres Institut für Mikrobiologie und Infektionsmedizin, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 28, 72076 Tübingen, Germany; German Centre for Infection Research (DZIF), Partner site Tübingen, IMIT, Auf der Morgenstelle 28, 72076 Tübingen, Germany
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Yang J, Fa J, Li B. APOPTOSIS INDUCTION OF EPIFRIEDELINOL ON HUMAN CERVICAL CANCER CELL LINE. AFRICAN JOURNAL OF TRADITIONAL, COMPLEMENTARY, AND ALTERNATIVE MEDICINES 2017. [PMID: 28638870 PMCID: PMC5471486 DOI: 10.21010/ajtcam.v14i4.10] [Citation(s) in RCA: 9] [Impact Index Per Article: 1.1] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Indexed: 12/02/2022]
Abstract
Background: Present investigation evaluates the antitumor activity of epifriedelinol for the management of cervical cancer by inducing process of apoptosis. Methods: Human Cervical Cancer Cell Line, C33A and HeLa were selected for study and treated with epifriedelinol at a concentration of (50-1000 µg/ml). Cytotoxicity of epifriedelinol was estimated by MTT assay and induction of apoptosis was assessed by estimating the activity of caspase 3, 8 and 9 enzyme, apoptosis assay and translocation of cytochrome c. Moreover an expression of several proteins that plays role in the apoptosis process was estimated by western blot method. Results: Result of the study suggested that treatment with epifriedelinol significantly decrease the viability count of cancerous cell in a dose perndent manner and also enhances the formation of oligonucleosome in both the cell lines. However activity of caspase enzymes and translocation of cytochrome c were enhanced after treatment with epifriedelinol. It was also observed that epifriedelinol treatment alters the ratio of pro-apoptotic to anti-apoptotic proteins and enhances the expressions of inhibitor of apoptosis proteins (IAP). Conclusion: Result of our study proves the anticancer activity of epifriedelinol in cervical cancer by inducing apoptosis as treatment with it enhances the production of oligonucleosomes, translocation of cytochrome c and activity caspase enzymes.
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Affiliation(s)
- Jie Yang
- Women's Health Center, Women and Children's Hospital of LinYi, Linyi, Shandong, China, 276000
| | - Jing Fa
- Department of Gynaecology, Linyi Cancer Hospital, Linyi, Shandong, China, 276000
| | - Bingxing Li
- Department of Obstetrics, Women and Children's Hospital of LinYi, Linyi, Shandong, China, 276000
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Du H, Zhang M, Yao K, Hu Z. Protective effect of Aster tataricus extract on retinal damage on the virtue of its antioxidant and anti-inflammatory effect in diabetic rat. Biomed Pharmacother 2017; 89:617-622. [DOI: 10.1016/j.biopha.2017.01.179] [Citation(s) in RCA: 14] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/17/2017] [Revised: 01/23/2017] [Accepted: 01/23/2017] [Indexed: 12/18/2022] Open
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Peng WJ, Xin RH, Luo YJ, Liang G, Ren LH, Liu Y, Wang GB, Zheng JF. EVALUATION OF THE ACUTE AND SUBCHRONIC TOXICITY OF Aster tataricus L. F. AFRICAN JOURNAL OF TRADITIONAL, COMPLEMENTARY, AND ALTERNATIVE MEDICINES 2016; 13:38-53. [PMID: 28480359 PMCID: PMC5412200 DOI: 10.21010/ajtcam.v13i6.8] [Citation(s) in RCA: 9] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Indexed: 01/01/2023]
Abstract
BACKGROUND Aster tataricus L. f. is used as a traditional Chinese drug to relieve cough and asthma symptoms and to eliminate phlegm. However, Aster tataricus L. f. possesses toxicity, and little systematic research has been conducted on its toxic effects in the laboratory. METHODS AND MATERIALS The acute group was administered 75% alcohol extract of Aster tataricus L. f. in a single dose. A subchronic toxicity study was performed via daily oral administration of Aster tataricus L. f. at a dose of 0.34 g/kg body weight in SD rats. The rats were divided into six groups: a petroleum ether extract (PEA) group, an ethyl acetate extract (EEA) group, an n-butyl alcohol extract (NEA) group, a remaining lower aqueous phases (REA) group, a 75% alcohol extract (AEA) group and a control group. Quantitative measurements of cytokines were obtained by fluorescence with a laser scanner using a Cy3 equivalent dye. RESULTS The LD50 of the 75% alcohol extract of Aster tataricus L. f. was 15.74 g/kg bw. In the subchronic toxicity study, no significant differences were observed among groups in relative organ weights, urine traits, liver antioxidase levels, or cytokine levels. However, significant sporadic differences were observed in body weight gains, haematology indices, biochemistry values, and histopathology features in PEA, EEA group. In addition, sporadic changes in other groups in measures such as WBC, MCHC, CK, ALP, AST, ALT, LDH, T-BIL, LDL-C, HDL-C, and TC were observed. CONCLUSION The toxicity study showed that Aster tataricus L. f. can produce toxic effects, mainly on the liver; much less on the heart. The LD50 was 15.74 g/kg BW in mice, and the subchronic toxicity study, used a dosage of 0.34 g/kg/d.BW, showed that the toxic components of Aster tataricus L. f. were mainly concentrated in the petroleum ether fraction, followed by the ethyl acetate fraction, the n-butyl alcohol fraction, the lower aqueous phase and the 75% ethanol extracts. Abbreviations: PEA, petroleum ether extract of Aster tataricus L. f.; EEA, ethyl acetate extract of Aster tataricus L. f.; NEA: n-butyl alcohol extract of Aster tataricus L. f.; REA: lower aqueous phases of Aster tataricus L. f.; AEA, 75% alcohol extract of Aster tataricus L. f.; WBC, white blood cell; RBC, red blood cell, PLT, platelet; HCT, haematocrit; MCV, mean corpuscular volume; HGB, haemoglobin; MCH, mean corpuscular haemoglobin; MCHC, mean corpuscular haemoglobin concentration; CREA, creatinine; LDH, lactate dehydrogenase; HDL-C, high-density lipoprotein cholesterol; LDL-C, low-density lipoprotein cholesterol; T-BIL, total bilirubin; ALT, alanine aminotransferase; ALP, alkaline phosphatase; AST, aspartate aminotransferase; TP, total protein; ALB, albumin; Glu, glucose; TC, total cholesterol; TG, triglycerides; CK, creatine kinase; GSH, Glutathione; MDA, malondialdehyde; T-SOD, total superoxide dismutase; TNF, tumour necrosis factor; IFN, interferon; MCP, monocyte chemotactic protein C.
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Affiliation(s)
- Wen-Jing Peng
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Rui-Hua Xin
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Yong-Jiang Luo
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Ge Liang
- Sichuan Animal Science Academy, Chengdu 610066, PR China
| | - Li-Hua Ren
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Yan Liu
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Gui-Bo Wang
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
| | - Ji-Fang Zheng
- Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Key Laboratory of New Animal Drug Project of Gansu Province, Engineering & Technology Research Center of Traditional Chinese Veterinary Medicine of Gansu Province, Key Laboratory of Veterinary Pharmaceutics Development, Ministry of Agriculture, Lanzhou 730050, PR China
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Zhang WM, Wang W, Zhang JJ, Wang ZR, Wang Y, Hao WJ, Huang WY. Antibacterial Constituents of HainanMorinda citrifolia(Noni) Leaves. J Food Sci 2016; 81:M1192-6. [DOI: 10.1111/1750-3841.13302] [Citation(s) in RCA: 23] [Impact Index Per Article: 2.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/24/2015] [Revised: 02/26/2016] [Accepted: 03/18/2016] [Indexed: 12/12/2022]
Affiliation(s)
- Wei-Min Zhang
- College of Food Science and Technology; Huazhong Agricultural Univ; Hubei 430070 PR China
| | - Wei Wang
- College of Food Science and Technology; Huazhong Agricultural Univ; Hubei 430070 PR China
| | - Jing-Jing Zhang
- College of Food Science; Hainan Univ; Haikou 570228 PR China
| | - Zhi-Rong Wang
- College of Food Science; Hainan Univ; Haikou 570228 PR China
| | - Yu Wang
- College of Food Science; Hainan Univ; Haikou 570228 PR China
| | - Wang-Jun Hao
- College of Food Science; Hainan Univ; Haikou 570228 PR China
| | - Wu-Yang Huang
- Inst. of Farm Product Processing; Jiangsu Academy of Agricultural Sciences; PR China
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Yang H, Shi H, Zhang Q, Liu Y, Wan C, Zhang L. Simultaneous Determination of Five Components in Aster tataricus by Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry. J Chromatogr Sci 2015; 54:500-6. [PMID: 26620425 DOI: 10.1093/chromsci/bmv171] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/01/2014] [Indexed: 11/14/2022]
Abstract
A novel quantitative method using high-performance liquid chromatography coupled to electrospray ionization tandem mass spectrometry was developed for simultaneous determination of the important active constituents including shionone, luteolin, quercetin, kaempferol and ferulic acid in Aster tataricus from different habitats. The separation was performed on a C18 column with acidified aqueous acetonitrile gradients. Quantification of the analytes was achieved by the use of a hybrid quadrupole spectrometer. Multiple reaction monitoring scanning was employed with positive and negative modes at the same time in a single run. The validated results of the method indicated that the method was simple, rapid, specific and reliable. The results demonstrated that the quantitative difference in content of five active compounds was useful not only for chemotaxonomy of numerous samples from different sources but also for the standardization and differentiation of several similar samples. It was the first time to report a UPLC-ESI-MS-MS method for determination of five components in A. tataricus extract. Simultaneous quantification of bioactive components by UPLC-ESI-MS could be a well-acceptable strategy to control the quality of A. tataricus extract comprehensively.
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Affiliation(s)
- Haotian Yang
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
| | - He Shi
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
| | - Qiaoyue Zhang
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
| | - Yanyan Liu
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
| | - Changchen Wan
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
| | - Lantong Zhang
- Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, PR China
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Kang HR, Lee YA, Kim YH, Lee DG, Kim BJ, Kim KJ, Kim BG, Oh MG, Han CK, Lee S, Ryu BY. Petasites japonicus Stimulates the Proliferation of Mouse Spermatogonial Stem Cells. PLoS One 2015. [PMID: 26207817 PMCID: PMC4514868 DOI: 10.1371/journal.pone.0133077] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/15/2023] Open
Abstract
Oriental natural plants have been used as medical herbs for the treatment of various diseases for over 2,000 years. In this study, we evaluated the effect of several natural plants on the preservation of male fertility by assessing the ability of plant extracts to stimulate spermatogonial stem cell (SSC) proliferation by using a serum-free culture method. In vitro assays showed that Petasites japonicus extracts, especially the butanol fraction, have a significant effect on germ cells proliferation including SSCs. The activity of SSCs cultured in the presence of the Petasites japonicus butanol fraction was confirmed by normal colony formation and spermatogenesis following germ cell transplantation of the treated SSCs. Our findings could lead to the discovery of novel factors that activate SSCs and could be useful for the development of technologies for the prevention of male infertility.
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Affiliation(s)
- Hye-Ryun Kang
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Yong-An Lee
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Yong-Hee Kim
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Dong Gu Lee
- Department of Integrative Plant Science, Chung-Ang University, Anseong, Republic of Korea
| | - Bang-Jin Kim
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Ki-Jung Kim
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Byung-Gak Kim
- Department of Obstetrics, Gynecology & Reproductive Biology, Van Andel Institute, Michigan State University, Grand Rapids, Michigan, United States of America
| | - Myeong-Geun Oh
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
| | - Chan Kyu Han
- Korea Food Research Institute, Sungnam, Republic of Korea
| | - Sanghyun Lee
- Department of Integrative Plant Science, Chung-Ang University, Anseong, Republic of Korea
| | - Buom-Yong Ryu
- Department of Animal Science and Technology, Chung-Ang University, Anseong, Republic of Korea
- * E-mail:
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Antibacterial active compounds from Hypericum ascyron L. induce bacterial cell death through apoptosis pathway. Eur J Med Chem 2015; 96:436-44. [DOI: 10.1016/j.ejmech.2015.04.035] [Citation(s) in RCA: 19] [Impact Index Per Article: 1.9] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/05/2014] [Accepted: 04/15/2015] [Indexed: 11/19/2022]
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Shergis JL, Wu L, May BH, Zhang AL, Guo X, Lu C, Xue CC. Natural products for chronic cough: Text mining the East Asian historical literature for future therapeutics. Chron Respir Dis 2015; 12:204-11. [PMID: 25901012 DOI: 10.1177/1479972315583043] [Citation(s) in RCA: 16] [Impact Index Per Article: 1.6] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/26/2022] Open
Abstract
Chronic cough is a significant health burden. Patients experience variable benefits from over the counter and prescribed products, but there is an unmet need to provide more effective treatments. Natural products have been used to treat cough and some plant compounds such as pseudoephedrine from ephedra and codeine from opium poppy have been developed into drugs. Text mining historical literature may offer new insight for future therapeutic development. We identified natural products used in the East Asian historical literature to treat chronic cough. Evaluation of the historical literature revealed 331 natural products used to treat chronic cough. Products included plants, minerals and animal substances. These natural products were found in 75 different books published between AD 363 and 1911. Of the 331 products, the 10 most frequently and continually used products were examined, taking into consideration findings from contemporary experimental studies. The natural products identified are promising and offer new directions in therapeutic development for treating chronic cough.
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Affiliation(s)
- Johannah Linda Shergis
- Traditional and Complementary Medicine Research Program, School of Health Sciences and Health Innovations Research Institute (HIRi), RMIT University, Bundoora, Victoria, Australia
| | - Lei Wu
- Guangdong Provincial Hospital of Chinese Medicine, Guangdong Provincial Academy of Chinese Medical Sciences, and The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou, China
| | - Brian H May
- Traditional and Complementary Medicine Research Program, School of Health Sciences and Health Innovations Research Institute (HIRi), RMIT University, Bundoora, Victoria, Australia
| | - Anthony Lin Zhang
- Traditional and Complementary Medicine Research Program, School of Health Sciences and Health Innovations Research Institute (HIRi), RMIT University, Bundoora, Victoria, Australia
| | - Xinfeng Guo
- Guangdong Provincial Hospital of Chinese Medicine, Guangdong Provincial Academy of Chinese Medical Sciences, and The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou, China
| | - Chuanjian Lu
- Guangdong Provincial Hospital of Chinese Medicine, Guangdong Provincial Academy of Chinese Medical Sciences, and The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou, China
| | - Charlie Changli Xue
- Traditional and Complementary Medicine Research Program, School of Health Sciences and Health Innovations Research Institute (HIRi), RMIT University, Bundoora, Victoria, Australia Guangdong Provincial Hospital of Chinese Medicine, Guangdong Provincial Academy of Chinese Medical Sciences, and The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou, China
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4-hydroxyphenylacetic acid attenuated inflammation and edema via suppressing HIF-1α in seawater aspiration-induced lung injury in rats. Int J Mol Sci 2014; 15:12861-84. [PMID: 25050781 PMCID: PMC4139878 DOI: 10.3390/ijms150712861] [Citation(s) in RCA: 61] [Impact Index Per Article: 5.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/06/2014] [Revised: 06/24/2014] [Accepted: 07/02/2014] [Indexed: 02/03/2023] Open
Abstract
4-Hydroxyphenylacetic acid (4-HPA) is an active component of Chinese herb Aster tataricus which had been widely used in China for the treatment of pulmonary diseases. The aim of this study is to investigate the effect of 4-HPA on seawater aspiration-induced lung injury. Pulmonary inflammation and edema were assessed by enzyme-linked immunosorbent assay (ELISA), bronchoalveolar lavage fluid (BALF) white cell count, Evans blue dye analysis, wet to dry weight ratios, and histology study. Hypoxia-inducible factor-1α (HIF-1α) siRNA and permeability assay were used to study the effect of 4-HPA on the production of inflammatory cytokines and monolayer permeability in vitro. The results showed that 4-HPA reduced seawater instillation-induced mortality in rats. In lung tissues, 4-HPA attenuated hypoxia, inflammation, vascular leak, and edema, and decreased HIF-1α protein level. In primary rat alveolar epithelial cells (AEC), 4-HPA decreased hypertonicity- and hypoxia-induced HIF-1α protein levels through inhibiting the activations of protein translational regulators and via promoting HIF-1α protein degradation. In addition, 4-HPA lowered inflammatory cytokines levels through suppressing hypertonicity- and hypoxia-induced HIF-1α in NR8383 macrophages. Moreover, 4-HPA decreased monolayer permeability through suppressing hypertonicity and hypoxia-induced HIF-1α, which was mediated by inhibiting vascular endothelial growth factor (VEGF) in rat lung microvascular endothelial cell line (RLMVEC). In conclusion, 4-HPA attenuated inflammation and edema through suppressing hypertonic and hypoxic induction of HIF-1α in seawater aspiration-induced lung injury in rats.
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Sim JH, Lee HS, Lee S, Park DE, Oh K, Hwang KA, Kang HR, Ye SK, Kim HR. Anti-asthmatic activities of an ethanol extract of Aster yomena in an ovalbumin-induced murine asthma model. J Med Food 2014; 17:606-11. [PMID: 24738663 DOI: 10.1089/jmf.2013.2939] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Abstract] [Key Words] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/02/2023] Open
Abstract
Aster yomena is used in traditional remedies to treat cough, asthma and insect bites; however, its therapeutic mechanism is not completely understood. To elucidate the anti-asthmatic effect of A. yomena, we investigated the anti-asthmatic characteristics of an alcohol extract of A. yomena in an ovalbumin (OVA)-induced murine asthma model. In this study, we showed that A. yomena extract inhibited the overall pathophysiological features of asthma by suppressing Th2 responses and enzymes associated with the production of inflammatory mediators. This suppression resulted in decreased Th2 type cytokines and eosinophils in the bronchoalveolar lavage fluid and OVA-specific IgE in serum. Additionally, A. yomena extract significantly decreased airway hyperresponsiveness and abrogated the histopathological changes in the lungs, which reached normal levels in the OVA-challenged mice treated with A. yomena extract. These findings suggest that A. yomena could be a promising natural agent for treating bronchial asthma in humans.
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Affiliation(s)
- Ji Hyun Sim
- 1 Department of Anatomy & Biomedical Sciences, Seoul National University College of Medicine , Seoul, Korea
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Fong P, Tong HHY, Chao CM. In Silico Prediction of Tyrosinase and Adenylyl Cyclase Inhibitors from Natural Compounds. Nat Prod Commun 2014. [DOI: 10.1177/1934578x1400900214] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.2] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/16/2022] Open
Abstract
Although many herbal medicines are effective in the treatment of hyperpigmentation, the potency of different constituents remains unknown. In this work, more than 20,000 herbal ingredients from 453 herbs were docked into the crystal structures of adenylyl cyclase and a human homology tyrosinase model using Surflex-Dock. These two enzymes are responsible for melanin production and inhibition of them may attain a skin-whitening effect superior to currently available agents. The essential drug properties for topical formulation of the herbal ingredients, including skin permeability, sensitization, irritation, corrosive and carcinogenic properties were predicted by Dermwin, Skin Sensitization Alerts (SSA), Skin Irritation Corrosion Rules Estimation Tool (SICRET) and Benigni/Bossa rulebase module of Toxtree. Moreover, similarity ensemble and pharmacophore mapping approaches were used to forecast other potential targets for these herbal compounds by the software, SEArch and PharmMapper. Overall, this study predicted seven compounds to have advanced drug-like properties over the well-known effective tyrosinase inhibitors, arbutin and kojic acid. These seven compounds have the highest potential for further in vitro and in vivo investigation with the aim of developing safe and high-efficacy skin-whitening agents.
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Affiliation(s)
- Pedro Fong
- School of Health Sciences, Macao Polytechnic Institute, Macao, 999078, China
| | - Henry H. Y. Tong
- School of Health Sciences, Macao Polytechnic Institute, Macao, 999078, China
| | - Chi M. Chao
- School of Health Sciences, Macao Polytechnic Institute, Macao, 999078, China
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Delayed growth of glioma by a polysaccharide from Aster tataricus involve upregulation of Bax/Bcl-2 ratio, activation of caspase-3/8/9, and downregulation of the Akt. Tumour Biol 2013; 35:1819-25. [PMID: 24081677 DOI: 10.1007/s13277-013-1243-8] [Citation(s) in RCA: 18] [Impact Index Per Article: 1.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/09/2013] [Accepted: 09/20/2013] [Indexed: 12/11/2022] Open
Abstract
In this study, a homogeneous polysaccharide (ATP-II), with a molecular weight of 3.4 × 10(4) Da, was successfully purified from Aster tataricus by DEAE-Sepharose CL-6B ion exchange and Sepharose CL-6B gel filtration chromatography. Monosaccharide component analysis indicated that ATP-II was composed of glucose, galactose, mannose, rhamnose, and arabinose in molar ratios of 2.1:5.2:2.1:1.0:1.2. We evaluated the anticancer efficacy and associated mechanisms of ATP-II on glioma C6 cells in vitro and in vivo. The results showed that treatment of C6 cells with ATP-II inhibited cell proliferation and this biological response came from induction of DAN damage and consequent inducing apoptosis. Likewise, oral ATP-II administration resulted in consistent regression of glioma tumors and induced apoptosis of transplanted tumor tissues by increasing the ratio of Bax/Bcl-2 and activation of caspase-3, caspase-8, and caspase-9 cascade. Importantly, the efficient downregulation of Akt, which is successfully detected in tumor tissues, is a unique contribution to retard the tumor growth by ATP-II. These data suggest that ATP-II may be a potential candidate for glioma treatment.
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Phytochemical Compositions and Antioxidant and Anti-Inflammatory Activities of Crude Extracts from Ficus pandurata H. (Moraceae). EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE 2013; 2013:215036. [PMID: 24191163 PMCID: PMC3804050 DOI: 10.1155/2013/215036] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.4] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Received: 06/21/2013] [Revised: 08/26/2013] [Accepted: 08/26/2013] [Indexed: 11/17/2022]
Abstract
Background. Ficus pandurata H. (Moraceae) is widely used in traditional Chinese medicine as a healthy food condiment or a medicine for treatment of various diseases including inflammation. Objective. The purpose of the present study is to investigate the phytochemical compositions and antioxidant and anti-inflammatory activities of crude water (FPW) and ethanolic extracts (FPE) from Ficus pandurata H. Methods. Phytochemical compositions were identified by a high-performance liquid chromatography-electrospray ionization-mass spectrometry method (HPLC-ESI-MS). The antioxidant activities were evaluated by diphenylpicrylhydrazyl (DPPH) and hydroxyl radical assays, and the anti-inflammatory activities were evaluated by paw edema and levels of inflammatory mediator TNF-α and PGE2 in monosodium urate (MSU) crystal-induced rats. Results. Six compounds were identified by HPLC-MS method, and abundance of phenolics was found in FPE. The FPE showed concentration-dependent-significant scavenging of DPPH and hydroxyl radicals with IC50 values 118.4 and 192.9 μg/mL, respectively. The FPE treatment significantly inhibited the paw edema and the production of TNF-α and PGE2 in MSU crystal-induced rats. Conclusion. The FPE exerted stronger antioxidant and anti-inflammatory activities which may be attributed to its high phenolic content.
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Yon JM, Lin C, Oh KW, Baek HS, Lee BJ, Yun YW, Nam SY. Emodin prevents ethanol-induced developmental anomalies in cultured mouse fetus through multiple activities. ACTA ACUST UNITED AC 2013; 98:268-75. [PMID: 23696164 DOI: 10.1002/bdrb.21061] [Citation(s) in RCA: 8] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/12/2013] [Accepted: 04/04/2013] [Indexed: 11/11/2022]
Abstract
BACKGROUND Maternal alcohol ingestion on pregnant period causes fetal alcohol syndrome including psychological and behavioral problems, and developmental abnormality. In this study, we investigated the effect of emodin, an active anthraquinone component found in the roots and bark of the genus Rhamnus (Buckthorn), on ethanol-induced teratogenesis during embryonic organogenesis. METHODS We cultured mouse embryos on embryonic day 8.5 for 2 days with ethanol (5 μl/3 ml) and/or emodin (1×10(-5) and 1×10(-4) μg/ml) using a whole embryo culture system and then investigated the developmental evaluation, superoxide dismutase (SOD) activity, and expression patterns of cytoplasmic SOD (SOD1), mitochondrial SOD (SOD2), cytosolic glutathione peroxidase (cGPx), tumor necrosis factor-α (TNF-α), caspase 3, and hypoxia inducible factor 1α (HIF-1α). RESULTS Morphological parameters, including growth in yolk sac and fetal head, body length, and development of the central nervous system, circulation system, sensory organs, skeletal system, and limbs in embryos exposed to ethanol were significantly decreased compared to those of the normal control group, but co-treatment with emodin (1 × 10(-5) and 1 × 10(-4) μg/ml) significantly improved these parameters. Furthermore, the reduced levels of SOD activity, and SOD1, SOD2, cGPx, and HIF-1α and the increased gene levels of TNF-α and caspase-3 due to ethanol exposure were significantly restored by cotreatment with emodin. Birth Defects Res (Part B) 98:268-275, 2013. © 2013 Wiley Periodicals, Inc. CONCLUSIONS This study revealed that cotreatment with emodin significantly prevented teratogenesis induced by ethanol, not only by modulating hypoxia and antioxidant enzymes, but also by attenuating the enhanced levels of TNF-α and caspase 3 in cultured embryos. Therefore, emodin may be an effective preventive agent for ethanol-induced teratogenesis.
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Affiliation(s)
- Jung-Min Yon
- College of Veterinary Medicine and Research Institute of Veterinary Medicine, Chungbuk National University, Cheongju, Korea
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Ravipati AS, Zhang L, Koyyalamudi SR, Jeong SC, Reddy N, Bartlett J, Smith PT, Shanmugam K, Münch G, Wu MJ, Satyanarayanan M, Vysetti B. Antioxidant and anti-inflammatory activities of selected Chinese medicinal plants and their relation with antioxidant content. Altern Ther Health Med 2012; 12:173. [PMID: 23038995 PMCID: PMC3534023 DOI: 10.1186/1472-6882-12-173] [Citation(s) in RCA: 169] [Impact Index Per Article: 13.0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/11/2012] [Accepted: 09/20/2012] [Indexed: 11/10/2022]
Abstract
BACKGROUND The main aim of this study is to evaluate the antioxidant and anti-inflammatory properties of forty four traditional Chinese medicinal herbal extracts and to examine these activities in relation to their antioxidant content. METHODS The antioxidant activities were investigated using DPPH radical scavenging method and yeast model. The anti-inflammatory properties of the herbal extracts were evaluated by measuring their ability to inhibit the production of nitric oxide and TNF-α in RAW 264.7 macrophages activated by LPS and IFN- γ, respectively. The cytotoxic effects of the herbal extracts were determined by Alomar Blue assay by measuring cell viability. In order to understand the variation of antioxidant activities of herbal extracts with their antioxidant contents, the total phenolics, total flavonoids and trace metal (Mg, Mn, Cu, Zn, Se and Mo) quantities were estimated and a correlation analysis was carried out. RESULTS Results of this study show that significant levels of phenolics, flavonoids and trace metal contents were found in Ligustrum lucidum, Paeonia suffuticosa, Salvia miltiorrhiza, Sanguisorba officinalis, Spatholobus suberectus, Tussilago farfara and Uncaria rhyncophylla, which correlated well with their antioxidant and anti-inflammatory activities. Some of the plants displayed high antioxidant and anti-inflammatory activities but contained low levels of phenolics and flavonoids. Interestingly, these plants contained significant levels of trace metals (such as Zn, Mg and Se) which are likely to be responsible for their activities. CONCLUSIONS The results indicate that the phenolics, flavonoids and trace metals play an important role in the antioxidant activities of medicinal plants. Many of the plants studied here have been identified as potential sources of new antioxidant compounds.
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Synthesis and in vitro antitumor activity of novel scopoletin derivatives. Bioorg Med Chem Lett 2012; 22:5008-12. [DOI: 10.1016/j.bmcl.2012.06.014] [Citation(s) in RCA: 38] [Impact Index Per Article: 2.9] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/17/2012] [Revised: 06/04/2012] [Accepted: 06/07/2012] [Indexed: 11/18/2022]
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Suhas R, Channe Gowda D. Structure-Based Rationale Design and Synthesis of Aurantiamide Acetate Analogues - Towards a New Class of Potent Analgesic and Anti-inflammatory Agents. Chem Biol Drug Des 2012; 79:850-62. [DOI: 10.1111/j.1747-0285.2012.01331.x] [Citation(s) in RCA: 17] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/30/2022]
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Ra J, Chung JH, Lee H, Kim J. Reduction of interleukin-1β induced matrix metalloproteinase-3 release by extracts of six plants: inhibitory screening of 35 traditional medicinal plants. Immunopharmacol Immunotoxicol 2011; 33:461-5. [PMID: 21247370 DOI: 10.3109/08923973.2010.537663] [Citation(s) in RCA: 4] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/13/2022]
Abstract
Rheumatoid arthritis (RA) is a chronic inflammatory joint disease associated with matrix metalloproteinase (MMP)-3, leading to destruction of the cartilage. The objective of this study was to investigate and discuss the suitability of the 35 medicinal plants as therapeutic candidates to treat RA. Fibroblast-like synoviocytes (FLSs), derived from patients with RA, were adjusted to 2 × 10(6) cells/mL in a 24-well plate and pretreated with the distilled water extracts of the 35 plants (1, 10, and 100 µg/mL) for 1 h followed by interleukin-1β (IL-1β) (1 ng/mL) for 24 h. The concentration of MMP-3 was then determined using a Duoset ELISA Kit. The six plants (Artemisiae Capillaris Herba, AC; Bambusae Caulis In Taeniam, BC; Cassiae Semen, CS; Corni Fructus, CF; Leonuri Herba, LH; Schizonepetae Spica, SS) showed no toxicity, including MMP-3. The MMP-3 level was increased by 3.38-fold (212.23 μg/mL) in IL-1β-stimulated FLSs. The IL-1β-induced MMP-3 level was significantly and dose-dependently reduced by >50% by the six plants (P < 0.01: at 100 μg/ mL of CS and LH, P < 0.001: at 10 μg/mL of all plants, and at 100 μg/mL of AC, BC, CF, and SS). This is the first study on the MMP-3 inhibitory effect of the examined plants in FLSs isolated from RA patients. From our original research, the six candidate plants were identified.
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Affiliation(s)
- Jehyeon Ra
- Department of Oriental Physiology, College of Pharmacy, Kyung-Hee University, Seoul, Republic of Korea
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