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Mahajan V, Samra T, Puri G. Anaesthetic depth control using closed loop anaesthesia delivery system vs. target controlled infusion in patients with moderate to severe left ventricular systolic dysfunction. J Clin Anesth 2017; 42:106-113. [DOI: 10.1016/j.jclinane.2017.07.014] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/18/2017] [Revised: 07/17/2017] [Accepted: 07/29/2017] [Indexed: 12/22/2022]
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Automated anesthesia delivery systems in cardiac surgical patients with left ventricular dysfunction: All systems go? J Clin Anesth 2017; 42:103-105. [PMID: 28844674 DOI: 10.1016/j.jclinane.2017.08.017] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/27/2017] [Revised: 08/05/2017] [Accepted: 08/11/2017] [Indexed: 11/20/2022]
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Perioperative risk factors and cumulative duration of “triple-low” state associated with worse 30-day mortality of cardiac valvular surgery. J Clin Monit Comput 2016; 31:387-395. [DOI: 10.1007/s10877-016-9856-2] [Citation(s) in RCA: 7] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/24/2015] [Accepted: 03/01/2016] [Indexed: 10/22/2022]
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Ascenzi P, Leboffe L, di Masi A, Trezza V, Fanali G, Gioia M, Coletta M, Fasano M. Ligand binding to the FA3-FA4 cleft inhibits the esterase-like activity of human serum albumin. PLoS One 2015; 10:e0120603. [PMID: 25790235 PMCID: PMC4366387 DOI: 10.1371/journal.pone.0120603] [Citation(s) in RCA: 7] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/06/2014] [Accepted: 01/24/2015] [Indexed: 12/19/2022] Open
Abstract
The hydrolysis of 4-nitrophenyl esters of hexanoate (NphOHe) and decanoate (NphODe) by human serum albumin (HSA) at Tyr411, located at the FA3-FA4 site, has been investigated between pH 5.8 and 9.5, at 22.0°C. Values of Ks, k+2, and k+2/Ks obtained at [HSA] ≥ 5×[NphOXx] and [NphOXx] ≥ 5×[HSA] (Xx is NphOHe or NphODe) match very well each other; moreover, the deacylation step turns out to be the rate limiting step in catalysis (i.e., k+3 << k+2). The pH dependence of the kinetic parameters for the hydrolysis of NphOHe and NphODe can be described by the acidic pKa-shift of a single amino acid residue, which varies from 8.9 in the free HSA to 7.6 and 7.0 in the HSA:NphOHe and HSA:NphODe complex, respectively; the pK>a-shift appears to be correlated to the length of the fatty acid tail of the substrate. The inhibition of the HSA-Tyr411-catalyzed hydrolysis of NphOHe, NphODe, and 4-nitrophenyl myristate (NphOMy) by five inhibitors (i.e., diazepam, diflunisal, ibuprofen, 3-indoxyl-sulfate, and propofol) has been investigated at pH 7.5 and 22.0°C, resulting competitive. The affinity of diazepam, diflunisal, ibuprofen, 3-indoxyl-sulfate, and propofol for HSA reflects the selectivity of the FA3-FA4 cleft. Under conditions where Tyr411 is not acylated, the molar fraction of diazepam, diflunisal, ibuprofen, and 3-indoxyl-sulfate bound to HSA is higher than 0.9 whereas the molar fraction of propofol bound to HSA is ca. 0.5.
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Affiliation(s)
- Paolo Ascenzi
- Interdepartmental Laboratory of Electron Microscopy, Roma Tre University, Via della Vasca Navale 79, I-00146 Roma, Italy
| | - Loris Leboffe
- Department of Sciences, Roma Tre University, Viale Guglielmo Marconi 446, I-00146 Roma, Italy
| | - Alessandra di Masi
- Department of Sciences, Roma Tre University, Viale Guglielmo Marconi 446, I-00146 Roma, Italy
| | - Viviana Trezza
- Department of Sciences, Roma Tre University, Viale Guglielmo Marconi 446, I-00146 Roma, Italy
| | - Gabriella Fanali
- Biomedical Research Division, Department of Theoretical and Applied Sciences, University of Insubria, Via Alberto da Giussano 12, I-21052 Busto Arsizio (VA), Italy
| | - Magda Gioia
- Department of Clinical Sciences and Translational Medicine, University of Roma “Tor Vergata”, Via Montpellier 1, I-00133 Roma, Italy
- Interuniversity Consortium for the Research on the Chemistry of Metals in Biological Systems, Via Celso Ulpiani 27, I-70126 Bari, Italy
| | - Massimo Coletta
- Department of Clinical Sciences and Translational Medicine, University of Roma “Tor Vergata”, Via Montpellier 1, I-00133 Roma, Italy
- Interuniversity Consortium for the Research on the Chemistry of Metals in Biological Systems, Via Celso Ulpiani 27, I-70126 Bari, Italy
| | - Mauro Fasano
- Biomedical Research Division, Department of Theoretical and Applied Sciences, University of Insubria, Via Alberto da Giussano 12, I-21052 Busto Arsizio (VA), Italy
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Chen FC, Liao YC, Huang JM, Lin CH, Chen YY, Dou HY, Hsiung CA. Pros and cons of the tuberculosis drugome approach--an empirical analysis. PLoS One 2014; 9:e100829. [PMID: 24971632 PMCID: PMC4074101 DOI: 10.1371/journal.pone.0100829] [Citation(s) in RCA: 14] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/02/2014] [Accepted: 05/27/2014] [Indexed: 01/20/2023] Open
Abstract
Drug-resistant Mycobacterium tuberculosis (MTB), the causative pathogen of tuberculosis (TB), has become a serious threat to global public health. Yet the development of novel drugs against MTB has been lagging. One potentially powerful approach to drug development is computation-aided repositioning of current drugs. However, the effectiveness of this approach has rarely been examined. Here we select the "TB drugome" approach--a protein structure-based method for drug repositioning for tuberculosis treatment--to (1) experimentally validate the efficacy of the identified drug candidates for inhibiting MTB growth, and (2) computationally examine how consistently drug candidates are prioritized, considering changes in input data. Twenty three drugs in the TB drugome were tested. Of them, only two drugs (tamoxifen and 4-hydroxytamoxifen) effectively suppressed MTB growth at relatively high concentrations. Both drugs significantly enhanced the inhibitory effects of three first-line anti-TB drugs (rifampin, isoniazid, and ethambutol). However, tamoxifen is not a top-listed drug in the TB drugome, and 4-hydroxytamoxifen is not approved for use in humans. Computational re-examination of the TB drugome indicated that the rankings were subject to technical and data-related biases. Thus, although our results support the effectiveness of the TB drugome approach for identifying drugs that can potentially be repositioned for stand-alone applications or for combination treatments for TB, the approach requires further refinements via incorporation of additional biological information. Our findings can also be extended to other structure-based drug repositioning methods.
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Affiliation(s)
- Feng-Chi Chen
- Division of Biostatistics and Bioinformatics, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
- Department of Life Sciences, National Chiao-Tung University, Hsinchu, Taiwan
- Department of Dentistry, China Medical University, Taichung, Taiwan
| | - Yu-Chieh Liao
- Division of Biostatistics and Bioinformatics, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
| | - Jie-Mao Huang
- Division of Biostatistics and Bioinformatics, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
| | - Chieh-Hua Lin
- Division of Biostatistics and Bioinformatics, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
- Institute of Bioinformatics and Structural Biology, National Tsing Hua University, Hsinchu, Taiwan
| | - Yih-Yuan Chen
- National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
| | - Horng-Yunn Dou
- National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
| | - Chao Agnes Hsiung
- Division of Biostatistics and Bioinformatics, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
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Ma G, Chen J, Meng X, Deng L, Gao Y, Meng J. High-Dose Propofol Reduces S-100β Protein and Neuron-Specific Enolase Levels in Patients Undergoing Cardiac Surgery. J Cardiothorac Vasc Anesth 2013; 27:510-5. [DOI: 10.1053/j.jvca.2012.10.013] [Citation(s) in RCA: 6] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 06/06/2012] [Indexed: 11/11/2022]
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Massullo D, Di Benedetto P, Pinto G. Intraoperative strategy in patients with extended involvement of mediastinal structures. Thorac Surg Clin 2009; 19:113-120, vii-viii. [PMID: 19288826 DOI: 10.1016/j.thorsurg.2008.09.009] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.2] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/17/2022]
Abstract
The mediastinum is a virtual space containing several vital organs and structures. Biopsy and resection of lesions located within this region often require several considerations that bear on intraoperative strategy. To optimize outcome, clinicians must be able to predict which patients are at highest risk of anesthetic complications. Superior vena cava involvement, extensive compression of the airway, and pericardial effusion have a clear impact on the decision-making of the anesthetist and surgeon, who should plan together when forming the surgical strategy.
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Affiliation(s)
- Domenico Massullo
- Department of Anesthesiology, University of Rome La Sapienza, Ospedale S. Andrea, Via di Grottarossa 1035, 00189 Rome, Italy.
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Jeon JP, Chang HW, Kim ES. Anesthetic Management of Acute Massive Pulmonary Embolism after Intracerebral Hemorrhage - A case report -. Korean J Anesthesiol 2008. [DOI: 10.4097/kjae.2008.54.2.204] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/10/2022] Open
Affiliation(s)
- Jun Pyo Jeon
- Department of Anesthesiology and Pain Medicine, The Catholic University of Korea College of Medicine, Seoul, Korea
| | - Hae Wone Chang
- Department of Anesthesiology and Pain Medicine, The Catholic University of Korea College of Medicine, Seoul, Korea
| | - Eun Sung Kim
- Department of Anesthesiology and Pain Medicine, The Catholic University of Korea College of Medicine, Seoul, Korea
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Yang LQ, Yu WF, Cao YF, Gong B, Chang Q, Yang GS. Potential inhibition of cytochrome P450 3A4 by propofol in human primary hepatocytes. World J Gastroenterol 2003; 9:1959-62. [PMID: 12970884 PMCID: PMC4656652 DOI: 10.3748/wjg.v9.i9.1959] [Citation(s) in RCA: 17] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Indexed: 02/06/2023] Open
Abstract
AIM: Hepatic cytochrome P450 isoenzymes constitute a superfamily of hemoproteins that play a major role in the metabolism of endogenous compounds and in the detoxification of xenobiotic molecules. P450 3A4 is one of the most important forms in human being, and mediates the metabolism of around 70% of therapeutic drugs and endogenous compounds. Propofol, a widely used intravenous anesthetic drug, is known to inhibit cytochrome P450 activities in isolated rat hepatocytes. The goal of this study was to evaluate the potential efficacy of propofol on P450 3A4 in a dose-dependent manner to understand its drug-drug interaction.
METHODS: Hepatocytes were isolated from liver specimens from hepatic angioma patients undergone hepatic surgery. Primary incubated hepatocytes were treated with 0, 0.01, 0.05, 0.1, 0.5, and 1.0 mM propofol for 24 hours. P450 3A4 activity was measured with Nash’s colorimetry. The protein expression was assessed by Western blot analysis.
RESULTS: A dose-dependent inhibitory effect of propofol was observed in cytochrome P450 3A4 activity. A minimal dosage of propofol (0.01 mM) induced a significant inhibition of P450 3A4 activity, although its regular dosages (0.01-0.1 mM) showed no inhibitory effect on the cellular protein expression of P450 3A4.
CONCLUSION: Propofol may be a potential CYP3A4 inhibitor as this anesthetic can inhibit isoenzyme activity significantly and reduce the metabolic rate of CYP3A4 substrates. This inhibition occurs at post-expression level, and concentration of propofol used clinically does not affect CYP3A4 protein expression. propofol may thus induce drug interaction of cytochrome P450 3A4 activity at the dosage used clinically.
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Affiliation(s)
- Li-Qun Yang
- Department of Anesthesiology, Eastern Hepatobiliary Surgery Hospital, the Second Military Medical University, Shanghai 200438, China
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Bibliography Current World Literature. Curr Opin Anaesthesiol 2003. [DOI: 10.1097/01.aco.0000084472.59960.ce] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/25/2022]
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