植物甾醇作为新德里金属-β-内酰胺酶(NDM-1)的抑制剂:一项硅学研究。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2024-11-08 DOI:10.1007/s11030-024-11020-6
Mashihur Rahman, Mohd Ahsan, Md Tabish Rehman, Mohamed F AlAjmi, Md Khurshid Alam Khan
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引用次数: 0

摘要

新德里金属-β-内酰胺酶-1(NDM-1)在全球的出现给抗生素治疗带来了严峻的挑战,因为它对多种β-内酰胺类抗生素产生耐药性。本研究旨在找出 NDM-1 的潜在抑制剂,从而恢复现有抗生素的疗效。采用分子对接和分子动力学(MD)模拟相结合的综合计算方法,对植物甾醇库进行了筛选,以确定有希望抑制 NDM-1 活性的候选化合物。以一线碳青霉烯类抗生素美罗培南的结合能为参考,阿文甾醇、黄铜甾醇和豆甾醇成为有待进一步研究的候选植物甾醇。随后进行的 MD 模拟证实,NDM-1 与阿文甾醇和豆甾醇的复合物在模拟期间保持稳定,这表明它们具有潜在的药效。这些研究结果表明,阿文甾醇和豆甾醇可以有效抑制 NDM-1 的活性,需要通过体外和体内研究进行验证。此外,这些植物甾醇有望成为开发新型 NDM-1 抑制剂的先导化合物。它们的天然来源和对 NDM-1 的潜在抑制活性为开发替代抗菌疗法以对抗耐多药感染提供了令人信服的途径。这项研究强调了计算方法在药物发现中的实用性,并突出了植物甾醇作为解决抗生素耐药性问题的宝贵候选化合物的潜力。
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Phytosterols as inhibitors of New Delhi metallo-β-lactamase (NDM-1): an in silico study.

The global emergence of New Delhi metallo-β-lactamase-1 (NDM-1) poses a formidable challenge to antibiotic therapy, as it confers resistance to a wide range of β-lactam antibiotics. This study aims to identify potential inhibitors of NDM-1 and thereby restore the effectiveness of the current antibiotics. Employing a comprehensive computational approach integrating molecular docking and molecular dynamics (MD) simulations, a library of phytosterols was screened to identify promising candidates for inhibiting NDM-1 activity. Using the binding energy of meropenem, a frontline carbapenem antibiotic, as a reference, avenasterol, brassicasterol, and stigmasterol emerged as top phytosterol candidates for further investigation. Subsequent MD simulations confirmed the stability of NDM-1 complexes with avenasterol and stigmasterol over the simulation period, indicating their potential efficacy. These findings suggest that avenasterol and stigmasterol may effectively inhibit NDM-1 activity, warranting validation through in vitro and in vivo studies. Furthermore, these phytosterols hold promise as lead compounds for developing novel NDM-1 inhibitors. Their natural origin and potential inhibitory activity against NDM-1 offer compelling avenues for developing alternative antibacterial therapies to combat multidrug-resistant infections. This study underscores the utility of computational methods in drug discovery and highlights the potential of phytosterols as valuable candidates for addressing antibiotic resistance.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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