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桃金娘烯醇对……的抗菌和抗生物膜活性

Antibacterial and Antibiofilm Activity of Myrtenol against .

作者信息

Cordeiro Laísa, Figueiredo Pedro, Souza Helivaldo, Sousa Aleson, Andrade-Júnior Francisco, Barbosa-Filho José, Lima Edeltrudes

机构信息

Department of Pharmaceutical Science, Health Sciences Center, Federal University of Paraíba, João Pessoa 58033-455, Paraíba, Brazil.

Chemistry Department, Exact and Natural Sciences Center, Federal University of Paraíba, João Pessoa 58033-455, Brazil.

出版信息

Pharmaceuticals (Basel). 2020 Jun 25;13(6):133. doi: 10.3390/ph13060133.

DOI:10.3390/ph13060133
PMID:32630561
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7344394/
Abstract

The increase in resistance to conventional antibacterials and persistent infections related to biofilms, as well as the low availability of new antibacterial drugs, has made the development of new therapeutic alternatives necessary. Medicinal plants are one of the main sources of bioactive molecules and myrtenol is a natural product with several biological activities, although its antimicrobial activity is little explored. Based on this, the objective of this study was to evaluate the antibacterial activity of myrtenol against , determining the minimum inhibitory and bactericidal concentrations (MIC and MBC), investigating the possible molecular target through the analysis of molecular docking. It also aimed to evaluate the effect of its combination with antibacterial drugs and its activity against biofilms, in addition to performing an in silico analysis of its pharmacokinetic parameters. Myrtenol showed MIC and MBC of 128 µg/mL (bactericidal action) and probably acts by interfering with the synthesis of the bacterial cell wall. The effects of the association with antibacterials demonstrate favorable results. Myrtenol has remarkable antibiofilm activity and in silico results indicate a good pharmacokinetic profile, which make myrtenol a potential drug candidate for the treatment of infections caused by .

摘要

对传统抗菌药物的耐药性增加以及与生物膜相关的持续性感染,再加上新型抗菌药物的可获得性低,使得开发新的治疗选择成为必要。药用植物是生物活性分子的主要来源之一,桃金娘烯醇是一种具有多种生物活性的天然产物,尽管其抗菌活性鲜有研究。基于此,本研究的目的是评估桃金娘烯醇对[具体细菌名称未给出]的抗菌活性,确定最低抑菌浓度和杀菌浓度(MIC和MBC),通过分子对接分析研究可能的分子靶点。此外,除了对其药代动力学参数进行计算机模拟分析外,还旨在评估其与抗菌药物联合使用的效果及其对生物膜的活性。桃金娘烯醇的MIC和MBC为128 µg/mL(杀菌作用),可能通过干扰细菌细胞壁的合成起作用。与抗菌药物联合使用的效果显示出良好的结果。桃金娘烯醇具有显著的抗生物膜活性,计算机模拟结果表明其具有良好的药代动力学特征,这使得桃金娘烯醇成为治疗由[具体细菌名称未给出]引起的感染的潜在候选药物。

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