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松油烯-4-醇作为一种针对 的抗菌和抗生物膜剂。

Terpinen-4-ol as an Antibacterial and Antibiofilm Agent against .

机构信息

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

Chemistry Department, Federal University of Paraíba, João Pessoa 58033-455, Brazil.

出版信息

Int J Mol Sci. 2020 Jun 25;21(12):4531. doi: 10.3390/ijms21124531.

DOI:10.3390/ijms21124531
PMID:32630600
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7350221/
Abstract

is able to rapidly develop mechanisms of resistance to various drugs and to form strong biofilms, which makes it necessary to develop new antibacterial drugs. The essential oil of is used as an antibacterial, a property believed to be mainly due to the presence of terpinen-4-ol. Based on this, the objective of this study was to evaluate the antibacterial and antibiofilm potential of terpinen-4-ol against . The Minimal Inhibitory and Minimal Bactericidal Concentrations (MIC and MBC) of terpinen-4-ol were determined, and the effect of its combination with antibacterial drugs as well as its activity against biofilms were evaluated. In addition, an in silico analysis of its pharmacokinetic parameters and a molecular docking analysis were performed. Terpinen-4-ol presented a MIC of 0.25% () and an MBC of 0.5% () (bactericidal action); its association with antibacterials was also effective. Terpinen-4-ol has good antibiofilm activity, and the in silico results indicated adequate absorption and distribution of the molecule in vivo. Molecular docking indicated that penicillin-binding protein 2a is a possible target of terpinen-4-ol in . This work highlights the good potential of terpinen-4-ol as an antibacterial product and provides support for future pharmacological studies of this molecule, aiming at its therapeutic application.

摘要

能够迅速产生对各种药物的耐药机制,并形成强大的生物膜,这使得有必要开发新的抗菌药物。 被用作抗菌剂,其特性主要归因于存在松油烯-4-醇。基于此,本研究的目的是评估松油烯-4-醇对 的抗菌和抗生物膜潜力。测定了松油烯-4-醇的最小抑菌浓度(MIC)和最小杀菌浓度(MBC),并评估了其与抗菌药物联合使用的效果及其对 生物膜的活性。此外,还进行了其药代动力学参数的计算分析和分子对接分析。松油烯-4-醇的 MIC 为 0.25%()和 MBC 为 0.5%()(杀菌作用);其与抗菌药物的联合使用也具有效果。松油烯-4-醇具有良好的抗生物膜活性,计算分析结果表明该分子在体内具有足够的吸收和分布。分子对接表明青霉素结合蛋白 2a 可能是松油烯-4-醇在 中的靶标。这项工作突出了松油烯-4-醇作为抗菌产品的良好潜力,并为该分子的未来药理学研究提供了支持,旨在将其应用于治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/c2ef04fe9f0d/ijms-21-04531-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/a920005f75f3/ijms-21-04531-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/f34c02663015/ijms-21-04531-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/a77eb46f84b0/ijms-21-04531-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/c2ef04fe9f0d/ijms-21-04531-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/a920005f75f3/ijms-21-04531-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/f34c02663015/ijms-21-04531-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/a77eb46f84b0/ijms-21-04531-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7a8/7350221/c2ef04fe9f0d/ijms-21-04531-g004.jpg

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