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甲萘醌(维生素K)通过细胞膜通透机制增强药物的抗菌活性。

Menadione (vitamin K) enhances the antibiotic activity of drugs by cell membrane permeabilization mechanism.

作者信息

Andrade Jacqueline C, Morais Braga Maria Flaviana B, Guedes Gláucia Morgana M, Tintino Saulo R, Freitas Maria A, Quintans Lucindo J, Menezes Irwin R A, Coutinho Henrique D M

机构信息

Universidade Regional do Cariri, Crato (CE), Brazil.

Universidade Federal de Sergipe, Aracaju (SE), Brazil.

出版信息

Saudi J Biol Sci. 2017 Jan;24(1):59-64. doi: 10.1016/j.sjbs.2015.09.004. Epub 2015 Oct 21.

DOI:10.1016/j.sjbs.2015.09.004
PMID:28053572
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5198922/
Abstract

Menadione, vitamin K3, belongs to the class of lipid-soluble vitamins and lipophilic substances as menadione cause disturbances in the bacterial membrane, resulting in damage to the fundamental elements for the integrity of the membrane, thus allowing increased permeability. Accordingly, the aim of this study was to evaluate in vitro the antibiotic-modifying activity of menadione in multiresistant strains of , and , with a gradual increase in its subinhibitory concentration. In addition, menadione was compared with cholesterol and ergosterol for similarity in mechanism of drug modulatory action. Antibiotic-modifying activity and antibacterial effect were determined by the broth microdilution assay. Menadione, cholesterol and ergosterol showed modulatory activity at clinically relevant concentrations, characterizing them as modifiers of bacterial drug resistance, since they lowered the MIC of the antibiotics tested. This is the first report of the antibacterial activity of menadione and its potentiation of aminoglycosides against multiresistant bacteria.

摘要

甲萘醌,即维生素K3,属于脂溶性维生素和亲脂性物质类别,因为甲萘醌会干扰细菌膜,导致对膜完整性的基本要素造成损害,从而使通透性增加。因此,本研究的目的是在体外评估甲萘醌在多重耐药的金黄色葡萄球菌、大肠埃希菌和肺炎克雷伯菌菌株中的抗生素修饰活性,其亚抑菌浓度逐渐增加。此外,将甲萘醌与胆固醇和麦角固醇在药物调节作用机制方面的相似性进行了比较。通过肉汤微量稀释法测定抗生素修饰活性和抗菌效果。甲萘醌、胆固醇和麦角固醇在临床相关浓度下表现出调节活性,将它们表征为细菌耐药性的调节剂,因为它们降低了所测试抗生素的最低抑菌浓度。这是关于甲萘醌的抗菌活性及其对多重耐药菌增强氨基糖苷类抗生素作用的首次报道。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/235a/5198922/cf3a43bbef0d/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/235a/5198922/4b08a0df7c32/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/235a/5198922/cf3a43bbef0d/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/235a/5198922/4b08a0df7c32/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/235a/5198922/cf3a43bbef0d/gr2.jpg

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