新型糖肽类万古霉素合成抑制剂 Van-M-02 在耐万古霉素细菌中的作用机制。
Mode of action of Van-M-02, a novel glycopeptide inhibitor of peptidoglycan synthesis, in vancomycin-resistant bacteria.
机构信息
Discovery Research Laboratories, Shionogi & Co., Ltd., 3-1-1 Futaba-cho, Toyonaka, Osaka 561-0825, Japan.
出版信息
Antimicrob Agents Chemother. 2010 Feb;54(2):960-2. doi: 10.1128/AAC.00927-09. Epub 2009 Nov 23.
Abstract
Van-M-02, a novel glycopeptide, was revealed to exert potent activities against Gram-positive bacteria, including vancomycin-resistant enterococci (VRE) and vancomycin-resistant Staphylococcus aureus (VRSA). A crude assay system was then used to study the mode of action of Van-M-02 as a peptidoglycan synthesis model of both vancomycin-susceptible and -resistant strains. The results suggested that Van-M-02 inhibits the synthesis of lipid intermediates irrespective of their termini. This inhibitory activity may contribute to the anti-VRE and anti-VRSA activities observed.
摘要
Van-M-02 是一种新型糖肽，被证实对革兰氏阳性菌具有强大的活性，包括耐万古霉素肠球菌（VRE）和耐万古霉素金黄色葡萄球菌（VRSA）。然后使用粗筛检测系统研究了 Van-M-02 的作用模式，作为万古霉素敏感和耐药菌株的肽聚糖合成模型。结果表明，Van-M-02 抑制脂质中间体的合成，而与它们的末端无关。这种抑制活性可能有助于观察到的抗 VRE 和抗 VRSA 活性。
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