苯乙酸丁酯增强二线药物对临床分离结核分枝杆菌的效力。
Phenylethyl butyrate enhances the potency of second-line drugs against clinical isolates of Mycobacterium tuberculosis.
机构信息
Institute of Medical Microbiology, University of Zurich, Zurich, Switzerland.
出版信息
Antimicrob Agents Chemother. 2012 Feb;56(2):1142-5. doi: 10.1128/AAC.05649-11. Epub 2011 Nov 21.
Abstract
Ethionamide (ETH) is a second-line drug for the treatment of tuberculosis. As a prodrug, ETH has to be activated by EthA. ethA is controlled by its repressor EthR. 2-Phenylethyl-butyrate (2-PEB) inhibits EthR binding, enhances expression of EthA, and thereby enhances the growth-inhibitory effects of ethionamide, isoxyl, and thiacetazone in Mycobacterium tuberculosis strains with resistance to ETH due to inhA promoter mutations but not ethA mutations.
摘要
乙硫异烟胺（ETH）是治疗结核病的二线药物。作为前体药物，ETH 必须被 EthA 激活。ethA 受其阻遏物 EthR 控制。2-苯乙基丁酸（2-PEB）抑制 EthR 结合，增强 EthA 的表达，从而增强乙硫异烟胺、异烟肼和氨硫脲在结核分枝杆菌菌株中的生长抑制作用，这些菌株对 ETH 的耐药性是由于 inhA 启动子突变而不是 ethA 突变。
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