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[细菌外排泵——它们在抗生素耐药性中的作用及潜在抑制剂]

[Bacterial efflux pumps - their role in antibiotic resistance and potential inhibitors].

作者信息

Hricová Kristýna, Kolář Milan

机构信息

Department of Microbiology, Faculty of Medicine and Dentistry, Palacký University in Olomouc, Czech Republic, e-mail:

出版信息

Klin Mikrobiol Infekc Lek. 2014 Dec;20(4):116-20.

Abstract

Efflux pumps capable of actively draining antibiotic agents from bacterial cells may be considered one of potential mechanisms of the development of antimicrobial resistance. The most important group of efflux pumps capable of removing several types of antibiotics include RND (resistance - nodulation - division) pumps. These are three proteins that cross the bacterial cell wall, allowing direct expulsion of the agent out from the bacterial cell. The most investigated efflux pumps are the AcrAB-TolC system in Escherichia coli and the MexAB-OprM system in Pseudomonas aeruginosa. Moreover, efflux pumps are able to export other than antibacterial agents such as disinfectants, thus decreasing their effectiveness. One potential approach to inactivation of an efflux pump is to use the so-called efflux pump inhibitors (EPIs). Potential inhibitors tested in vitro involve, for example, phenylalanyl-arginyl-b-naphthylamide (PAbN), carbonyl cyanide m-chlorophenylhydrazone (CCCP) or agents of the phenothiazine class.

摘要

能够主动将抗生素从细菌细胞中排出的外排泵可被视为抗菌药物耐药性产生的潜在机制之一。能够排出多种类型抗生素的最重要的一类外排泵包括RND(耐药性-结瘤-分裂)泵。这是三种穿过细菌细胞壁的蛋白质,可使药物直接从细菌细胞中排出。研究最多的外排泵是大肠杆菌中的AcrAB-TolC系统和铜绿假单胞菌中的MexAB-OprM系统。此外,外排泵还能够排出除抗菌剂之外的其他物质,如消毒剂,从而降低其有效性。使外排泵失活的一种潜在方法是使用所谓的外排泵抑制剂(EPI)。体外测试的潜在抑制剂例如包括苯丙氨酰-精氨酰-β-萘酰胺(PAbN)、羰基氰化物间氯苯腙(CCCP)或吩噻嗪类药物。

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