细菌外排泵与抗生素耐药的相关性

摘要/Abstract

摘要： 抗生素耐药与临床用药紧密相关,一直以来都受到广泛关注。除了药物失活、靶点改变这些已经熟知的耐药机制以外,细菌外排泵的作用也是抗生素耐药的重要原因。外排泵在细菌中普遍存在并且底物十分广泛,其表达对多种细菌的先天耐药和后天耐药都有贡献。对于金黄色葡萄球菌、大肠杆菌、绿脓杆菌等细菌,外排泵导致的耐药是其耐药的主要原因,因此在临床用药过程中,外排泵产生的耐药成了不可忽略的因素。这也给新药研发提供了新的思路,已经有研究以外排泵为靶点开发新药,而开发能够规避外排泵作用的新型抗生素也是克服外排泵耐药的一个途径。本文从分类,结构,调控以及抑制剂等方面对近年来细菌外排转运体方面的研究进行综述,为进一步的探索提供参考。

关键词: 外排泵, 细菌, 抗生素, 耐药

Abstract: Drug resistance in bacteria has attracted much attention in clinical antibacterial therapy for years. In addition to the well known mechanisms, such as inactivation of drugs and alteration of targets, drug extruding pumps also play a major role in resistance to antibacterials. Efflux pumps are widespread in bacteria and have broad variety of substrates. Their presence contributes both intrinsic and acquired bacterial resistance. Efflux-mediated drug-resistance has been recognized as the major mechanism of resistance to antibacterial agents in Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The impact of antibiotic efflux pumps on therapy must be taken fully into account for the selection of antimicrobials. The design of specific, potent inhibitors appears to be an important goal for the improved control of infectious diseases in the near future. An alternative approach is to develop antibacterials that would bypass the action of efflux pumps. This paper will review recent progress on the role of bacterial efflux transporters in antibiotic resistance from the aspects of classification, structure, regulation and the inhibitors, which will provide references for the further investigation.

Key words: Efflux pump, Bacteria, Antibiotics, Drug resistance

中图分类号:

R978.1

孙渊, 査伟斌, 周芳, 吴晓兰, 张经纬, 王广基. 细菌外排泵与抗生素耐药的相关性[J]. 中国临床药理学与治疗学, 2012, 17(5): 593-600.

SUN Yuan, ZHA Wei-bin, ZHOU Fang, WU Xiao-lan, ZHANG Jing-wei, WANG Guang-ji. Relation between bacterial efflux pump and antibiotic resistance[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(5): 593-600.

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