外排泵抑制剂研究进展

细菌耐药性一直是全球关注的热点,细菌外排泵造成了抗生素耐药的严重问题,为此,近年来研究外排泵抑制剂广受关注。外排泵抑制剂可以抑制耐药细菌对药物的外排,从而恢复其对抗生素的敏感性。本文简要介绍了几类外排泵的结构,对其作用机制、化学合成、微生物代谢来源和天然产物来源的各类第三代外排泵抑制剂、筛选方法等方面进行了综述,及对三维结构的解析将有助于发现活性更好的新型外排泵抑制剂。

Research Progress on Inhibitor of Efflux Pump

Bacterial drug resistance had always been the hot spot of the global attention.Efflux pump(EP)of microbial had caused the serious problem of antibiotic resistance and for this purpose,widely attention had been paid to study of efflux pump inhibitors(EPIs)in recent years.EPIs could inhibited the efflux of drugs from bacteria and restored the susceptibility of drug-resistant bacteria to antibiotics.The structural features of several types of efflux pump was briefly introduced,and the mechanism of action,the current progress of chemical synthesis,the sources of microorganisms metabolic and the sources of natural products of the third generation efflux pump inhibitors,screening method,etc.were summarized in this review.Meanwhile,the analysis of three-dimensional structure will help to find out novel EPIs with higher inhibitory activity.