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作 者:孙影[1] 顾觉奋[1] SUN Ying;GU Juefen(School of Life Science and Technology China Pharmaceutical University,Nanjing 210009,China)
机构地区:[1]中国药科大学生命科学与技术学院,江苏南京210009
出 处:《药学进展》2018年第6期411-419,共9页Progress in Pharmaceutical Sciences
摘 要:细菌外排泵造成了抗生素耐药的严重问题,为此,近年来外排泵抑制剂研究广受关注。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。简要介绍几类外排泵的结构,综述化学合成和天然产物来源的各类外排泵抑制剂的研究进展,以期为研究者们提供新的思路,设计或筛选出活性更好的新型外排泵抑制剂。同时还提出了外排泵抑制剂的研究方法和药敏实验的规范化问题,希望人们更全面而准确地筛选、评价外排泵抑制剂及其临床应用价值。Bacterial efflux pump(EP) has caused serious antibiotic resistance, and consequently much attention has been paid to efflux pump inhibitors(EPIs) in recent years. EPIs could inhibit the efflux of drugs from bacteria and restore the susceptibility of drug-resistant bacteria to antibiotics. In this review, the structural features of several types of EPs were briefly introduced, and the current progress of synthetic and natural EPIs was summarized, hoping to provide researchers with new ideas to design or screen out new EPIs with higher inhibitory activity. Meanwhile, for more accurate and comprehensive screening and evaluation of EPIs and their clinical effects, research methods for EPIs and standardization of their antimicrobial susceptibility testing(AST) were also proposed
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