喹诺酮类药物的抗菌和抗性机制  

Antibacterial and Resistant Mechanisms of Quinolones

作　　者：卞佳豪 奉竹 林颖峥 李思思[1] 李树清 王恒安[1] 陈志飞 BIAN Jia-hao;FENG Zhu;LIN Ying-zheng;LI Si-si;LI Shu-qing;WANG Heng-an;CHEN Zhi-fei(Shanghai Key Laboratory of Veterinary Biotechnology,School of Agriculture and Biology,Shanghai Jiao Tong University,Shanghai 200240,China;Shanghai Customs District,P.R.China,Shanghai 200002,China)

机构地区：[1]上海交通大学农业与生物学院,上海市兽医生物技术重点实验室,上海200240 [2]中华人民共和国上海海关,上海200002

出　　处：《中国兽药杂志》2020年第1期80-85,共6页Chinese Journal of Veterinary Drug

基　　金：上海市科技兴农重点攻关项目(G2018-02-08-00-10-F01548)。

摘　　要：喹诺酮类药物是广泛使用的一类抗菌药物,日趋严峻的细菌耐药性已严重威胁其临床应用。介绍喹诺酮类药物的发展过程,其靶向细菌DNA促旋酶(DNA gyrase)和拓扑异构酶Ⅳ(topoisomeraseⅣ)抑制DNA复制的抗菌机制,并进一步探讨了细菌对喹诺酮类药物的抗性机制,包括染色体编码药物靶酶DNA促旋酶和拓扑异构酶Ⅳ的点突变,染色体编码的调节蛋白突变所引发的药物输入蛋白下调或药物输出蛋白上调,以及质粒编码的可阻断药物与靶酶的相互作用、增加药物输出和改变药物代谢等抗性蛋白。研究喹诺酮的抗菌原理及细菌对喹诺酮的抗性机制,将有助于筛查和防控喹诺酮耐药菌。Quinolones are one of the most commonly used classes of antibacterials in the world,and the rise of quinolones resistance threatens the clinical utility of this important class drugs.This review describes the development of the quinolones,the mechanism of quinolones for inhibiting DNA replication by targeting bacterial gyrase and topoisomeraseⅣ,and further discusses the mechanisms of bacterial resistance against quinolones as followed,the mutations in chromosome-encoded DNA gyrase and topoisomeraseⅣ,the under-expression of influx proteins or the over-expression of e ux pumps due to the mutations in chromosome-encoded upstream regulators,several kinds of plasmid-encoded resistance proteins which can disrupt interactions between quinolones and its target enzymes,increase quinolone e ux,or alter drug metabolism,respectively.Thoroughly understanding of quinolone action and resistance mechanisms will significantly help to monitor,prevent and control drug-resistant bacteria in clinic.

关 键 词：喹诺酮 抗菌机制 细菌 抗性机制 

分 类 号：S859.796[农业科学—临床兽医学]