喹诺酮类药物的抗菌活性与细菌耐药性研究进展

doi:10.16431/j.cnki.1671-7236.2017.09.033

摘要/Abstract

摘要：

喹诺酮类药物（quinolones，QLs）是一类化学合成的抗菌药物，曾在世界范围内广泛应用于临床细菌病的治疗。其作用靶点为细菌DNA螺旋酶和拓扑异构酶，形成药-酶-DNA三元复合体，阻止蛋白质合成，从而达到抑菌效果。目前，通过对许多三元复合体的晶体结构解析，以及非催化镁离子模型的建立，进一步合理地解释了喹诺酮类药物活性受到影响的现象。临床常见致病菌对喹诺酮类药物产生耐药现象的机理研究较多，主要是基因突变、膜对药物的通透性改变及质粒介导的喹诺酮耐药性（PMQR）3个方面。文章主要对喹诺酮类药物的作用机制和细菌耐药机理进行综述，以期为后期喹诺酮类药物结构优化提供更多的信息支持。

关键词: 喹诺酮类药物; 作用机制; 耐药机理

Abstract:

Quinolones (QLs) are synthetic antimicrobials and widely used to treat clinical bacterial disease in the world. Quinolones trap DNA gyrase or topoisomerase Ⅳ to form reversible drug-enzyme-DNA complexes and prevent protein synthesis,resulting in bacteriostasis. Recently, the analysis of crystal structures of cleaved complexes and building of the model of noncatalytic magnesium ion present a reasonable explanation for the phenomenon of the effect of quinolones antibacterial activity. There are many researches for the mechanisms of resistance of quinolones, gene mutation, altered drug permeation and plasmid-mediated quinolone resistance are three main aspects. Here, the molecular basis for the antibacterial action and mechanisms of resistance of quinolones were fully discussed and updated, so as to provide a large number of information for optimization of quinolone antimicrobials based on structural transformation.

Key words: quinolones; mechanism; drug-resistant mechanism

中图分类号:

邵莉萍, 张继瑜. 喹诺酮类药物的抗菌活性与细菌耐药性研究进展[J]. 《中国畜牧兽医》, 2017, 44(9): 2773-2782.

SHAO Li-ping, ZHANG Ji-yu. Research Advances on Antibacterial Activity and Bacterial Resistance of Quinolones[J]. , 2017, 44(9): 2773-2782.

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