| 喹诺酮类药物的抗菌活性与细菌耐药性研究进展 |
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| 引用本文： | 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. |
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| 作者姓名： | 邵莉萍 张继瑜 |
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| 作者单位： | 中国农业科学院兰州畜牧与兽药研究所, 农业部兽药创制重点实验室, 兰州 730050 |
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| 基金项目： | 十二五国家科技支撑计划项目（2015BAD1101）；国家现代农业产业技术体系专项（CAR-38） |
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| 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。
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| 关 键 词： | 喹诺酮类药物 作用机制 耐药机理 |
| 收稿时间： | 2017-01-12 |
Research Advances on Antibacterial Activity and Bacterial Resistance of Quinolones |
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| SHAO Li-ping,ZHANG Ji-yu.Research Advances on Antibacterial Activity and Bacterial Resistance of Quinolones[J].China Animal Husbandry & Veterinary Medicine,2017,44(9):2773-2782. |
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| Authors: | SHAO Li-ping ZHANG Ji-yu |
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| Institution: | Key Laboratory of Veterinary Pharmaceutical Development, Ministry of Agriculture, Lanzhou Institute of Husbandry and Pharmaceutical Science, Chinese Academy of Agricultural Sciences, Lanzhou 730050, China |
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| 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. |
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| Keywords: | quinolones mechanism drug-resistant mechanism |
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