关键词: Enterobacteriaceae DNA gyrase efflux pumps plasmid-mediated quinolone resistance porins quinolone resistance

Mesh : Anti-Bacterial Agents / pharmacology therapeutic use Bacterial Proteins / genetics Drug Resistance, Bacterial / drug effects genetics Enterobacteriaceae / drug effects genetics isolation & purification Enterobacteriaceae Infections / drug therapy Humans Microbial Sensitivity Tests Plasmids / drug effects genetics Porins / drug effects genetics Quinolones / pharmacology therapeutic use

来  源:   DOI:10.1093/trstmh/traa041   PDF(Sci-hub)

Abstract:
Quinolones are broad-spectrum antibiotics, which are used for the treatment of different infectious diseases associated with Enterobacteriaceae. During recent decades, the wide use as well as overuse of quinolones against diverse infections has led to the emergence of quinolone-resistant bacterial strains. Herein, we present the development of quinolone antibiotics, their function and also the different quinolone resistance mechanisms in Enterobacteriaceae by reviewing recent literature.
All data were extracted from Google Scholar search engine and PubMed site, using keywords; quinolone resistance, Enterobacteriaceae, plasmid-mediated quinolone resistance, etc.
The acquisition of resistance to quinolones is a complex and multifactorial process. The main resistance mechanisms consist of one or a combination of target-site gene mutations altering the drug-binding affinity of target enzymes. Other mechanisms of quinolone resistance are overexpression of AcrAB-tolC multidrug-resistant efflux pumps and downexpression of porins as well as plasmid-encoded resistance proteins including Qnr protection proteins, aminoglycoside acetyltransferase (AAC(6\')-Ib-cr) and plasmid-encoded active efflux pumps such as OqxAB and QepA. The elucidation of resistance mechanisms will help researchers to explore new drugs against the resistant strains.
摘要:
喹诺酮类药物是广谱抗生素,用于治疗与肠杆菌科相关的不同传染病。近几十年来,喹诺酮类药物对各种感染的广泛使用和过度使用导致了喹诺酮耐药菌株的出现。在这里,我们介绍了喹诺酮类抗生素的发展,通过回顾最近的文献,它们的功能以及肠杆菌科细菌中不同的喹诺酮耐药机制。
所有数据均来自GoogleScholar搜索引擎和PubMed网站,使用关键词;喹诺酮耐药,肠杆菌科,质粒介导的喹诺酮耐药,等。
喹诺酮类药物抗性的获得是一个复杂的多因素过程。主要的抗性机制由改变目标酶的药物结合亲和力的靶位点基因突变中的一个或组合组成。喹诺酮耐药的其他机制是AcrAB-tolC多药耐药外排泵的过表达和孔蛋白的下调以及质粒编码的耐药蛋白,包括Qnr保护蛋白,氨基糖苷乙酰转移酶(AAC(6')-Ib-cr)和质粒编码的主动外排泵,例如OqxAB和QepA。阐明耐药机制将有助于研究人员探索针对耐药菌株的新药。
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