Piddock L J
Department of Infection, University of Birmingham, England.
Drugs. 1995;49 Suppl 2:29-35. doi: 10.2165/00003495-199500492-00006.
This paper gives an update on the mechanisms of bacterial resistance to fluoroquinolones. The laboratory techniques currently used to determine the mechanism(s) of resistance are outlined, including the use of restriction fragment length polymorphism and single-stranded conformational polymorphism analysis of mutations in gyrA. Alterations in gyrA have continued to be the most reported cause of resistance, with high level resistance due to 2 or more mutations in this gene. Recently, mutations in gyrA of Mycobacterium tuberculosis and Campylobacter jejuni have been described. Complementation studies with plasmid encoded cloned gyrB from Escherichia coli suggest that high fluoroquinolone resistance (minimum inhibitory concentration = 32 mg/L) in Salmonella typhimurium can be due to mutation in both gyrA and gyrB. Decreased fluoroquinolone accumulation into E. coli has been shown to be due to mutations in a number of genes at different loci. Current interest has focused upon the marRAB and soxRS loci, with mutations in genes of either loci giving rise to decreased susceptibility to several unrelated drugs, including fluoroquinolones, tetracycline, chloramphenicol and some beta-lactams, and decreased expression of OmpF. The genetic characterisation of fluoroquinolone efflux from Staphylococcus aureus has shown that efflux occurs in both fluoroquinolone-susceptible and -resistant bacteria. The most likely cause of resistance is overexpression of NorA, giving rise to increased efflux. Recently, 2 efflux systems in Pseudomonas aeruginosa have been proposed, MexA-MexB-OprK and MexC-MexD-OprM, conferring decreased susceptibility to fluoroquinolones, tetracycline, chloramphenicol and some beta-lactams.(ABSTRACT TRUNCATED AT 250 WORDS)
本文介绍了细菌对氟喹诺酮类药物耐药机制的最新情况。概述了目前用于确定耐药机制的实验室技术,包括使用限制性片段长度多态性和对gyrA基因突变进行单链构象多态性分析。gyrA基因的改变仍然是最常报道的耐药原因,该基因发生2个或更多突变会导致高水平耐药。最近,已描述了结核分枝杆菌和空肠弯曲菌gyrA基因的突变。用来自大肠杆菌的质粒编码克隆gyrB进行的互补研究表明,鼠伤寒沙门氏菌中高氟喹诺酮耐药性(最低抑菌浓度=32mg/L)可能是由于gyrA和gyrB基因均发生突变。已证明大肠杆菌中氟喹诺酮类药物蓄积减少是由于不同位点的多个基因突变所致。目前的研究兴趣集中在marRAB和soxRS位点,这两个位点中任何一个位点的基因突变都会导致对包括氟喹诺酮类、四环素、氯霉素和一些β-内酰胺类在内的几种不相关药物的敏感性降低,以及OmpF表达减少。金黄色葡萄球菌氟喹诺酮外排的遗传学特征表明,氟喹诺酮敏感菌和耐药菌中均存在外排现象。最可能的耐药原因是NorA过度表达,导致外排增加。最近,有人提出铜绿假单胞菌中有2种外排系统,即MexA-MexB-OprK和MexC-MexD-OprM,它们会导致对氟喹诺酮类、四环素、氯霉素和一些β-内酰胺类药物的敏感性降低。(摘要截选至250字)