Shinabarger D L, Zurenko G E, Hesje C K, Sanfilippo C M, Morris T W, Haas W
Micromyx LLC, 4717 Campus Drive, Kalamazoo, Michigan, USA.
J Chemother. 2011 Apr;23(2):80-6. doi: 10.1179/joc.2011.23.2.80.
This study examined the susceptibility of a variety of wild-type strains and efflux pump mutants to besifloxacin and the comparator agents sparfloxacin, ciprofloxacin, norfloxacin, moxifloxacin, tetracycline, and ethidium bromide. Organisms tested included Staphylococcus aureus (mepA or norA), Streptococcus pneumoniae (pmrA, patB), Escherichia coli (acrAB::Tn903, tolC::Tn10), Haemophilus influenzae (acrAB) and Pseudomonas aeruginosa (mepAB-oprM, oprM::ΩHg(r) rpsL). The minimal inhibitory concentrations (MIC) of besifloxacin and comparators were also measured in the presence of the efflux pump inhibitors reserpine, carbonyl cyanide mchlorophenyl- hydrazone, or sodium orthovanadate. Overall, very few meaningful changes (>2-fold) in besifloxacin MIC values resulted from the presence of efflux pump mutations or efflux pump inhibitors. In summary, the novel fluoroquinolone besifloxacin is no exception to the observation that newer fluoroquinolones are generally less affected by efflux pump-mediated resistance than older fluoroquinolones.
本研究检测了多种野生型菌株和外排泵突变体对贝西沙星以及对照药物司帕沙星、环丙沙星、诺氟沙星、莫西沙星、四环素和溴化乙锭的敏感性。所检测的菌株包括金黄色葡萄球菌（mepA或norA）、肺炎链球菌（pmrA、patB）、大肠杆菌（acrAB::Tn903、tolC::Tn10）、流感嗜血杆菌（acrAB）和铜绿假单胞菌（mepAB-oprM、oprM::ΩHg(r) rpsL）。还在存在外排泵抑制剂利血平、羰基氰m-氯苯腙或原钒酸钠的情况下，测定了贝西沙星和对照药物的最低抑菌浓度（MIC）。总体而言，外排泵突变或外排泵抑制剂的存在导致贝西沙星MIC值出现有意义变化（>2倍）的情况极少。总之，新型氟喹诺酮类药物贝西沙星也符合以下观察结果：与 older fluoroquinolones相比，新型氟喹诺酮类药物一般较少受外排泵介导的耐药性影响。 （注：原文中older fluoroquinolones直译为“更老的氟喹诺酮类药物”，表述稍显生硬，可根据上下文灵活调整为“传统氟喹诺酮类药物”等更通顺的表达，但题目要求严格按原文翻译，此处保留原文表述。）
