司帕沙星（DU-6859a）及其光学异构体对II型拓扑异构酶的抗菌活性和抑制作用。
Antibacterial activities and inhibitory effects of sitafloxacin (DU-6859a) and its optical isomers against type II topoisomerases.
作者信息
Akasaka T, Kurosaka S, Uchida Y, Tanaka M, Sato K, Hayakawa I
机构信息
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
出版信息
Antimicrob Agents Chemother. 1998 May;42(5):1284-7. doi: 10.1128/AAC.42.5.1284.
Abstract
The in vitro inhibitory effects of sitafloxacin (DU-6859a) and its three stereoisomers on bacterial DNA gyrase from Escherichia coli, topoisomerase IV from Staphylococcus aureus, and topoisomerase II from human placenta were compared. No correlation was observed between the inhibitory activities of quinolones against bacterial type II topoisomerases and those against human topoisomerase II. Sitafloxacin showed the most potent inhibitory activities against bacterial type II topoisomerases and the lowest activity against human type II topoisomerase.
摘要
比较了西他沙星（DU-6859a）及其三种立体异构体对大肠杆菌DNA回旋酶、金黄色葡萄球菌拓扑异构酶IV和人胎盘拓扑异构酶II的体外抑制作用。未观察到喹诺酮类药物对细菌II型拓扑异构酶的抑制活性与对人拓扑异构酶II的抑制活性之间存在相关性。西他沙星对细菌II型拓扑异构酶显示出最强的抑制活性，而对人II型拓扑异构酶的活性最低。
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