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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.

DOI:10.1128/AAC.42.5.1284
PMID:9593169
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC105807/
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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本文引用的文献

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Inhibitory activities of quinolones against DNA gyrase and topoisomerase IV purified from Staphylococcus aureus.喹诺酮类药物对从金黄色葡萄球菌中纯化的DNA回旋酶和拓扑异构酶IV的抑制活性。
Antimicrob Agents Chemother. 1997 Nov;41(11):2362-6. doi: 10.1128/AAC.41.11.2362.
2
Involvement of topoisomerase IV and DNA gyrase as ciprofloxacin targets in Streptococcus pneumoniae.拓扑异构酶IV和DNA促旋酶作为环丙沙星在肺炎链球菌中的作用靶点。
Antimicrob Agents Chemother. 1996 Oct;40(10):2321-6. doi: 10.1128/AAC.40.10.2321.
3
ParC subunit of DNA topoisomerase IV of Streptococcus pneumoniae is a primary target of fluoroquinolones and cooperates with DNA gyrase A subunit in forming resistance phenotype.肺炎链球菌DNA拓扑异构酶IV的ParC亚基是氟喹诺酮类药物的主要作用靶点，并与DNA回旋酶A亚基协同形成耐药表型。
Antimicrob Agents Chemother. 1996 Oct;40(10):2252-7. doi: 10.1128/AAC.40.10.2252.
4
Quinolone-resistant mutants of escherichia coli DNA topoisomerase IV parC gene.大肠杆菌DNA拓扑异构酶IV parC基因的喹诺酮抗性突变体
Antimicrob Agents Chemother. 1996 Mar;40(3):710-14. doi: 10.1128/AAC.40.3.710.
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Genetic evidence for a role of parC mutations in development of high-level fluoroquinolone resistance in Escherichia coli.关于parC突变在大肠杆菌高水平氟喹诺酮耐药性形成中作用的遗传学证据。
Antimicrob Agents Chemother. 1996 Apr;40(4):879-85. doi: 10.1128/AAC.40.4.879.
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