司帕沙星（DU-6859a）对肺炎链球菌DNA旋转酶和拓扑异构酶IV的双重抑制活性。
Dual inhibitory activity of sitafloxacin (DU-6859a) against DNA gyrase and topoisomerase IV of Streptococcus pneumoniae.
作者信息
Onodera Y, Uchida Y, Tanaka M, Sato K
机构信息
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd, Tokyo, Japan.
出版信息
J Antimicrob Chemother. 1999 Oct;44(4):533-6. doi: 10.1093/jac/44.4.533.
The in-vitro inhibitory activities of sitafloxacin (DU-6859a) and other quinolones against Streptococcus pneumoniae DNA gyrase and topoisomerase IV were measured. IC50s of levofloxacin, ciprofloxacin, sparfloxacin and tosufloxacin against DNA gyrase were almost three to 12 times higher than those against topoisomerase IV. On the other hand, sitafloxacin showed dual inhibitory activity against both enzymes and its IC50s were the lowest among those of the quinolones tested. These results suggest that sitafloxacin is an effective agent against pneumococcal infections and that the incidence of drug-resistant mutants is low.
测定了西他沙星（DU-6859a）及其他喹诺酮类药物对肺炎链球菌DNA回旋酶和拓扑异构酶IV的体外抑制活性。左氧氟沙星、环丙沙星、司帕沙星和妥舒沙星对DNA回旋酶的IC50值比对拓扑异构酶IV的IC50值高近3至12倍。另一方面，西他沙星对这两种酶均表现出双重抑制活性，其IC50值在所测试的喹诺酮类药物中是最低的。这些结果表明，西他沙星是一种治疗肺炎球菌感染的有效药物，且耐药突变体的发生率较低。
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