喹诺酮类药物对大肠杆菌DNA回旋酶及胎牛胸腺拓扑异构酶II的抑制作用。
Inhibitory effects of quinolones on DNA gyrase of Escherichia coli and topoisomerase II of fetal calf thymus.
作者信息
Hoshino K, Sato K, Une T, Osada Y
机构信息
Research Institute, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
出版信息
Antimicrob Agents Chemother. 1989 Oct;33(10):1816-8. doi: 10.1128/AAC.33.10.1816.
Abstract
The in vitro inhibitory effects of quinolones on the bacterial DNA gyrase of Escherichia coli KL-16 and topoisomerase II of fetal calf thymus were compared. All the quinolones tested required higher concentrations to inhibit the topoisomerase II than to inhibit the DNA gyrase, and no correlation existed among their inhibitory activities against both enzymes. However, there was a large difference among the quinolones in their selectivities between the bacterial enzyme and its eucaryotic counterpart. The selectivity of ofloxacin was highest, and the selectivities of CI-934 and nalidixic acid were lowest.
摘要
比较了喹诺酮类药物对大肠杆菌KL-16的细菌DNA促旋酶和胎牛胸腺拓扑异构酶II的体外抑制作用。所有测试的喹诺酮类药物抑制拓扑异构酶II所需的浓度均高于抑制DNA促旋酶所需的浓度，且它们对这两种酶的抑制活性之间不存在相关性。然而，喹诺酮类药物在细菌酶与其真核对应物之间的选择性存在很大差异。氧氟沙星的选择性最高，CI-934和萘啶酸的选择性最低。
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