[Inhibitory activity of NM394, the active form of prodrug prulifloxacin against type II topoisomerase from Pseudomonas aeruginosa].
[Inhibitory activity of NM394, the active form of prodrug prulifloxacin against type II topoisomerase from Pseudomonas aeruginosa].
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[NM394（前药普利沙星的活性形式）对铜绿假单胞菌 II 型拓扑异构酶的抑制活性]。
DOI：
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发表时间：
2002
期刊：
影响因子：
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通讯作者：
H. Watabe
中科院分区：
文献类型：
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作者：
M. Tani;K. Maebashi;M. Araake;H. Watabe
将前药普利沙星的活性形式 NM394 对铜绿假单胞菌 II 型拓扑异构酶的抑制活性与环丙沙星 (CPFX)、左氧氟沙星 (LVFX) 和加替沙星 (GFLX) 进行比较。 NM394对DNA旋转酶的超螺旋活性和拓扑异构酶IV的去链活性的50%抑制浓度(IC50S)分别为1.21和21.1微克/ml。 NM394的IC50与CPFX相同，但低于LVFX和GFLX。四种药物对DNA旋转酶的抑制活性也与药物对铜绿假单胞菌PAO1的抗菌活性相对应。测试拓扑异构酶IV的去链活性的药物的IC50S比DNA旋转酶的超螺旋活性的IC50高17.4至24.2倍。这些结果表明DNA旋转酶比拓扑异构酶IV对喹诺酮类药物更敏感，并且可能是铜绿假单胞菌中喹诺酮类药物的主要靶标。我们得出结论，NM394 通过其对 DNA 旋转酶的强抑制活性发挥有效的抗菌活性。
The inhibitory activity of NM394, the active form of the prodrug prulifloxacin, against type II topoisomerase from Pseudomonas aeruginosa was compared with those of ciprofloxacin (CPFX), levofloxacin (LVFX) and gatifloxacin (GFLX). The 50% inhibitory concentrations (IC50S) of NM394 for supercoiling activity of DNA gyrase and the decatenation activity of topoisomerase IV were 1.21 and 21.1 micrograms/ml, respectively. The IC50 of NM394 was equal to that of CPFX and lower than those of LVFX and GFLX. The inhibitory activity of the four drugs for DNA gyrase was also corresponding to the antimicrobial activity of the drugs for P. aeruginosa PAO1. The IC50S of the drugs tested for the decatenation activity of topoisomerase IV were from 17.4 to 24.2 times higher than those for the supercoiling activities of DNA gyrase. These results show that DNA gyrase is more sensitive to quinolones than is topoisomerase IV and may be a primary target of quinolones in P. aeruginosa. We concluded that NM394 exerts the potent antimicrobial activity through its strong inhibitory activity for DNA gyrase.