In vitro antichlamydial activity of garenoxacin against Chlamydia trachomatis

被引:0
|
作者
Futakuchi, Naoko [1 ]
Nakatani, Masatoshi [1 ]
Takahata, Masahiro [1 ]
Mitsuyama, Junichi [1 ]
机构
[1] Toyama Chem Co Ltd, Res Labs, Toyama 9308508, Japan
关键词
Garenoxacin; Chlamydia trachomatis; DNA gyrase; Transmission electron microscopy; TOPOISOMERASE-IV; DNA GYRASE; QUINOLONE-RESISTANCE; PHARMACOKINETICS; BMS-284756; MUTATIONS; T-3811ME; REGIONS; SAFETY; PARC;
D O I
10.1007/s10156-011-0345-8
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Garenoxacin showed the most potent chlamydial activity against Chlamydia trachomatis D/UW-3/Cx among three tested quinolones and azithromycin. The DNA gyrase genes, gyrA and gyrB, of C. trachomatis D/UW-3/Cx were cloned and the GyrA and GyrB subunits of DNA gyrase protein were separately expressed as histidine-tagged proteins in Escherichia coli. The mean 50% inhibitory concentration (IC50) of garenoxacin against the supercoiling activity of C. trachomatis D/UW-3/Cx gyrase was 2.9 +/- 0.4 mu g/ml, which was the most potent inhibitory activity against DNA gyrase among the quinolones tested in this study. At an extracellular concentration of 0.5 mu g/ml, the cellular-to-extracellular concentration ratio of garenoxacin was 15.3 +/- A 1.3, equivalent to that of moxifloxacin and greater than that of levofloxacin. In a time-kill experiment, after exposure to garenoxacin at a concentration of 0.5 mu g/ml at 0-6, 5-11, and 24-30 h after infection, the percentages of recoverable chlamydial inclusion-forming units were 11.1 +/- A 3.3, 0.6 +/- A 0.1, and 2.6 +/- A 0.5%, respectively. On transmission electron microscopy observation, after exposure to garenoxacin at 24-30 h after infection, some C. trachomatis elementary bodies remained in the inclusion body; however, the reticulate bodies were completely disrupted. In conclusion, garenoxacin is expected to be a useful quinolone in the treatment of infectious diseases caused by C. trachomatis.
引用
收藏
页码:428 / 435
页数:8
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