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- Title
In vitro antichlamydial activity of garenoxacin against Chlamydia trachomatis.
- Authors
Futakuchi, Naoko; Nakatani, Masatoshi; Takahata, Masahiro; Mitsuyama, Junichi
- Abstract
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 (IC) of garenoxacin against the supercoiling activity of C. trachomatis D/UW-3/Cx gyrase was 2.9 ± 0.4 μg/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 μg/ml, the cellular-to-extracellular concentration ratio of garenoxacin was 15.3 ± 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 μg/ml at 0-6, 5-11, and 24-30 h after infection, the percentages of recoverable chlamydial inclusion-forming units were 11.1 ± 3.3, 0.6 ± 0.1, and 2.6 ± 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.
- Subjects
CHLAMYDIA; CHLAMYDIA infection treatment; CHLAMYDIA trachomatis; TRANSMISSION electron microscopy; DNA topoisomerase II; THERAPEUTICS
- Publication
Journal of Infection & Chemotherapy (Springer Science & Business Media B.V.), 2012, Vol 18, Issue 4, p428
- ISSN
1341-321X
- Publication type
Article
- DOI
10.1007/s10156-011-0345-8