title: In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae.
abstract: The in-vitro antibacterial activity of sitafloxacin (DU-6859a) against Mycobacterium leprae was evaluated and compared with those of ofloxacin, levofloxacin, and ciprofloxacin. Two biochemical indicators (intracellular ATP and uptake of [(3)H]-thymidine) were used to measure the in-vitro growth of M. leprae in Dhople-Hanks (DH) medium. Sitafloxacin was found to be more potent than the other three commonly used fluoroquinolones, with the minimum inhibitory concentration (MIC) against M. leprae being 0.1875 microg/ml and the action being bactericidal. The MICs of ofloxacin, levofloxacin, and ciprofloxacin were 1.5, 0.75, and 3.0 microg/ml, respectively. Similar to ofloxacin and levofloxacin, sitafloxacin also exhibited synergistic activity when combined with either rifabutin or KRM-1648, but not with rifampin. Thus, further studies on the incorporation of sitafloxacin in multidrug therapy regimens in treating leprosy patients are suggested.
authors.affiliation: Department of Biological Sciences, Florida Institute of Technology, 150 W University Boulevard, Melbourne, Florida 32901-6975, USA. adhople@fit.edu
authors.forename: Arvind M
authors.initials: AM
authors.lastname: Dhople
authors.forename: Kenji
authors.initials: K
authors.lastname: Namba
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology*; D001135:Armadillos; D004357:Drug Synergism; D004359:Drug Therapy, Combination; D024841:Fluoroquinolones; D006801:Humans; D007917:Leprostatic Agents / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009166:Mycobacterium leprae / Q000187:drug effects*; D017828:Rifabutin / Q000494:pharmacology; D012293:Rifampin / Q000031:analogs & derivatives / Q000494:pharmacology; D012294:Rifamycins / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D007917:Leprostatic Agents; D012294:Rifamycins; C068980:KRM 1648; D017828:Rifabutin; C076246:sitafloxacin; D012293:Rifampin