title: [In vitro short-term bactericidal activity and accumulation of NM394, the active metabolite of prulifloxacin, for Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa: comparison with ciprofloxacin, levofloxacin, and gatifloxacin].
abstract: The in vitro short-term bactericidal activity and accumulation of NM394, the active metabolite of prulifloxacin, was compared with those of ciprofloxacin (CPFX), levofloxacin (LVFX) and gatifloxacin (GFLX), using Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Of the 4 fluoroquinolones examined, NM394 accumulated to the highest concentration in all three strains. The order of concentration of the fluoroquinolones accumurated in S. aureus 209P JC-1, E. coli NIHJ JC-2 and P. aeruginosa PAO1 were NM394 >> CPFX > GFLX > or = LVFX. The accumulation of fluoroquinolones into bacterial cells correlated with their MICs of the drugs for E. coli and P. aeruginosa, whereas there was no correlation between the accumulation and MICs of the drugs for S. aureus. We also studied the reduction of viable cells after addition of each fluoroquinolones to clarify relationship between the short-term bactericidal activity and the accumulation of the quinolones. The short-term bactericidal activity of NM394 against S. aureus 209P JC-1, E. coli NIHJ JC-2 and P. aeruginosa PAO1 were stronger than those of CPFX, LVFX and GFLX when compared at the same concentration. In conclusion, the strong short-term bactericidal activity of NM394 may be attributed to its high accumulation in bacterial cells.
authors.affiliation: Department of Microbiology, Kyoto Pharmaceutical University.
authors.forename: Masaki
authors.initials: M
authors.lastname: Shimizu
authors.forename: Makiko
authors.initials: M
authors.lastname: Tabata
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Hara
authors.forename: Minako
authors.initials: M
authors.lastname: Araake
authors.forename: Hiroomi
authors.initials: H
authors.lastname: Watabe
authors.forename: Takeshi
authors.initials: T
authors.lastname: Nishino
mesh_terms: D000890:Anti-Infective Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000493:pharmacokinetics / Q000494:pharmacology; D004148:Dioxolanes / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial; D004926:Escherichia coli / Q000187:drug effects* / Q000378:metabolism; D024841:Fluoroquinolones; D000077734:Gatifloxacin; D064704:Levofloxacin; D015242:Ofloxacin / Q000493:pharmacokinetics / Q000494:pharmacology; D010879:Piperazines / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011355:Prodrugs / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects* / Q000378:metabolism; D015363:Quinolones / Q000493:pharmacokinetics* / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000378:metabolism; D013997:Time Factors
chemical_list: D000890:Anti-Infective Agents; D004148:Dioxolanes; D024841:Fluoroquinolones; D010879:Piperazines; D011355:Prodrugs; D015363:Quinolones; D002939:Ciprofloxacin; D064704:Levofloxacin; D015242:Ofloxacin; C074190:ulifloxacin; C074191:prulifloxacin; D000077734:Gatifloxacin