title: DNA strand-breaking activities of quinolone antimicrobial agents under visible light irradiation.
abstract: The DNA strand-breaking activities of 9 quinolones, widely used as antimicrobial agents and suspected to induce photo-dermatological disorders in humans, were examined under irradiation using standard domestic fluorescent lamps. Two quinolones, tosufloxacin and enoxacin, converted the supercoiled covalently closed circular plasmid DNA to the open circular form under visible light irradiation. The maximum of photodynamic single strand-breaking activity for tosufloxacin was found to be 12% at 50 microM and that of enoxacin was 33% at a concentration of 2 mM. The DNA strand-breaking activities of photoirradiated tosufloxacin and enoxacin were markedly inhibited by NaN3 but only partially by D-mannitol, superoxide dismutase (SOD) and catalase did not inhibit these activities. These results suggest that some quinolone antimicrobial agents can be activated by visible light and induce phototoxic DNA damage in various organisms. We should carefully investigate such phototoxic activities during the development of new quinolones to avoid producing phototoxic disorders in man.
authors.affiliation: Department of Microbiology, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Iwamoto
authors.forename: A
authors.initials: A
authors.lastname: Kurita
authors.forename: T
authors.initials: T
authors.lastname: Shimizu
authors.forename: T
authors.initials: T
authors.lastname: Masuzawa
authors.forename: K
authors.initials: K
authors.lastname: Uno
authors.forename: M
authors.initials: M
authors.lastname: Yagi
authors.forename: T
authors.initials: T
authors.lastname: Kitagawa
authors.forename: T
authors.initials: T
authors.lastname: Oku
authors.forename: Y
authors.initials: Y
authors.lastname: Yanagihara
mesh_terms: D042462:4-Quinolones; D000890:Anti-Infective Agents / Q000494:pharmacology*; D004249:DNA Damage; D004269:DNA, Bacterial / Q000737:chemistry / Q000187:drug effects* / Q000528:radiation effects; D004591:Electrophoresis, Polyacrylamide Gel; D004926:Escherichia coli / Q000235:genetics / Q000378:metabolism; D016166:Free Radical Scavengers; D008027:Light; D010957:Plasmids / Q000187:drug effects / Q000528:radiation effects
chemical_list: D042462:4-Quinolones; D000890:Anti-Infective Agents; D004269:DNA, Bacterial; D016166:Free Radical Scavengers