Antitrichomonad Action, Mutagenicity, and Reduction of Metronidazole and Other Nitroimidazoles
AUTOR(ES)
Lindmark, Donald G.
RESUMO
Twelve 4- and 5-nitroimidazole derivatives, including metronidazole and two of its metabolites, tinidazole, dimetridazole, and nimorazole, were tested for antitrichomonad action on Tritrichomonas foetus (KV1) and Trichomonas vaginalis (ATCC 30001) for mutagenicity on a nitroreductase-positive (TA 100) and a nitroreductase-deficient (TA 100-FR1) strain of Salmonella typhimurium, as well as for the reducibility of the nitro group by T. foetus homogenates. Compounds with activity <1% of that of metronidazole are regarded as inactive. All antitrichomonad compounds induce mutations and can be reduced. S. typhimurium TA 100 gave mutations under both aerobiosis and anaerobiosis; TA 100-FR1, however, gave mutations only under anaerobiosis. Certain compounds that are reducible, and the nonreducible derivatives, were inactive. Metronidazole and its inactive 4-nitro analogue were reduced in a four-electron process in ferredoxin- or methyl viologen-mediated reactions with the same velocity. The results underscore the role of the reduction of the nitro group in the antitrichomonad and in the mutagenic activity of nitroimidazoles.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=429775Documentos Relacionados
- Strain of Trichomonas vaginalis Resistant to Metronidazole and Other 5-Nitroimidazoles
- Mutagenicity, Carcinogenicity, and Teratogenicity of Industrial Pollutants
- Studies of genotoxicity and mutagenicity of nitroimidazoles: demystifying this critical relationship with the nitro group
- Efficacy of New 5-Nitroimidazoles against Metronidazole-Susceptible and -Resistant Giardia, Trichomonas, and Entamoeba spp.
- Antiseptics and Disinfectants: Activity, Action, and Resistance