The organospecific activity of metronidazole and azanidazole in the intrasanguineous host-mediated assay. 1985

G Cantelli-Forti, and P Hrelia, and M Paolini, and G Bronzetti, and G L Biagi

The genotoxicity of nitroimidazoles and, in particular, their potential carcinogenicity has been demonstrated. In order to investigate the specific target organ(s) for these drugs or their metabolites, a method for measuring mutations in microorganisms, with reference to the metabolism of mammals, was used in mice. Metronidazole and azanidazole were tested for their ability to induce genetic effects in a diploid strain (D7) of Saccharomyces cerevisiae in the Intrasanguineous Host-Mediated Assay. The test compounds showed dose-related increases of point mutation and mitotic gene conversion frequencies in liver, kidney and lung. Azanidazole seemed to favour the kidney and the liver, although increases in genotoxicity were observed also in the lung. Metronidazole was toxic and induced both point mutation and mitotic gene conversion when recovered from the liver. Yeast recovered from the kidney and the lung showed an increase especially in point mutation. This work provides more information about the mechanisms involved in the mutagenicity of nitroimidazoles at the site of action.

UI MeSH Term Description Entries
D008297 Male Males
D008795 Metronidazole A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS. 2-Methyl-5-nitroimidazole-1-ethanol,Bayer 5360,Clont,Danizol,Flagyl,Gineflavir,Metric,MetroGel,Metrodzhil,Metrogyl,Metronidazole Hydrochloride,Metronidazole Monohydrochloride,Metronidazole Phosphate,Metronidazole Phosphoester,Satric,Trichazol,Trichopol,Trivazol,Vagilen,2 Methyl 5 nitroimidazole 1 ethanol
D009153 Mutagens Chemical agents that increase the rate of genetic mutation by interfering with the function of nucleic acids. A clastogen is a specific mutagen that causes breaks in chromosomes. Clastogen,Clastogens,Genotoxin,Genotoxins,Mutagen
D009154 Mutation Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations. Mutations
D009593 Nitroimidazoles IMIDAZOLES having a nitro moiety. Nitroimidazole
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004353 Drug Evaluation, Preclinical Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications. Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000994 Antitrichomonal Agents Agents used to treat trichomonas infections. Antitrichomonal Drugs,Antitrichomonals,Trichomonicides,Agents, Antitrichomonal,Drugs, Antitrichomonal
D012441 Saccharomyces cerevisiae A species of the genus SACCHAROMYCES, family Saccharomycetaceae, order Saccharomycetales, known as "baker's" or "brewer's" yeast. The dried form is used as a dietary supplement. Baker's Yeast,Brewer's Yeast,Candida robusta,S. cerevisiae,Saccharomyces capensis,Saccharomyces italicus,Saccharomyces oviformis,Saccharomyces uvarum var. melibiosus,Yeast, Baker's,Yeast, Brewer's,Baker Yeast,S cerevisiae,Baker's Yeasts,Yeast, Baker

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