Mutagenic activity of 4 active-principle forms of pharmaceutical drugs. Comparative study in the Salmonella typhimurium microsome test, and the HGPRT and Na+/K+ ATPase systems in cultured mammalian cells.
The nitroimidazole derivatives used in human therapy have shown a strong mutagenic activity in bacterial tests using Ames strains of Salmonella typhimurium. Our study compared the response of 4 products of this family on bacterial target cells as well as on mammalian target cells (Chinese hamster V79 cells). The strong positive response on TA100 was greatly reduced on the nitroreductase-deficient strain TA100 Frl. Furthermore, no mutagenic activity was found in V79 mammalian cells that we examined for ouabain and 6-thioguanine resistance.
D000818:Animals; D001711:Biotransformation; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D007041:Hypoxanthine Phosphoribosyltransferase / Q000378:metabolism*; D008168:Lung; D008297:Male; D008795:Metronidazole / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000378:metabolism; D009152:Mutagenicity Tests; D009153:Mutagens / Q000494:pharmacology; D009154:Mutation; D009554:Nimorazole / Q000494:pharmacology*; D009560:Niridazole / Q000494:pharmacology*; D009593:Nitroimidazoles / Q000494:pharmacology*; D010042:Ouabain / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D012486:Salmonella typhimurium / Q000187:drug effects*; D000254:Sodium-Potassium-Exchanging ATPase / Q000378:metabolism*; D013866:Thioguanine / Q000494:pharmacology; D014011:Tinidazole / Q000494:pharmacology*
D009153:Mutagens; D009593:Nitroimidazoles; D014011:Tinidazole; D008795:Metronidazole; D009554:Nimorazole; D010042:Ouabain; D007041:Hypoxanthine Phosphoribosyltransferase; D000254:Sodium-Potassium-Exchanging ATPase; D013866:Thioguanine; D009560:Niridazole