Bartoli-Klugmann F, Pani B, Babudri N, Montibragadin C, Tamaro M, Venturini S
Carcinogenesis. 1982;3(5):467-71. doi: 10.1093/carcin/3.5.467.
The in vitro mutagenic activity of 5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide (DTIC), has been studied in bacteria and Chinese hamster cells with and without metabolic activation by rat liver microsomes. DTIC was found to be highly mutagenic in the two systems. It is noteworthy that DTIC in the prokaryotic systems did not require metabolic activation to be effective. By comparing the mutagenic activity on bacteria of DTIC and of its monomethyl-and hydroxy-methyl-derivatives (MIC and HMIC), it is evident that MIC and HMIC display a pattern of mutagenicity different from DTIC. It suggests that neither MIC nor HMIC are the direct responsible metabolites for the mutagenic activity of DTIC in bacteria.
5-(3,3-二甲基-1-三氮烯基)-咪唑-4-甲酰胺(DTIC)在有或无大鼠肝微粒体代谢激活的情况下,对细菌和中国仓鼠细胞的体外诱变活性已被研究。发现DTIC在这两种系统中具有高度诱变性。值得注意的是,DTIC在原核系统中不需要代谢激活就能发挥作用。通过比较DTIC及其单甲基和羟甲基衍生物(MIC和HMIC)对细菌的诱变活性,很明显MIC和HMIC表现出与DTIC不同的诱变模式。这表明MIC和HMIC都不是DTIC在细菌中诱变活性的直接责任代谢物。