The mutagenicity of rutacridone and rutacridone epoxide was investigated using Salmonella typhimurium without as well as with different metabolic activation systems. Rutacridone epoxide was found to be a direct acting mutagen in S. typhimurium strains TA98, TA100 and TA1538; addition of rat liver preparations resulted in a marked decrease of mutagenicity. In contrast, rutacridone required metabolic conversion to exhibit mutagenic activity. Neither of the compounds had any effect on tester strain TA1978. S9 mixes as well as microsomal and cytosolic preparations from untreated, phenobarbital-treated and 3-methylcholanthrene-treated rats were used to study the activation and deactivation capacities of the enzyme mixtures. In addition, the influence of enzyme inhibitors on the activation and deactivation of the furoacridones were tested. Evidence is presented that rutacridone is metabolized by rat liver enzymes to the corresponding epoxide as the ultimate mutagen.
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Paulini et al. (1989) studied this question.