Umezawa K, Haresaku M, Muramatsu M, Matsushima T
Institute of Microbial Chemistry, Tokyo.
Biomed Pharmacother. 1987;41(5):214-8.
Aclacinomycin A was nonmutagenic, while most anthracycline drugs such as daunomycin and adriamycin are highly mutagenic in a Salmonella test. But its derivative, N-demethylaclacinomycin A, was mutagenic. Similarly, aclavin, a hydrolysis product of aclacinomycin A, was nonmutagenic, but N-demethylaclavin was mutagenic. N-Methyldaunomycin showed only weak mutagenicity, and N-dimethyldaunomycin was nonmutagenic. Thus, the amino moiety of anthracycline glycosides is concluded to be essential for mutagenesis. Bleomycins were nonmutagenic to most Salmonella tester strains such as TA98, TA100 and TA92 and also to a Escherichia coli strain WP2/uvrA. Bleomycins were weakly mutagenic to Salmonella TA102 and TA94 strains which were extremely sensitive to detect DNA cross linking agents.
阿克拉霉素A无致突变性,而大多数蒽环类药物如柔红霉素和阿霉素在沙门氏菌试验中具有高度致突变性。但其衍生物N-去甲基阿克拉霉素A具有致突变性。同样,阿克拉霉素A的水解产物阿克拉文无致突变性,但N-去甲基阿克拉文具有致突变性。N-甲基柔红霉素仅表现出微弱的致突变性,而N-二甲基柔红霉素无致突变性。因此,蒽环类糖苷的氨基部分被认为是诱变作用所必需的。博来霉素对大多数沙门氏菌测试菌株如TA98、TA100和TA92以及大肠杆菌菌株WP2/uvrA无致突变性。博来霉素对沙门氏菌TA102和TA94菌株有微弱的致突变性,这两种菌株对检测DNA交联剂极为敏感。