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达卡巴嗪类似物对氨基苯甲酸钠钾盐在细菌细胞中的诱变活性。

Mutagenic activity of the dacarbazine analog p-(3,3-dimethyl-1-triazeno)benzoic acid potassium salt in bacterial cells.

作者信息

Tamaro M, Dolzani L, Monti-Bragadin C, Sava G

出版信息

Pharmacol Res Commun. 1986 May;18(5):491-501. doi: 10.1016/0031-6989(86)90169-4.

Abstract

The mutagenic activity of the antimetastatic agent p-(3,3-dimethyl-1-triazeno)benzoic acid potassium salt (DM-COOK) was studied in procaryotic cells and compared with that of dacarbazine (DTIC) which is clinically used in the management of human neoplasms. The results indicated that DM-COOK has a very low mutagenic activity on the Salmonella typhimurium strains tested, while it is more effective in inducing trp+ revertants in E. coli B strains. The magnitude of these effects was always less pronounced than that displayed by DTIC. The mutagenic activity of DM-COOK appeared to be independent from the addition of a metabolic activating system and had a different pattern from that displayed by MM-COOK. It is therefore unlikely that DM-COOK acts through conversion into the monomethyl derivative.

摘要

研究了抗转移剂对-(3,3-二甲基-1-三氮烯)苯甲酸钾盐(DM-COOK)在原核细胞中的诱变活性,并与临床上用于治疗人类肿瘤的达卡巴嗪(DTIC)进行了比较。结果表明,DM-COOK在所测试的鼠伤寒沙门氏菌菌株上具有非常低的诱变活性,而在诱导大肠杆菌B菌株中的色氨酸+回复突变体方面更有效。这些效应的程度总是比DTIC表现出的效应不那么明显。DM-COOK的诱变活性似乎与添加代谢激活系统无关,并且具有与MM-COOK不同的模式。因此,DM-COOK不太可能通过转化为单甲基衍生物起作用。

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