Qadri S A, Islam S, Ahmad M
Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, India.
Mutat Res. 1992 Nov;298(1):53-60. doi: 10.1016/0165-1218(92)90028-x.
Oxathiolanes and disulfonyl derivatives of steroids were tested for mutagenic activity in the Ames tester strains. The test compounds exhibited mutagenic activity without metabolic activation although metabolic activation markedly enhanced their activity. A significant decrease in the survival of the radiation-sensitive mutants recA, lexA and rer of E. coli was observed as compared to their wild-type counterpart in the presence of the test steroid. Structural features which appear to be crucial for the mutagenic activity in these steroidal drugs are: (i) an electron-donating group at position 3, and (ii) a bulky group anchored at the 5th and 6th positions. The test steroids appear to damage DNA which in turn initiates the SOS repair with the concomitant induction of mutation.
对甾体的氧硫杂环戊烷和二磺酰基衍生物进行了艾姆斯试验菌株中的致突变活性测试。测试化合物在没有代谢激活的情况下表现出致突变活性，尽管代谢激活显著增强了它们的活性。与野生型大肠杆菌相比，在测试甾体存在的情况下，观察到辐射敏感突变体recA、lexA和rer的存活率显著降低。对于这些甾体药物中的致突变活性似乎至关重要的结构特征是：(i) 3位的供电子基团，以及 (ii) 锚定在第5和6位的庞大基团。测试甾体似乎会损伤DNA，进而引发SOS修复并伴随诱导突变。
