Seixas G M, Andon B M, Hollingshead P G, Thilly W G
Mutat Res. 1982 Oct-Nov;102(3):201-12. doi: 10.1016/0165-1218(82)90130-6.
Several unsubstituted aza-arenes have been found to be more mutagenic to Salmonella typhimurium than their corresponding parent hydrocarbons. In most cases, the activity of these compounds depended on the presence of a post-mitochondrial supernatant for metabolic activation, although acridine was mutagenic only in the absence of such an activating system. An examination of the effect of the metabolizing system's concentration on mutagenicity showed that quinoline, benzo[f]quinoline, and phenanthridine have different optima. In an attempt to uncover active intermediates in aza-arene metabolism, N-oxides of quinoline and phenanthridine were synthesized and found to be non-mutagenic, and coincubation with the epoxide hydrase inhibitor trichloropropylene oxide did not affect the mutagenic activity of quinoline or phenanthridine.
已发现几种未取代的氮杂芳烃对鼠伤寒沙门氏菌的致突变性比其相应的母体烃更强。在大多数情况下，这些化合物的活性取决于线粒体后上清液的存在以进行代谢活化，尽管吖啶仅在没有这种活化系统的情况下才具有致突变性。对代谢系统浓度对致突变性的影响进行的研究表明，喹啉、苯并[f]喹啉和菲啶具有不同的最佳浓度。为了揭示氮杂芳烃代谢中的活性中间体，合成了喹啉和菲啶的N-氧化物，发现它们无致突变性，并且与环氧水解酶抑制剂三氯环氧丙烷共同孵育并不影响喹啉或菲啶的致突变活性。
