Smith C, Payne V, Doolittle D J, Debnath A K, Lawlor T, Hansch C
R.J. Reynolds Tobacco Company, Winston-Salem, NC 27102.
Mutat Res. 1992 May 1;279(1):61-73. doi: 10.1016/0165-1218(92)90267-4.
26 synthetic and naturally occurring heterocyclic amines were tested in the Salmonella/microsome assay (Ames test) using tester strains TA98 and TA100 in the presence of an Aroclor-induced rat-liver S9 fraction. 9 of the compounds were protein-pyrolysis products which had previously been shown to be mutagenic. Mutagenic potencies similar to previously reported values were demonstrated for these compounds with the exception that Trp-P-1 was only mutagenic in strain TA98 in our study, although it had previously been reported to be weakly mutagenic in strain TA100. 17 structurally diverse heterocyclic amines were synthesized and tested for mutagenicity. The structural diversity of these synthetic heterocyclic amines will enhance the sensitivity of future quantitative structure-activity relationship (QSAR) studies by demonstrating the structural characteristics essential for mutagenicity. The results of this study provide a large data base for the mutagenicity of this important class of compounds.
在存在艾氏剂诱导的大鼠肝脏S9组分的情况下，使用测试菌株TA98和TA100，在沙门氏菌/微粒体试验（Ames试验）中对26种合成的和天然存在的杂环胺进行了测试。其中9种化合物是蛋白质热解产物，先前已证明具有致突变性。除了Trp-P-1在我们的研究中仅在TA98菌株中具有致突变性外，这些化合物的致突变效力与先前报道的值相似，尽管之前报道它在TA100菌株中具有弱致突变性。合成了17种结构多样的杂环胺并测试了其致突变性。这些合成杂环胺的结构多样性将通过证明致突变性所必需的结构特征来提高未来定量构效关系（QSAR）研究的灵敏度。本研究结果为这类重要化合物的致突变性提供了一个大型数据库。
