Nagao M, Fujita Y, Wakabayashi K, Sugimura T
Biochem Biophys Res Commun. 1983 Jul 29;114(2):626-31. doi: 10.1016/0006-291x(83)90826-4.
A mutant strain of Salmonella typhimurium TA98/1,8-DNP6 isolated by McCoy et al. (1) was reported to be defective in esterifying activity. We have found that 2-amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole (Glu-P-1), 2-aminodipyrido[1,2-a:3',2'-d]imidazole (Glu-P-2), 2-amino-3-methylimidazo-[4,5-f]quinoline (IQ), 2-amino-3,4-dimethylimidazo[4,5-f]quinoline (MeIQ) and 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) were not mutagenic to TA98/1,8-DNP6 with S9 mix, while these compounds were strongly mutagenic to the original TA98 with S9 mix. The mutagenicities of some of these heterocyclic amines to TA98 were inhibited by pentachlorophenol, an aryl sulfotransferase inhibitor. These results indicate that the ultimate forms of these heterocyclic amines are probably sulfate esters of heterocyclic amine N-hydroxides. Contrary to this, 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole (Trp-P-1), 3-amino-1-methyl-5H-pyrido[4,3-b]indole (Trp-P-2), 2-amino-9H-pyrido[2,3-b]indole (A alpha C) and 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeA alpha C) were definitely mutagenic to TA98/1,8-DNP6, although less than to TA98.
麦科伊等人（1）分离出的鼠伤寒沙门氏菌TA98/1,8 - DNP6突变株据报道在酯化活性方面存在缺陷。我们发现，2 - 氨基 - 6 - 甲基二吡啶并[1,2 - a:3',2'- d]咪唑（Glu - P - 1）、2 - 氨基二吡啶并[1,2 - a:3',2'- d]咪唑（Glu - P - 2）、2 - 氨基 - 3 - 甲基咪唑并[4,5 - f]喹啉（IQ）、2 - 氨基 - 3,4 - 二甲基咪唑并[4,5 - f]喹啉（MeIQ）和2 - 氨基 - 3,8 - 二甲基咪唑并[4,5 - f]喹喔啉（MeIQx）在有S9混合物存在的情况下对TA98/1,8 - DNP6无致突变性，而这些化合物在有S9混合物存在的情况下对原始的TA98有很强的致突变性。这些杂环胺中的一些对TA98的致突变性受到芳基磺基转移酶抑制剂五氯苯酚的抑制。这些结果表明，这些杂环胺的最终形式可能是杂环胺N - 氧化物的硫酸酯。与此相反，3 - 氨基 - 1,4 - 二甲基 - 5H - 吡啶并[4,3 - b]吲哚（Trp - P - 1）、3 - 氨基 - 1 - 甲基 - �H - 吡啶并[4,3 - b]吲哚（Trp - P - 2）、2 - 氨基 - 9H - 吡啶并[2,3 - b]吲哚（AαC）和2 - 氨基 - 3 - 甲基 - 9H - 吡啶并[2,3 - b]吲哚（MeAαC）对TA98/1,8 - DNP6肯定有致突变性，尽管比对TA98的致突变性小。
