Takahashi K, Kaiya T, Kawazoe Y
Mutat Res. 1987 Apr;187(4):191-7. doi: 10.1016/0165-1218(87)90036-x.
The mutagenicity of 7 positional isomers of aminoquinolines (AQ) and their N-acetyl derivatives (AcAQ) was tested in Salmonella typhimurium TA100 and TA98 in the presence and absence of S9 mix. In a series of aminoquinolines, the order of mutagenic potency in the presence of S9 mix is: 5-AQ greater than 8-AQ greater than 7-AQ greater than 3-AQ greater than 2-AQ much greater than 4-AQ, 6-AQ. The alpha-positional isomers, 5-AQ and 8-AQ, are more mutagenic than the beta-isomer, 2-, 3-, 6-, 7-AQ's. These results are in contrast to the finding that beta-naphthylamine is more mutagenic than alpha-naphthylamine. In a series of N-acetylaminoquinolines, the order of mutagenic potency in the presence of S9 mix is: 7-AcAQ greater than 6-AcAQ greater than 8-AcAQ much greater than all the others. It is suggested that the AQ and AcAQ series might exert their mutagenicity through different molecular mechanisms (i.e., metabolic activation) from each other. The rate of metabolic activation does not seem to be correlated with the mutagenic potency of the compounds. It is noteworthy that 7-AQ and 8-AQ are mutagenic in both the strains tested in the absence of S9 mix.
在有和没有S9混合物存在的情况下，在鼠伤寒沙门氏菌TA100和TA98中测试了7种氨基喹啉（AQ）及其N - 乙酰基衍生物（AcAQ）的位置异构体的诱变性。在一系列氨基喹啉中，在有S9混合物存在时诱变性强度的顺序为：5 - AQ大于8 - AQ大于7 - AQ大于3 - AQ大于2 - AQ远大于4 - AQ、6 - AQ。α-位置异构体5 - AQ和8 - AQ比β-异构体2 -、3 -、6 -、7 - AQ更具诱变性。这些结果与β-萘胺比α-萘胺更具诱变性的发现形成对比。在一系列N - 乙酰氨基喹啉中，在有S9混合物存在时诱变性强度的顺序为：7 - AcAQ大于6 - AcAQ大于8 - AcAQ远大于所有其他异构体。有人提出，AQ和AcAQ系列可能通过彼此不同的分子机制（即代谢活化）发挥其诱变性。代谢活化速率似乎与化合物的诱变性强度无关。值得注意的是，7 - AQ和8 - AQ在没有S9混合物的情况下在所测试的两种菌株中均具有诱变性。
