Fukushima S, Ishihara Y, Nishio O, Ogiso T, Shirai T, Ito N
Cancer Lett. 1981 Nov;14(2):115-23. doi: 10.1016/0304-3835(81)90120-8.
In Ames test, the quinoline derivatives, 6-nitroquinoline (6-NQ), 8-nitroquinoline (8-NQ), 6-methylquinoline (6-NQ), 8-methylquinoline (8-MQ) and 8-hydroxyquinoline (8-HQ) are mutagenic, whereas 5,7-dibromo-quinoline (5,7-DQ) is not. These compounds were administered to groups of male and female F344 rats in their diet for 104 weeks. 8-NQ induced forestomach tumors in male and female rats: it induced squamous cell papillomas in 28 (93.3%) of 30 males and in 36 (97.3%) of 37 females, and squamous cell carcinomas in 20 (66.7%) of 30 males and 24 (64.9%) of 37 females. Thus there was no sex difference in its carcinogenicity. 6-NQ induced only focal hyperplasia of the forestomach at an incidence of 30.0% in male rats and 52.8% in female rats. These results indicate a discrepancy between the mutagenicities of quinoline derivatives and their carcinogenicities to rats: only 8-NQ was carcinogenic to F344 rats.
在艾姆斯试验中,喹啉衍生物6-硝基喹啉(6-NQ)、8-硝基喹啉(8-NQ)、6-甲基喹啉(6-MQ)、8-甲基喹啉(8-MQ)和8-羟基喹啉(8-HQ)具有致突变性,而5,7-二溴喹啉(5,7-DQ)则不具有。这些化合物通过混入饲料的方式给予多组雄性和雌性F344大鼠,持续104周。8-NQ在雄性和雌性大鼠中均诱发了前胃肿瘤:在30只雄性大鼠中有28只(93.3%)诱发了鳞状细胞乳头瘤,在37只雌性大鼠中有36只(97.3%)诱发了鳞状细胞乳头瘤;在30只雄性大鼠中有20只(66.7%)诱发了鳞状细胞癌,在37只雌性大鼠中有24只(64.9%)诱发了鳞状细胞癌。因此,其致癌性不存在性别差异。6-NQ仅诱发了前胃局灶性增生,在雄性大鼠中的发生率为30.0%,在雌性大鼠中的发生率为52.8%。这些结果表明喹啉衍生物的致突变性与其对大鼠的致癌性之间存在差异:只有8-NQ对F344大鼠具有致癌性。