Taniguchi S, Kimura N T, Baba T
Jpn J Pharmacol. 1981 Apr;31(2):243-7. doi: 10.1254/jjp.31.243.
To assess the effects of pH on the cytotoxicity of carboquone (CQ), use was made of the mouse tail skin and HeLa cells in culture. CQ had the most potent cytotoxic effect at pH 6 rather than at pH7 or 8. Regarding the interaction between 14C-CQ and HeLa cells, both the intracellular accumulation of free 14C-CQ and the ratio of bound 14C-CQ to total 14C-CQ uptake were enhanced at pH6. Among the fractionated biomolecules of DNA, RNA and protein, DNA was the most active in binding CQ, under the same conditions of pH. The 14C-CQ binding to nucleic acids at pH 6 was more apparent than was the binding to protein. Thus, the enhancement of CQ cytotoxicity at low pHs is probably due to an increase in the intracellular accumulation of free CQ as well as to an enhanced reactivity of CQ with DNA, within the ranges of a lower pH.
为评估pH值对卡波醌（CQ）细胞毒性的影响，利用了小鼠尾皮和培养的HeLa细胞。CQ在pH 6时具有最强的细胞毒性，而非在pH 7或8时。关于14C - CQ与HeLa细胞之间的相互作用，在pH 6时，游离14C - CQ的细胞内积累以及结合的14C - CQ与总14C - CQ摄取量的比率均有所增强。在DNA、RNA和蛋白质的分级生物分子中，在相同pH条件下，DNA与CQ结合的活性最高。14C - CQ在pH 6时与核酸的结合比与蛋白质的结合更为明显。因此，在较低pH范围内，CQ细胞毒性的增强可能是由于游离CQ细胞内积累的增加以及CQ与DNA反应性的增强。
