Babich H, Stern A, Munday R
Department of Biological Sciences, Stern College, Yeshiva University, New York, NY 10016.
Toxicol Lett. 1993 Jul;69(1):69-75. doi: 10.1016/0378-4274(93)90147-p.
The acute cytotoxicities of a series of alkyl-1,4-naphthoquinones (NQ) and of 2-hydroxy-3-alkyl-1,4-NQs, as well as some amino derivatives, were evaluated with the neutral red cytotoxicity assay, using BALB/c mouse 3T3 fibroblasts. As compared to the unsubstituted 1,4-NQ: (i) Substitution at the 2 position reduced toxicity, with the extent of reduction following the sequence, hydroxyl >> dimethylamino >> C1-C5 alkyl group. (ii) Substitution with C2-C5 alkyl groups at position 3 enhanced toxicity. As noted with the n-alkyl-1,4-NQs, increasing the chain length of the 2-hydroxy-3-alkyl-1,4-NQs did not appreciably change potency of the test agent. (iii) Substitution with amino groups at position 3 had little effect on cytotoxicity. Some differences in cytotoxicity of specific test agent were noted between the 3T3 fibroblasts and isolated rat hepatocytes, as reported in the literature.
使用BALB/c小鼠3T3成纤维细胞，通过中性红细胞毒性试验评估了一系列烷基-1,4-萘醌（NQ）、2-羟基-3-烷基-1,4-NQ以及一些氨基衍生物的急性细胞毒性。与未取代的1,4-NQ相比：（i）2位取代降低了毒性，降低程度遵循以下顺序：羟基>>二甲氨基>>C1-C5烷基。（ii）3位用C2-C5烷基取代增强了毒性。正如正烷基-1,4-NQ的情况一样，增加2-羟基-3-烷基-1,4-NQ的链长对受试药物的效力没有明显影响。（iii）3位用氨基取代对细胞毒性影响很小。如文献报道，在3T3成纤维细胞和分离的大鼠肝细胞之间，观察到特定受试药物在细胞毒性方面存在一些差异。
