杂环醌类化合物细胞毒性活性与还原电位的相关性。

Faculty of Pharmaceutical Sciences, Kobe Pharmaceutical University, Higashinada, Kobe, Japan.

Molecules. 2010 Sep 20;15(9):6559-69. doi: 10.3390/molecules15096559.

To search for possible anti-tumor agents or anti-tumor promoters among natural or synthetic products, we used cyclic voltammetry to determine the reduction-oxidation potentials of heterocyclic quinones in phosphate buffer at pH 7.2. We determined the growth inhibitory- and cytotoxic activities of 12 heterocyclic quinone anti-tumor agent candidates against a panel of 39 human cancer cell lines (JFCR39). The average concentrations of the heterocyclic quinones required for 50% growth inhibition (GI(50)) against JFCR39 ranged from 0.045 to 13.2 µM, and the 50% lethal concentration (LC(50)) against JFCR39 ranged from 0.398 to 77.7 µM. The average values of GI(50) or LC(50) of the heterocyclic quinones correlated significantly with their reduction potentials. These results suggested that reduction-oxidation potentials could be a useful method for the discovery of novel antitumor agents.

为了在天然或合成产物中寻找可能的抗肿瘤剂或抗肿瘤促进剂，我们使用循环伏安法在 pH 7.2 的磷酸盐缓冲液中测定杂环醌的氧化还原电位。我们测定了 12 种杂环醌抗肿瘤候选药物对一组 39 个人类癌细胞系（JFCR39）的生长抑制和细胞毒性活性。杂环醌对 JFCR39 的 50%生长抑制浓度（GI(50)）的平均浓度范围为 0.045 至 13.2 μM，对 JFCR39 的 50%致死浓度（LC(50)）范围为 0.398 至 77.7 μM。杂环醌的 GI(50)或 LC(50)的平均值与它们的还原电位显著相关。这些结果表明，氧化还原电位可能是发现新型抗肿瘤剂的一种有用方法。