Jin Yan, Chen Shi-Wu, Tian Xuan
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China.
Bioorg Med Chem. 2006 May 1;14(9):3062-8. doi: 10.1016/j.bmc.2005.12.025. Epub 2006 Jan 9.
In order to find compounds with superior bioactivity and less toxicity, a series of spin-labeled podophyllotoxin derivatives were synthesized and tested for the partition coefficients and cytotoxicity against P-388 and A-549. Furthermore, we also determined antioxidant activities of target molecular in tissues of SD rats by the TBA method. Results revealed that most synthesized compounds showed more significant cytotoxicity against P-388 and A-549 in vitro than VP-16. Among them, 9d exhibited most potent cytotoxicity against P-388 and A-549 cells (IC50 is <0.01 and 0.13 microM, respectively). Also, the antioxidative activities showed that the modified compounds of 4'-demethylepipodophyllotoxin (9a-d and 10a-c) are higher than those of podophyllotoxin series (8a-d). The relationship between the cytotoxicity and antioxidative activity discussed.
为了寻找具有优异生物活性且毒性较小的化合物，合成了一系列自旋标记的鬼臼毒素衍生物，并测试了它们的分配系数以及对P - 388和A - 549的细胞毒性。此外，我们还通过TBA法测定了目标分子在SD大鼠组织中的抗氧化活性。结果表明，大多数合成化合物在体外对P - 388和A - 549显示出比VP - 16更显著的细胞毒性。其中，9d对P - 388和A - 549细胞表现出最有效的细胞毒性（IC50分别<0.01和0.13微摩尔）。此外，抗氧化活性表明，4'-去甲基表鬼臼毒素的修饰化合物（9a - d和10a - c）高于鬼臼毒素系列（8a - d）。讨论了细胞毒性与抗氧化活性之间的关系。
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