Synthesis and biological evaluation of new spin-labeled derivatives of podophyllotoxin
Synthesis and biological evaluation of new spin-labeled derivatives of podophyllotoxin
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DOI：
10.1016/j.bmc.2005.12.025
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发表时间：
2006-05-01
影响因子：
3.5
通讯作者：
Tian, X
中科院分区：
文献类型：
--
作者：
Jin, Y;Chen, SW;Tian, X
为了寻找具有上级生物活性和低毒性的化合物，合成了一系列自旋标记的鬼臼毒素衍生物，并测试了其对P-388和A-549的分配系数和细胞毒性。此外，我们还采用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，大多数合成的化合物在体外对P-388和A-549的细胞毒性比VP-16更显著。其中。9d对P-388和A-549细胞表现出最强的细胞毒性（IC 50分别为< 0.01和0.13 μ M）。抗氧化活性测定结果表明，4 ′-去甲基表鬼臼毒素修饰物（9a-d和10a-c）的抗氧化活性高于鬼臼毒素系列化合物（8a-d）。讨论了细胞毒性与抗氧化活性的关系。(c)2005爱思唯尔有限公司保留所有权利。
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 mu M, 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 cytotoxity and antioxidative activity discussed. (c) 2005 Elsevier Ltd. All rights reserved.