The synthesis of ursolic acid derivatives with cytotoxic activity and the investigation of their preliminary mechanism of action
The synthesis of ursolic acid derivatives with cytotoxic activity and the investigation of their preliminary mechanism of action
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DOI：
10.1016/j.bmc.2008.11.036
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发表时间：
2009-01-15
影响因子：
3.5
通讯作者：
Wang, Yi-Zheng
中科院分区：
文献类型：
--
作者：
Meng, Yan-Qiu;Liu, Dan;Wang, Yi-Zheng
合成了19个在C-3和C-28位进行修饰的熊果酸衍生物（15个新化合物）。采用MTT法评价了衍生物对HeLa、BGC-823和SKOV 3细胞的细胞毒活性。用流式细胞仪和DNA片段化技术检测了衍生物对HeLa细胞的凋亡诱导作用和对细胞周期分布的影响。化合物10 b和11 b通过诱导细胞凋亡和阻滞细胞周期进程而特别具有抑制HeLa细胞生长的活性。细胞出现典型的“亚G1峰”和DNA梯状条带，细胞周期阻滞于S期，并呈剂量依赖性。(C)2008爱思唯尔有限公司保留所有权利。
Nineteen ursolic acid derivatives (15 novel compounds) modified at the C-3 and the C-28 positions were synthesized. The cytotoxic activity of the derivatives was evaluated against HeLa, BGC-823 and SKOV3 cells by MTT assay. Inducing apoptosis and affecting cell cycle distribution by the derivatives in HeLa cells were assessed by flow cytometry and DNA fragmentation. Compounds 10b and 11b were particularly active to inhibit HeLa cells growth through inducing apoptosis and arresting cell cycle progression. The typical 'sub-G1 peak' and DNA ladder formation were checked and cell cycle was arrested at the S phase in a dose-dependent manner. (C) 2008 Elsevier Ltd. All rights reserved.