Synthesis, anti-proliferative and proapoptotic activity of novel oleanolic acid azaheterocyclic derivatives

被引：28
|
作者：
Kang, Xiao [2 ]
Hu, Jun [1 ]
Gao, Zhenbei [2 ]
Ju, Yong [1 ]
Xu, Chuanlian [2 ]
机构：
[1] Tsinghua Univ, Dept Chem, Minist Educ, Key Lab Bioorgan Phosphorus Chem & Chem Biol, Beijing 100084, Peoples R China
[2] Zhejiang Sci Tech Univ, Coll Life Sci, Lab Promet & Mol Enzymol, Hangzhou 310018, Peoples R China
来源：
MEDCHEMCOMM | 2012年 / 3卷 / 10期
关键词：
ANTI-HIV ACTIVITY; URSOLIC ACID; INHIBITION; TRITERPENOIDS; AGENTS; CELLS; RING;
D O I：
10.1039/c2md20051a
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Oleanolic acid (OA) derivatives with azaheterocyclic groups at the 2,3-positions of A ring were synthesized and their anti-proliferative effect and apoptosis induction abilities were determined in human hepatocellular carcinoma BEL-7404 cells. The results showed that compounds 4 and 5 with different azaheterocycle groups possessed better anti-proliferative activity than oleanolic acid. Meanwhile, their apoptosis induction and signal pathway were investigated which indicated that compound 4 significantly induced cell apoptosis through down-regulating Bcl-2 expression, up-regulating Bax expression, releasing cytochrome c and activating the caspase-3 pathway.
引用
收藏
页码：1245 / 1249
页数：5
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