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

页码：1245 / 1249

页数：5

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