熊果酸
化学
细胞毒性
赫拉
立体化学
二聚体
萜烯
细胞毒性T细胞
齐墩果酸
氨基酸
细胞凋亡
化学合成
生物活性
体外
IC50型
MTT法
细胞培养
生物化学
有机化学
色谱法
作者
Cui Ma,Shao‐Qing Cai,Jinshi Cui,Ruiqing Wang,Pengfei Tu,Masao Hattori,Mohsen Daneshtalab
标识
DOI:10.1016/j.ejmech.2005.01.001
摘要
Ursolic acid and 2alpha-hydroxyursolic acid isolated from apple peels were found to show growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela. Structural modifications were performed on the C-3, C-28 and C-11 positions of ursolic acid and the cytotoxicity of the derivatives was evaluated. The SAR revealed that the triterpenes possessing two hydrogen-bond forming groups (an H-donor and a carbonyl group) at positions 3 and 28 exhibit cytotoxic activity. The configuration at C-3 was found to be important for the activity. Introduction of an amino group increased the cytotoxicity greatly. A 3beta-amino derivative was 20 times more potent than the parent ursolic acid. The 28-aminoalkyl dimer compounds showed selective cytotoxicity.
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