Chemical modification of alisol B23-acetate and their cytotoxic activity

被引：12

作者：

Lee, S

Min, B

Bae, K ^{[1
]}

机构：

[1] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea

[2] Korea Res Inst Biosci & Biotechnol, Taejon 305600, South Korea

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2002年 / 25卷 / 05期

关键词：

Alismatis Rhizoma; protostane; cytotoxic activity;

D O I：

10.1007/BF02976929

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11beta,23S-dihydroxyprotost-13(17)-en-3-hy-droxy-imine (12) exhibited significant cytotoxic activities;against A549, SK-OV3, B16-F10, and HT1080 tumor cells with ED50 values of 10.0, 8.7, 5.2, and 3.1 mug/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11beta-hydroxyprotost-3-one(5), 13(17),24R(25)-diepoxy-11beta,23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11beta,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11beta, 23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against B16-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.

引用

页码：608 / 612

页数：5

共 6 条

[1] Effect of alisol B acetate, a plant triterpene, on apoptosis in vascular smooth muscle cells and lymphocytes [J].