Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis

被引:43
作者
Lee, WS
Lee, DW
Baek, YI
An, SJ
Cho, KH
Choi, YK
Kim, HC
Park, HY
Bae, KH
Jeong, TS
机构
[1] Korea Res Inst Biosci & Biotechnol, Taejon 305333, South Korea
[2] Insect Biotech Co, Taejon 305811, South Korea
[3] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea
关键词
hACAT-1 and hACAT-2; inhibitor; lignans; S; chinensis; hypocholesterolemic activity;
D O I
10.1016/j.bmcl.2004.04.023
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The sesquineolignan, saucerneol B (1), and dineolignans, manassantin A (2), and manassantin B (3), were isolated from the methanol extracts of Saururus chinensis root and elucidated by their spectroscopic data analysis. Compounds 1-3 inhibited hACAT-1 and hACAT-2 with IC50 values of 43.0 and 124.0 muM for 1, of 39.0 and 8.0 muM for 2, of 82.0 muM and only 32% inhibition at 1 mM for 3, respectively. The EtOAc-soluble fraction, which contained compounds 1-3, of methanol extracts of S. chinensis exhibited strong cholesterol-lowering effect in high cholesterol-fed mice. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3109 / 3112
页数:4
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