Acyl-CoA: Cholesterol acyltransferase inhibitors from flex macropoda

被引:9
作者
Im, KR
Jeong, TS
Kwon, BM
Baek, NI
Kim, SH
Kim, DK [1 ]
机构
[1] Woosuk Univ, Coll Pharm, Samrye 565701, South Korea
[2] Korea Res Inst Biosci & Biotechnol, Taejon 305333, South Korea
[3] Kyung Hee Univ, Grad Sch Biotechnol, Suwon 449701, South Korea
[4] Kyung Hee Univ, Plant Metab Res Ctr, Suwon 449701, South Korea
[5] Kyung Hee Univ, Grad Sch EW Med Sci, Suwon 449701, South Korea
关键词
Ilex macropoda; ACAT inhibitory activity; Lupeol; Betulin;
D O I
10.1007/BF02969391
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Twigs from flex macropoda were extracted with MeOH, and the concentrated extracts were partitioned with CH2Cl2, EtOAc, n-BuOH, and H2O. Repeated column chromatography of the CH2Cl2 fraction ultimately resulted in the isolation of two compounds, via activity-guided fractionation, using ACAT inhibitory activity measurements. According to the physico-chemical data, the chemical structures of these isolated compounds were identified as lupeol (1) and betulin (2). Compounds 1 and 2 were shown to inhibit the activity of hACAT-1 and hACAT-2 in a dose-dependent manner, and compounds 1 and 2 inhibited hACAT-1 with IC50 values of 48 and 83 mu M, respectively.
引用
收藏
页码:191 / 194
页数:4
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