Diacylglycerol acyltransferase-inhibitory compounds from Erythrina senegalensis

被引：20
|
作者：
Oh, Won Keun [1 ,4 ]
Lee, Chul- Ho [1 ,3 ]
Seo, Jee Hee [1 ,3 ]
Chung, Mi Yeon [1 ,3 ]
Cui, Long [1 ,3 ]
Fomum, Z. Tanee [1 ,5 ]
Kang, Jong Seong [1 ,6 ]
Lee, Hyun Sun [2 ,3 ]
机构：
[1] Korea Res Inst Bioscience & Biotechnol KRIBB, Nat Med Res Ctr, Taejon 305333, South Korea
[2] Korea Res Inst Bioscience & Biotechnol KRIBB, Mol Canc Res Ctr, Taejon 305333, South Korea
[3] KRIBB, Nat Med Res Ctr, Taejon 305333, South Korea
[4] Chosun Univ, Coll Pharm, Kwangju 501759, South Korea
[5] Univ Yaounde I, Fac Sci, Dept Organ Chem, Yaounde, Cameroon
[6] Chungnam Natl Univ, Coll Pharm, Taejon 305763, South Korea
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2009年 / 32卷 / 01期
关键词：
Erythrina senegalensis; Prenylflavonoid; Diacylglycerol acyltransferase; FLAVONOIDS; RESISTANCE; OBESITY; INSULIN;
D O I：
10.1007/s12272-009-1116-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT) is proposed to be a drug target for the treatment of obesity and type 2 diabetes. Bioassay-guided fractionation of the CH2Cl2-soluble extract of the stem bark of Erythrina senegalensis, using an in vitro DGAT enzyme assay, resulted in the isolation of eight known prenylflavonoids, 8-prenylleutone (1), auriculatin (2), erysenegalensein O (3), erysenegalensein D (4), erysenegalensein N (5), derrone (6), alpinumisoflavone (7), and 6,8-diprenylgenistein (8). Compounds 1, 2-4, 6, and 8 inhibited DGAT activity, with IC50 values ranging from 1.1 +/- 0.3 to 15.1 +/- 1.1 mu g/mL. On the basis of the data obtained, we propose isoflavonoids with isoprenyl groups as a novel class of DGAT inhibitors.
引用
收藏
页码：43 / 47
页数：5
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