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苯并呋喃和从安石榴中分离出的香豆素激活 AMP 激活的蛋白激酶(AMPK)。

AMP-activated protein kinase (AMPK) activation by benzofurans and coumestans isolated from Erythrina abyssinica.

机构信息

BK21 Project Team, College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, Republic of Korea.

出版信息

J Nat Prod. 2010 Apr 23;73(4):598-602. doi: 10.1021/np900745g.

Abstract

AMP-activated protein kinase (AMPK) has been proposed as a therapeutic target for the treatment of metabolic syndrome including obesity and type-2 diabetes. The bioassay-guided fractionation of an EtOAc-soluble extract of the stem bark of Erythrina abyssinica led to the isolation of a new coumestan, erythribyssin N (1), and two new benzofurans, erythribyssin F (2) and erythribyssin H (3), along with five known compounds (4-8). When tested for their stimulatory effects on AMPK activity at a concentration of 10 muM, compounds 4 and 5 showed potent activation, while compounds 1, 2, and 7 had moderate effects. These results suggest that benzofurans and coumestans may be new lead compounds for regulating the AMPK enzyme.

摘要

AMP 激活的蛋白激酶 (AMPK) 已被提议作为治疗代谢综合征(包括肥胖和 2 型糖尿病)的治疗靶点。从非洲紫檀茎皮的 EtOAc 可溶部分的生物活性指导分离得到一个新的香豆素,erythribysin N(1),以及两个新的苯并呋喃,erythribysin F(2)和 erythribysin H(3),以及五个已知的化合物(4-8)。当在 10 μM 浓度下测试它们对 AMPK 活性的刺激作用时,化合物 4 和 5 表现出很强的激活作用,而化合物 1、2 和 7 则具有中等作用。这些结果表明,苯并呋喃和香豆素可能是调节 AMPK 酶的新的先导化合物。

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