Antidiabetic activities of triterpenoids isolated from bitter melon associated with activation of the AMPK pathway

作     者：Tan, Min-Jia Ye, Ji-Ming Turner, Nigel Hohnen-Behrens, Cordula Ke, Chang-Qiang Tang, Chun-Ping Chen, Tong Weiss, Hans-Christoph Gesing, Ernst-Rudolf Rowland, Alex James, David E. Ye, Yang 

作者机构：Univ New S Wales Garvan Inst Med Res Diabet & Obes Res Program Sydney NSW 2010 Australia Chinese Acad Sci Shanghai Inst Biol Sci Shanghai Inst Mat Med State Key lab Drug Res Shanghai 201203 Peoples R China Bayer Ind Serv GmbH & Co D-51368 Leverkusen Germany Bayer CropSci AG R&D Ctr Agr D-40789 Monheim Germany 

出 版 物：《CHEMISTRY & BIOLOGY》 (化学与生物学)

年 卷 期：2008年第15卷第3期

页      面：263-273页

核心收录：

学科分类：0710[理学-生物学] 071010[理学-生物化学与分子生物学] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 

基　　金：Ministry of Science and Technology of China, (2004CB518902) National Health and Medical Research Council of Australia National Health and Medical Research Council, NHMRC, (481334) National Health and Medical Research Council, NHMRC National Natural Science Foundation of China, NSFC, (30770236) National Natural Science Foundation of China, NSFC 

主　　题：CHEMBIO SIGNALING 

摘      要：Four cucurbitane glycosides, momordicosides Q, R, S, and T, and stereochemistry-established karaviloside XI, were isolated from the vegetable bitter melon (Momordica charantia). These compounds and their aglycones exhibited a number of biologic effects beneficial to diabetes and obesity. In both L6 myotubes and 3T3-L1 adipocytes, they stimulated GLUT4 translocation to the cell membrane-an essential step for inducible glucose entry into cells. This was associated with increased activity of AM P-activated protein kinase (AMPK), a key pathway mediating glucose uptake and fatty acid oxidation. Furthermore, momordicoside(s) enhanced fatty acid oxidation and glucose disposal during glucose tolerance tests in both insulin-sensitive and insulin-resistant mice. These findings indicate that cucurbitane triterpenoids, the characteristic constituents of M. charantia, may provide leads as a class of therapeutics for diabetes and obesity.