中科院上海藥物研究所科研人員與澳大利亞伽爾文(Garvan)醫(yī)學(xué)研究所合作,，從苦瓜中發(fā)現(xiàn)了數(shù)個具有治療糖尿病應(yīng)用前景的活性化合物成分,。雙方共同的研究結(jié)果發(fā)表在最新一期《細胞》出版社期刊《化學(xué)與生物學(xué)》（Chemistry & Biology）雜志上。
苦瓜作為中藥使用已有數(shù)百年歷史,。近代對苦瓜化學(xué)成分及其藥理活性的研究頗多,，但其中主要的降糖活性化學(xué)物質(zhì)及其作用機理一直未明確。中科院上海藥物研究所研究員葉陽課題組通過多年探索,，從苦瓜中分離和鑒定了一系列新的天然化學(xué)成分,，并與伽爾文研究所合作，在細胞和動物水平上首次明確了這些天然成分具有降低血糖的活性,?？茖W(xué)家推測這些化合物在細胞中是通過一條新型信號通路起作用的,，進一步發(fā)現(xiàn)這條信號通路將對發(fā)現(xiàn)研究治療糖尿病的新途徑和發(fā)明治療糖尿病新藥都是一件非常有意義的事情。
對化合物的降糖作用機制研究表明,，這些化合物能激活體內(nèi)與能量代謝相關(guān)的一個重要蛋白——單磷酸腺苷活化蛋白激酶(AMPK),。該蛋白具有調(diào)控人體能量代謝和促進葡萄糖攝取的作用。采取有效措施激活A(yù)MPK是2型糖尿病治療的一個重要途徑,。
據(jù)悉,，中科院上海藥物研究所和伽爾文研究所已簽署了合作協(xié)議，將對苦瓜的降糖治療作用進行深入全面評價和作用機制研究,。（來源：科學(xué)時報 黃辛）
生物谷推薦原始出處：
（Chemistry & Biology）,，Vol 15, 263-273, 21 March 2008，Min-Jia Tan, David E. James and Yang Ye
Antidiabetic Activities of Triterpenoids Isolated from Bitter Melon Associated with Activation of the AMPK Pathway
Min-Jia Tan,1,5 Ji-Ming Ye,2,5 Nigel Turner,2,5 Cordula Hohnen-Behrens,2 Chang-Qiang Ke,1 Chun-Ping Tang,1 Tong Chen,1 Hans-Christoph Weiss,3 Ernst-Rudolf Gesing,4 Alex Rowland,2 David E. James,2, and Yang Ye1,
1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China
2 Diabetes and Obesity Research Program, Garvan Institute of Medical Research, University of New South Wales, Sydney, NSW 2010, Australia
3 Bayer Industry Services GmbH & Co., Leverkusen 51368, Germany
4 Bayer CropScience AG, R & D, Agricultural Center, Monheim 40789, Germany
Summary
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 AMP-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.
