AMP-activated protein kinase (AMPK) activators from Myristica fragrans (nutmeg) and their anti-obesity effect

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• 作者：Phi Hung Nguyen ; Thi Van Thu Le ; Hu Won Kang ; Jooyoung Chae ; Sang Kyum Kim ; Kwang-iI Kwon ; Dae Bang Seo ; Sang Jun Lee ; Won Keun Oh
• 关键词：Myristica fragrans ; Myristicaceae ; Tetrahydrofuran lignans ; AMP-activated protein kinase (AMPK)
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 July 2010
• 年：2010
• 卷：20
• 期：14
• 页码：4128-4131
• 全文大小：326 K

文摘

AMP-activated protein kinase (AMPK) is a potential therapeutic target for the treatment of metabolic syndrome including obesity and type-2 diabetes. As part of an ongoing search for new AMPK activators from plants, this study found that the total extract of Myristica fragrans (nutmeg) activated the AMPK enzyme in differentiated C2C12 cells. As active constituents, seven 2,5-bis-aryl-3,4-dimethyltetrahydrofuran lignans, tetrahydrofuroguaiacin B (1), saucernetindiol (2), verrucosin (3), nectandrin B (4), nectandrin A (5), fragransin C₁ (6), and galbacin (7) were isolated from this extract. Among the isolates, compounds 1, 4, and 5 at 5 μM produced strong AMPK stimulation in differentiated C2C12 cells. In addition, the preventive effect of a tetrahydrofuran mixture (THF) on weight gain in a diet-induced animal model was further examined. These results suggest that nutmeg and its active constituents can be used not only for the development of agents to treat obesity and possibly type-2 diabetes but may also be beneficial for other metabolic disorders.