Anthraquinones from Morinda longissima and their insulin mimetic activities via AMP-activated protein kinase (AMPK) activation

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• 作者：Phi-Hung Nguyen^a ; ¹ ; Hong Seok Choi^a ; Thi Kim Quy Ha^b ; Ji Yeon Seo^b ; Jun-Li Yang^b ; Da-Woon Jung^c ; Darren R. Williams^c ; Won-Keun Oh^b ; ^{wkoh1@snu.ac.kr}
• 关键词：Morinda longissima ; Anthraquinone ; AMP-activated protein kinase (AMPK) ; Glucose uptake
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：40-44
• 全文大小：969 K
• 卷排序：27

文摘

AMP-activated protein kinase (AMPK) activators are known to increase energy metabolism and to reduce body weight, as well as to improve glucose uptake. During for searching AMPK activators, a new anthraquinone, modasima A (10), along with eighteen known analogues (1–9 and 11–19) were isolated from an ethanol extract of the roots of Morinda longissima Y. Z. Ruan (Rubiaceae). Using the fluorescent tagged glucose analogues, 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxy-D-glucose (2-NBDG), insulin mimetics were screened with compounds 1–19 in 3T3-L1 adipocytes. Among them, compounds 2, 8 and 10 enhanced significantly glucose uptake into adipocytes and up-regulated the phosphorylated AMPK (Thr172) whereas the glucose uptake enhancing activities of compounds 2, 8 and 10 were abrogated by treatment of compound C, an AMPK inhibitor. Taken together, these anthraquinones showed the potential action as insulin mimetic to improve glucose uptake via activation of AMPK.