Selected compounds derived from Moutan Cortex stimulated glucose uptake and glycogen synthesis via AMPK activation in human HepG2 cells

• Published in: Journal of ethnopharmacology 2010-09, Vol.131 (2), p.417-424
• Main Authors: Ha, Do Thi, Trung, Trinh Nam, Hien, Tran Thi, Dao, Trong Tuan, Yim, Namhui, Ngoc, Tran Minh, Oh, Won Keun, Bae, KiHwan
• Format: Article
• Language: English
• Subjects: Acetophenones; Acetyl-CoA Carboxylase - antagonists & inhibitors; adenosine monophosphate; AMP-activated protein kinase; AMP-Activated Protein Kinases - metabolism; AMPK pathway; bark; biochemical pathways; Biological and medical sciences; carbohydrate metabolism; cultured cells; dosage; dose response; Dose-Response Relationship, Drug; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacology; endothelial cells; Endothelial Cells - drug effects; Endothelial Cells - metabolism; Endothelium, Vascular - drug effects; Endothelium, Vascular - metabolism; Fatty Acid Synthases - antagonists & inhibitors; General pharmacology; glucose; Glucose - metabolism; Glucose uptake; glycemic effect; glycogen; Glycogen - biosynthesis; Glycogen Synthase Kinase 3 - metabolism; Glycogen Synthase Kinase 3 beta; Glycogen synthesis; Hep G2 Cells; human cell lines; Humans; hypoglycemic agents; Hypoglycemic Agents - pharmacology; insulin resistance; liver; Liver - drug effects; Liver - metabolism; Medical sciences; medicinal plants; Monoterpenes; Moutan Cortex; Nitric Oxide Synthase Type III - metabolism; Paeonia - chemistry; Paeonia suffruticosa; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Phosphorylation; phytochemicals; Plant Bark; Plant Roots; protein kinases; protein phosphorylation; protein synthesis; roots; Type-2 diabetes; Umbilical Veins
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2010.07.010

To evaluate the effect of selected compounds derived from Moutan Cortex on glucose uptake and glycogen synthesis associated with AMPK activation in insulin-resistant human HepG2 cell. The effect of isolated compounds ( 1– 16) on glucose uptake and glycogen synthesis was performed using HepG2 cells. The western blot was used to determine the expression of AMPK and its downstream substrates, ACC, p-ACC, and p-GSK-3β. The effects of the 16 compounds from Moutan Cortex on glucose metabolism in HepG2 cells under high glucose conditions were evaluated. Compounds 2, 3, and 6 displayed highly potent effects on the stimulation of glucose uptake and glycogen synthesis in human HepG2 cells under high glucose conditions. Compounds 2, 3, and 6 phosphorylate AMPK (AMP-activated protein kinase), and resulted in increased phosphorylation of GSK-3β and suppression of lipogenic expression (ACC and FAS) in a dose-dependent manner. Compounds 2, 3, and 6 also demonstrated interesting, strong eNOS phosphorylation in human umbilical vein endothelial cells (HUVECs). Compounds 1, 4, 5–12, and 14 displayed considerable effects on hepatic glucose production, AMPK activation, and phosphorylation of GSK-3β in HepG2 cells under high glucose conditions. These effects may indicate that the activation of AMPK by the active compounds from Moutan Cortex has considerable potential for reversing the metabolic abnormalities associated with type-2 diabetes.