title: Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle.
abstract: AMP-activated kinase (AMPK) as a key controller in the regulation of whole-body energy homeostasis, plays an important role in protecting the body from metabolic diseases. Recently, improved glucose, lipid utility and increased insulin sensitivity were observed on several diabetic rodent models treated with crude mogrosides isolated from the fruit of Siraitia grosvenorii Swingle, but the precise active compounds responsible for the anti-diabetic activity of this plant have not been clearly identified. In our current work, acid hydrolysis of crude mogrosides provided five new cucurbitane triterpenoids (1-4, 8), along with three known ones (5-7). The main aglycone mogrol (7) and compounds 4 and 8 were found to be potent AMPK activators in the HepG2 cell line. This result suggested AMPK activation by the mogroside aglycones 7 and 8 was proved to contribute at least partially to the anti-hyperglycemic and anti-lipidemic properties in vivo of S. grosvenorii.
authors: School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.
authors: Xu-bing
authors: XB
authors: Chen
authors: Jing-jing
authors: JJ
authors: Zhuang
authors: Jun-hua
authors: JH
authors: Liu
authors: Min
authors: M
authors: Lei
authors: Lei
authors: L
authors: Ma
authors: Jing
authors: J
authors: Chen
authors: Xu
authors: X
authors: Shen
authors: Li-hong
authors: LH
authors: Hu
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000737:chemistry* / Q000378:metabolism; D019662:Cucurbitaceae / Q000737:chemistry*; D004789:Enzyme Activation / Q000187:drug effects; D020536:Enzyme Activators / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry; D006027:Glycosides / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D020536:Enzyme Activators; D006027:Glycosides; D007004:Hypoglycemic Agents; D014315:Triterpenes; C514277:cucurbitane; D055372:AMP-Activated Protein Kinases