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Bioorg Med Chem. 2011 Oct 1;19(19):5776-81. doi: 10.1016/j.bmc.2011.08.030. Epub 2011 Aug 22.

Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle.

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1
School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

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.

PMID:
21893415
DOI:
10.1016/j.bmc.2011.08.030
[Indexed for MEDLINE]

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