Phosphoenolpyruvate carboxykinase (PEPCK) is the key enzyme catalyzing the first step in hepatic gluconeogenesis. Insulin could repress PEPCK transcription, therefore lowering glucose production. Compounds that are able to repress PEPCK expression could constitute a new class of hypoglycemic agents. Polygonum multiflorum (PM) is a tonic and anti-aging agent in traditional Chinese medicine. We have demonstrated that PM crude extract has remarkable antidiabetic effect in a type 2 diabetic mice model. To search for the efficacious compounds in the extract responsible for this effect, we evaluated trans-stilbene glycoside (SG) which is the major active compound of PM, and cis-SG which could be induced from trans-SG with UV light, with PEPCK assay. We established the assay in HepG2 cell line and recorded changes in PEPCK gene expression with RT-PCR. Studies using inhibitors of specific subcellular biochemical pathways were performed to potentially elucidate a mode of action of the two compounds.

Cis-stilbene glycoside and trans-stilbene glycoside from Polygonum multiflorum suppress PEPCK gene expression and gluconeogenesis in HepG2 cell

244th National Meeting (2012)

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