Stimulatory Effect of Puerarin on α_1A-Adrenoceptor to Increase Glucose Uptake into Cultured C₂C₁₂Cells of Mice

Abstract

Effects of puerarin, an active principle contained in the roots of Pueraria lobata (Leguminosae), on the regulation of glucose metabolism in an insulin deficient state were investigated in cultured myoblast C 2 C 12 cells using glucose uptake as indicator. Puerarin enhanced the uptake of radioactive glucose into C 2 C 12 cells in a concentration-dependent manner, which was abolished by prazosin pretreatment. Activation of alpha 1 -adrenoceptors by puerarin was further indicated by the displacement of [ 3H]prazosin binding in C 2 C 12 cells. The stimulatory action of puerarin on glucose uptake was also reduced in C 2 C 12 cells pre-incubated with the antagonists, both WB 4101 and RS 17 056, at concentrations sufficient to block alpha 1A -adrenoceptor (alpha 1A -AR). An activation of alpha 1A -AR seems responsible for the action of puerarin in C 2 C 12 cells. Pharmacological inhibition of phospholipase C (PLC) by U73312 resulted a concentration-dependent decrease of puerarin-stimulated glucose uptake in C 2 C 12 cells. This inhibition of glucose uptake by U73122 was specific because the inactive congener, U73343, failed to block puerarin-stimulated glucose uptake. Moreover, both chelerythrine and GF 109203X diminished the action of puerarin at concentration sufficient to inhibit protein kinase C (PKC). The obtained data suggest that an activation of alpha 1A -AR by puerarin in C 2 C 12 cells may increase the glucose uptake via the PLC-PKC pathway.

A Preadipocyte Differentiation Assay as a Method for Screening Potential Anti-Type II Diabetes Drugs from Herbal Extracts

“…We assayed the known drug rosiglitazone and 20 compounds extracted from Chinese herbs and successfully identified two non-cytotoxic compounds, puerarin and astragaloside IV. Puerarin has been reported to possess complex pharmacological effects related to diabetes [27], [28], and our results are in agreement with the previous findings. We examined the ability of puerarin and astragaloside IV to modulate glucose uptake and PPARg gene expression.…”

Acute Effect of High‐dose Isoflavones from Pueraria lobata (Willd.) Ohwi on Lipid and Bone Metabolism in Ovariectomized Mice

“…It contains a unique main isoflavone called puerarin (daidzein 8‐ C ‐glucoside), which shows potent antioxidant and hypolipidemic activities (Chung et al ., ). Many studies have shown various biological activities, such as hypocholesterolemic, antioxidative, hypoglycaemic (Hsu et al ., ; Chung et al ., ) and hypopigmentation effects. Pueraria lobata also contains genistein and daidzein, which are common isoflavones in soybeans (Guerra et al ., ).…”

The study of anti-metabolic syndrome effect of puerarin in vitro

“…Our study shows that, as rosiglitazone, puerarin dose-dependently potentiate the glucose-uptake of adipocytes, which have been induced insulin resistance by high glucose. Hsu et al reported that puerarin might increase the glucose uptake of C2C12 cell via activating alpha1- adrenoreceptor (Hsu et al, 2002). Our study shows a slow and dissimilar pharmacological action on adipocyte, which implies a new different mechanism with the variation of cell.…”