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ARS Home » Southeast Area » Oxford, Mississippi » Natural Products Utilization Research » Research » Publications at this Location » Publication #299391
Title: Alpha-glucosidase inhibitory effect of resveratrol and piceatannol

Author
item ZHANG, ALBERT J - Auburn University
item Rimando, Agnes
item MIZUNO, CASSIA - University Of New England
item MATHEWS, SURESH - University Of Auburn

Submitted to: Journal of Agricultural and Food Chemistry
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 5/16/2017
Publication Date: 5/25/2017
Publication URL: http://handle.nal.usda.gov/10113/5801785
Citation: Zhang, A., Rimando, A.M., Mizuno, C.S., Mathews, S.T. 2017. Alpha-glucosidase inhibitory effect of resveratrol and piceatannol. Journal of Agricultural and Food Chemistry. 47:86-93. doi:10.1016/j.jnutbio.2017.05.008.

Interpretive Summary: Resveratrol, a compound found in grapes and wine, has been previously reported to inhibit the activity of an enzyme (alpha-glucosidase) that is a target of some anti-diabetic drugs. Derivatives of resveratrol were synthesized, and tested for inhibition of mammalian alpha-glucosidase activity. Of all the compounds tested in vitro, resveratrol and piceatannol showed strong inhibition. Compared to acarbose, a clinically used drug, piceatannol and resveratrol inhibited mammalian a-glucosidase to a lesser extent. We investigated the effect of piceatannol and resveratrol on postprandial blood glucose response in mice. Animals administered resveratrol (30 mg/kg BW) or piceatannol (14 mg/kg BW) had a delayed absorption of carbohydrates, resulting in significant lowering of postprandial blood glucose concentrations, similar to the antidiabetic drug acarbose. Our studies demonstrate that the polyphenols resveratrol and piceatannol lower post-prandial hyperglycemia, and indicate that inhibition of intestinal a-glucosidase activity as a potential target for their anti-diabetic property.

Technical Abstract: Dietary polyphenols have been shown to inhibit a-glucosidase, an enzyme target of some anti-diabetic drugs. Resveratrol, a polyphenol found in grapes and wine, has been reported to inhibit the activity of yeast a-glucosidase. This triggered our interest to synthesize analogs and determine their effect on mammalian a-glucosidase activity. Using either sucrose or maltose as substrate, resveratrol, piceatannol and 3’-hydroxypterostilbene (0.5 mg/ml) showed strong inhibition of mammalian a-glucosidase activity; pinostilbene, cis- and trans-desoxyrhapontigenin had moderate inhibition. Compared to acarbose (IC50 3-13 µg/ml), piceatannol and resveratrol inhibited mammalian a-glucosidase to a lesser extent (IC50 14-84 and 111-120 µg/ml, respectively). 3’-Hydroxypterostilbene (IC50 105-302 µg/ml) was 23-35 fold less potent than acarbose. We investigated the effect of piceatannol and resveratrol on postprandial blood glucose response in high-fat fed C57Bl/6 mice. Animals administered resveratrol (30 mg/kg BW) or piceatannol (14 mg/kg BW) 60 min prior to sucrose- or starch-loading had a delayed absorption of carbohydrates, resulting in significant lowering of postprandial blood glucose concentrations, similar to the antidiabetic drug acarbose, while no significant effect was observed with the glucose-loaded animnals. Our studies demonstrate that the dietary polyphenols resveratrol and piceatannol lower post-prandial hyperglycemia and indicate that inhibition of intestinal a-glucosidase activity may be a potential mechanism contributing to their anti-diabetic property.