α-Glucosidase inhibitory effect of resveratrol and piceatannol
Abstract
Dietary polyphenols have been shown to inhibit α-glucosidase, an enzyme target of some antidiabetic drugs. Resveratrol, a polyphenol found in grapes and wine, has been reported to inhibit the activity of yeast α-glucosidase. This triggered our interest to synthesize analogs and determine their effect on mammalian α-glucosidase activity. Using either sucrose or maltose as substrate resveratrol, piceatannol and 3'-hydroxypterostilbene showed strong inhibition of mammalian α-glucosidase activity; pinostilbene, cis-desoxyrhapontigenin and trans-desoxyrhapontigenin had moderate inhibition. Compared to acarbose (IC 50 3-13 μg/ml), piceatannol and resveratrol inhibited mammalian α-glucosidase to a lesser extent (IC 50 14-84 and 111-120 μg/ml, respectively). 3'-Hydroxypterostilbene (IC 50 105-302 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 body weight [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 animals. Our studies demonstrate that the dietary polyphenols resveratrol and piceatannol lower postprandial hyperglycemia and indicate that inhibition of intestinal α-glucosidase activity may be a potential mechanism contributing to their antidiabetic property.
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Flavonoids may possess strong inhibitory activities on the intestinal alpha-glucosidase enzyme, delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic excursions.
“In addition to this, several in vitro studies have confirmed that flavonoids may possess strong inhibitory activities on the intestinal α-glucosidase enzyme that catalyzes the cleavage of glucose from disaccharides, thereby delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic excursions [61,62].”
From Mediterranean diet nutrients to turn the tide against insulin resistance and related diseases (2020) · cites this paper as [61]
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Mediterranean diet nutrients to turn the tide against insulin resistance and related diseases
Mirabelli, M., Chiefari, E., Arcidiacono, B., Corigliano, D. M., Brunetti, F. S., Maggisano, V., Russo, D., Foti, D. P., & Brunetti, A. (2020) · Nutrients · doi:10.3390/nu12041066 · Cited by 272 · see citing works
“In addition to this, several in vitro studies have confirmed that flavonoids may possess strong inhibitory activities on the intestinal α-glucosidase enzyme that catalyzes the cleavage of glucose from disaccharides, thereby delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic e…”
Background
- Authors
- Zhang, A. J., Rimando, A. M., Mizuno, C. S., & Mathews, S. T.
- Affiliations
- Auburn University (US)
- Agricultural Research Service (US)
- Corresponding author
- Mathews, Suresh T.
- Venue
- The Journal of Nutritional Biochemistry
- Publisher
- Elsevier BV
- Published
- 2017-09
- Volume
- 47
- Pages
- 86-93
- ISSN
- 0955-2863 (ISSN-L)
- OpenAlex
- W2618610934
- Cited by
- 99
- References
- 51
- Citations by year
- 2026: 9 · 2025: 10 · 2024: 15 · 2023: 3 · 2022: 13 · 2021: 12 · 2020: 15 · 2019: 13 · 2018: 7 · 2017: 2
- FWCI
- 7.99
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Journal of Nutritional Biochemistry (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
- Health Sciences › Medicine › Geriatrics and Gerontology › Sirtuins and Resveratrol in Medicine
- Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
- Keywords
- resveratrol, piceatannol, α-glucosidase inhibition, dietary polyphenols, postprandial hyperglycemia, antidiabetic activity, acarbose, sucrose loading
- MeSH terms
- Resveratrol, alpha-Glucosidases, Animals, Blood Glucose, Dietary Carbohydrates, Gastrointestinal Agents, Hyperglycemia, Hypoglycemic Agents, Intestinal Absorption, Kinetics, Mice, Inbred C57BL, Obesity, Random Allocation, Starch, Stilbenes, Dietary Sucrose, Postprandial Period, Acarbose, Rats, Diet, High-Fat, Glycoside Hydrolase Inhibitors
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