Department of Nutrition and Dietetics, Boshell Diabetes and Metabolic Diseases Research Program, Auburn University, Auburn, AL 36849.
U.S. Department of Agriculture, Agricultural Research Service, Natural Products Utilization Research Unit, P.O. Box 1848, University, MS 38677.
J Nutr Biochem. 2017 Sep;47:86-93. doi: 10.1016/j.jnutbio.2017.05.008. Epub 2017 May 25.
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 3-13 μg/ml), piceatannol and resveratrol inhibited mammalian α-glucosidase to a lesser extent (IC 14-84 and 111-120 μg/ml, respectively). 3'-Hydroxypterostilbene (IC 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.
膳食多酚已被证明能抑制α-葡萄糖苷酶，这种酶是一些抗糖尿病药物的作用靶点。白藜芦醇是一种存在于葡萄和葡萄酒中的多酚，已被报道能抑制酵母α-葡萄糖苷酶的活性。这激发了我们合成类似物并确定它们对哺乳动物α-葡萄糖苷酶活性的影响的兴趣。使用蔗糖或麦芽糖作为底物时，白藜芦醇、白皮杉醇和 3'-羟基紫檀芪对哺乳动物α-葡萄糖苷酶活性表现出强烈的抑制作用；松脂素、顺式去氧续随子素和反式去氧续随子素具有中等抑制作用。与阿卡波糖（IC 3-13 μg/ml）相比，白藜芦醇和白皮杉醇对哺乳动物α-葡萄糖苷酶的抑制作用较小（IC 14-84 和 111-120 μg/ml）。3'-羟基紫檀芪（IC 105-302 μg/ml）的效力比阿卡波糖低 23-35 倍。我们研究了白藜芦醇和白皮杉醇对高脂肪喂养的 C57Bl/6 小鼠餐后血糖反应的影响。动物在给予蔗糖或淀粉负荷前 60 分钟给予白藜芦醇（30 mg/kg 体重）或白皮杉醇（14 mg/kg BW），导致碳水化合物吸收延迟，餐后血糖浓度显著降低，与抗糖尿病药物阿卡波糖相似，而葡萄糖负荷动物则没有观察到显著影响。我们的研究表明，膳食多酚白藜芦醇和白皮杉醇可降低餐后高血糖，并表明抑制肠道α-葡萄糖苷酶活性可能是其抗糖尿病特性的潜在机制。
