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Inhibition of Intestinal α-Glucosidases and Anti-Postprandial Hyperglycemic Effect of Grape Seed Extract

机译:葡萄籽提取物对肠道α-葡萄糖苷酶的抑制作用及抗餐后高血糖作用

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Because intestinal α-glucosidase plays a key role in carbohydrate digestion, its inhibition provides a therapeutic option for diabetes by suppressing postprandial blood glucose. We recently identified a grape seed extract (GSE) significantly inhibiting a-glucosidases. The inhibitory activity of GSE on yeast a-glucosidase was significantly stronger than that of acarbose. GSE also inhibited rat a-glucosidases in vitro in a dose- and time-dependent manner. The potential anti-diabetic effect of GSE was further evaluated in an animal model. Male 6 week-old C57BLK/6NCr mice were treated by streptozocin to induce diabetes. The results showed the oral intake of GSE (400mg/kg, body weight) suppressed postprandial blood glucose in STZ-induced diabetic mice. Oral administration of GSE reduced postprandial blood glucose in the diabetic mice by 11.5% and 16.6% at 30 and 60 min after the starch meal. Overall, GSE intake significantly reduced the incremental AUC_(0-120min)(area under postprandial glycemic curve) by 27.3% as compared to the control. Our results strongly suggest the potential of developing GSE, as a novel inhibitor of α-glucosidases, for diabetes prevention and treatment.
机译:由于肠道α-葡萄糖苷酶在碳水化合物的消化中起关键作用,因此其抑制作用可通过抑制餐后血糖为糖尿病提供治疗选择。我们最近确定了一种葡萄籽提取物(GSE),可显着抑制a-葡萄糖苷酶。 GSE对酵母α-葡萄糖苷酶的抑制活性明显强于阿卡波糖。 GSE在体外也以剂量和时间依赖性方式抑制大鼠α-葡萄糖苷酶。在动物模型中进一步评估了GSE的潜在抗糖尿病作用。用链佐星治疗雄性6周大的C57BLK / 6NCr小鼠,以诱导糖尿病。结果表明,口服摄入GSE(400mg / kg,体重)可抑制STZ诱导的糖尿病小鼠的餐后血糖。在淀粉餐后30和60分钟,口服GSE可将糖尿病小鼠的餐后血糖降低11.5%和16.6%。总体而言,与对照组相比,摄入GSE显着降低了AUC_(0-120min)的增量(餐后血糖曲线下的面积)27.3%。我们的结果有力地表明,开发GSE作为一种新型的α-葡萄糖苷酶抑制剂可用于糖尿病的预防和治疗。

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