Grape skin extract inhibits mammalian intestinal α-glucosidase activity and suppresses postprandial glycemic response in streptozocin-treated mice

Intestinal alpha-glucosidases are the key enzymes responsible for starch digestion and absorption and their inhibition has been proven effective in both preventing and treating diabetes through improvement of postprandial hyperglycaemia. This study, for the first time, identified that a Norton grape skin extract (GSE) significantly inhibited mammalian intestinal alpha-glucosidases but not other digestive enzymes including structurally relevant pancreatic alpha-amylase. Norton GSE inhibited rat intestinal alpha-glucosidases through a competitive mode with an IC50 of 0.384 mg/ml. Further animal study revealed that the oral intake of Norton GSE (400 mg/kg) significantly reduced postprandial blood glucose by 30.9% in the streptozocin-treated male C57BL/6 J mice following starch challenge. These findings suggest that Norton GSE may have a unique property of suppressing postprandial blood glucose through a mechanism involving the inhibition of alpha-glucosidases, thereby providing a novel dietary opportunity for diabetes management. (C) 2010 Elsevier Ltd. All rights reserved.