Inhibition of human salivary and pancreatic alpha-amylase by resveratrol oligomers.

Abstract

A key strategy to mitigate postprandial hyperglycemia involves inhibiting alpha-amylases, which commence the starch digestion process in the gut. This study examined the inhibitory effects of resveratrol and stilbenoid tetramers, vaticanol B, (-)-hopeaphenol, and vatalbinoside A on human salivary and pancreatic alpha-amylases experimentally and through molecular docking studies. Vaticanol B demonstrated the most potent inhibition with IC50 values of 5.3 +/- 0.3 muM for salivary and 6.1 +/- 0.5 muM for pancreatic alpha-amylase (compared to acarbose with IC50 values of 1.2 +/- 0.1 muM and 0.5 +/- 0.0 muM, respectively). Kinetic analysis suggested a competitive inhibition mode for vaticanol B. Resveratrol and vatalbinoside A were poor inhibitors of human alpha-amylases, while (-)-hopeaphenol exhibited moderate inhibition. Molecular docking supported the inhibition data, and several aspects of the structural configurations explained the stronger inhibition exerted by vaticanol B. Overall, vaticanol B shows promise as a natural alternative to acarbose for inhibiting alpha-amylase.Copyright © 2024 The Authors. Published by American Chemical Society.