(+)-Pinoresinol is a putative hypoglycemic agent in defatted sesame (Sesamum indicum) seeds though inhibiting α-glucosidase

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5215-7. doi: 10.1016/j.bmcl.2012.06.068. Epub 2012 Jul 3.

Abstract

Defatted sesame seeds have been reported for hypoglycemic effect in mice and T2DM women. An attempted to identify active components responsible for this effect was conducted using α-glucosidase-guided fractionation, resulting in the isolation of various lignans. Of compounds isolated, only (+)-pinoresinol showed inhibitory activity against rat intestinal maltase with an IC(50) value of 34.3 μM. The kinetic study indicated that enzymatic hydrolysis of maltose is inhibited by (+)-pinoresinol through competitive and noncompetitive manners. However, a lower dissociation constant (k(i) 288 M) of EI complex suggested that competitive inhibition is predominant over noncompetitive mode (k'(i) 1342 M).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / therapeutic use
  • Female
  • Furans / chemistry*
  • Furans / isolation & purification
  • Furans / therapeutic use
  • Glycoside Hydrolase Inhibitors*
  • Humans
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / isolation & purification
  • Hypoglycemic Agents / therapeutic use
  • Intestines / enzymology
  • Kinetics
  • Lignans / chemistry*
  • Lignans / isolation & purification
  • Lignans / therapeutic use
  • Mice
  • Rats
  • Seeds / chemistry
  • Sesamum / chemistry*
  • Stereoisomerism
  • alpha-Glucosidases / metabolism

Substances

  • Enzyme Inhibitors
  • Furans
  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • Lignans
  • alpha-Glucosidases
  • pinoresinol