Phytogenic Polyphenols as Glycogen Phosphorylase Inhibitors: The Potential of Triterpenes and Flavonoids for Glycaemic Control in Type 2 Diabetes

Curr Med Chem. 2017;24(4):384-403. doi: 10.2174/0929867324666161118122534.

Abstract

Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors of GP. These compounds have both pharmaceutical and nutraceutical potential for glycemic control in diabetes type 2. This review focuses mainly on the most successful (potent) of these compounds discovered to date. The protein-ligand interactions that form the structural basis of their potencies are discussed, highlighting the potential for exploitation of their scaffolds in the future design of new GP inhibitors.

Keywords: Alpha-glucosidases; antioxidants; diabetes; flavonoids; glycogen phosphorylase; pentacyclic triterpenes.

Publication types

  • Review

MeSH terms

  • Animals
  • Blood Glucose / metabolism*
  • Diabetes Mellitus, Type 2 / blood
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Glycogen Phosphorylase / antagonists & inhibitors*
  • Glycogen Phosphorylase / chemistry
  • Glycogen Phosphorylase / metabolism
  • Humans
  • Polyphenols / metabolism
  • Polyphenols / pharmacology*
  • Polyphenols / therapeutic use
  • Triterpenes / metabolism
  • Triterpenes / pharmacology*
  • Triterpenes / therapeutic use

Substances

  • Blood Glucose
  • Enzyme Inhibitors
  • Polyphenols
  • Triterpenes
  • Glycogen Phosphorylase