Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist

FASEB J. 2017 Jun;31(6):2603-2611. doi: 10.1096/fj.201601339R. Epub 2017 Mar 7.


The physiologic properties of glucagon-like peptide 1 (GLP-1) make it a potent candidate drug target in the treatment of type 2 diabetes mellitus (T2DM). GLP-1 is capable of regulating the blood glucose level by insulin secretion after administration of oral glucose. The advantages of GLP-1 for the avoidance of hypoglycemia and the control of body weight are attractive despite its poor stability. The clinical efficacies of long-acting GLP-1 derivatives strongly support discovery pursuits aimed at identifying and developing orally active, small-molecule GLP-1 receptor (GLP-1R) agonists. The purpose of this study was to identify and characterize a novel oral agonist of GLP-1R (i.e., myricetin). The insulinotropic characterization of myricetin was performed in isolated islets and in Wistar rats. Long-term oral administration of myricetin demonstrated glucoregulatory activity. The data in this study suggest that myricetin might be a potential drug candidate for the treatment of T2DM as a GLP-1R agonist. Further structural modifications on myricetin might improve its pharmacology and pharmacokinetics.-Li, Y., Zheng, X., Yi, X., Liu, C., Kong, D., Zhang, J., Gong, M. Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist.

Keywords: GLP-1 receptor; glucose tolerance test; insulin secretagogue; oral agonist.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids
  • Animals
  • Blood Glucose / metabolism
  • Chromium
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Flavonoids / pharmacology*
  • Glucagon-Like Peptide-1 Receptor / agonists*
  • Humans
  • Insulin / metabolism*
  • Islets of Langerhans / drug effects*
  • Islets of Langerhans / metabolism
  • Male
  • Mice
  • Mice, Knockout
  • Nicotinic Acids
  • Rats, Wistar
  • Rats, Zucker


  • Amino Acids
  • Blood Glucose
  • Flavonoids
  • Glucagon-Like Peptide-1 Receptor
  • Insulin
  • Nicotinic Acids
  • glucose tolerance factor
  • Chromium
  • myricetin