Chalcones and their therapeutic targets for the management of diabetes: structural and pharmacological perspectives

Eur J Med Chem. 2015 Mar 6:92:839-65. doi: 10.1016/j.ejmech.2015.01.051. Epub 2015 Jan 26.

Abstract

Diabetes Mellitus (DM) is the fastest growing metabolic disorder affecting about 387 million people across the globe and is estimated to affect 592 million people by year 2030. The search for newer anti-diabetic agents is the foremost need to control the accelerating diabetic population. Several natural and (semi) synthetic chalcones deserve the credit of being potential candidates that act by modulating the therapeutic targets PPAR-γ, DPP-4, α-glucosidase, PTP1B, aldose reductase, and stimulate insulin secretion and tissue sensitivity. In this review, a comprehensive study (from January 1977 to October 2014) of anti-diabetic chalcones, their molecular targets, structure activity relationships (SARs), mechanism of actions (MOAs) and patents have been described. The compounds which showed promising activity and have a well-defined MOAs, SARs must be considered as prototype for the design and development of potential anti-diabetic agents. They should be evaluated critically at all clinical stages to ensure their therapeutic and toxicological profile to meet the demand of diabetics.

Keywords: Chalcone; DPP-4; Diabetes; PPAR-γ; PTP1B; α-Glucosidase.

Publication types

  • Review

MeSH terms

  • Chalcones / chemistry
  • Chalcones / therapeutic use*
  • Diabetes Mellitus / drug therapy*
  • Diabetes Mellitus / metabolism
  • Glycoside Hydrolase Inhibitors / chemistry
  • Glycoside Hydrolase Inhibitors / pharmacology*
  • Humans
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / therapeutic use*
  • Molecular Structure
  • Structure-Activity Relationship
  • alpha-Glucosidases / metabolism

Substances

  • Chalcones
  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • alpha-Glucosidases