New Trends in the Pharmacological Intervention of PPARs in Obesity: Role of Natural and Synthetic Compounds

Curr Med Chem. 2021;28(20):4004-4022. doi: 10.2174/1570162X18666201123114934.

Abstract

Obesity is a major health concern for a growing fraction of the population, as its prevalence and related metabolic disorders are not fully understood. Over the last decade, many attempts have been undertaken to understand the mechanisms at the basis of this condition, in which the accumulation of fat occurring in adipose tissue leads to the pathogenesis of obesity- related disorders. Among the most recent studies, those on Peroxisome Proliferator Activated Receptors (PPARs) revealed that these nuclear receptor proteins acting as transcription factors, among others, regulate the expression of genes involved in energy, lipid, and glucose metabolisms, and chronic inflammation. The three different isotypes of PPARs, with different tissue expression and ligand binding specificity, exert similar or overlapping functions directly or indirectly linked to obesity. In this study, we reviewed the available scientific reports concerning the PPARs structure and functions, especially in obesity, considering both natural and synthetic ligands and their role in the therapy of obesity and obesity-associated disorders. On the whole, the collected data suggest that there are both natural and synthetic compounds that show beneficial and promising activity as PPAR agonists in chronic diseases related to obesity.

Keywords: Cardiovascular; Endogenous and exogenous ligands; Natural and synthetic agonists; Obesity; PPAR; Peroxisome proliferator–activated receptors; natural remedy for obesity..

Publication types

  • Review

MeSH terms

  • Humans
  • Ligands
  • Obesity* / drug therapy
  • Peroxisome Proliferator-Activated Receptors*
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors

Substances

  • Ligands
  • Peroxisome Proliferator-Activated Receptors
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors