Celastrol in metabolic diseases: Progress and application prospects

Pharmacol Res. 2021 May:167:105572. doi: 10.1016/j.phrs.2021.105572. Epub 2021 Mar 20.

Abstract

Metabolic diseases are becoming increasingly common in modern society. Therefore, it is essential to develop effective drugs or new treatments for metabolic diseases. As an active ingredient derived from plants, celastrol has shown great potential in the treatment of a wide variety of metabolic diseases and received considerable attention in recent years. In reported studies, the anti-obesity effect of celastrol resulted from regulating leptin sensitivity, energy metabolism, inflammation, lipid metabolism and even gut microbiota. Celastrol reversed insulin resistance via multiple routes to protect against type 2 diabetes. Celastrol also showed effects on atherosclerosis, cholestasis and osteoporosis. Celastrol in treating metabolic diseases seem to be versatile and the targets or pathways were diverse. Here, we systematically review the mechanism of action, and the therapeutic properties of celastrol in various metabolic diseases and complications. Based on this review, potential research strategies might contribute to the celastrol's clinical application in the future.

Keywords: Application limitations; Celastrol; Celastrol (PubChem CID: 122724); Mechanisms; Metabolic diseases; Targets.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Energy Metabolism / drug effects
  • Humans
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Insulin Resistance
  • Lipid Metabolism / drug effects
  • Metabolic Diseases / drug therapy*
  • Metabolic Diseases / metabolism
  • Obesity / drug therapy
  • Obesity / metabolism
  • Pentacyclic Triterpenes / chemistry
  • Pentacyclic Triterpenes / pharmacology
  • Pentacyclic Triterpenes / therapeutic use*
  • Tripterygium / chemistry

Substances

  • Pentacyclic Triterpenes
  • celastrol