Pharmacological Potential of Betulin as a Multitarget Compound

Biomolecules. 2023 Jul 12;13(7):1105. doi: 10.3390/biom13071105.

Abstract

Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways. Given its potential to influence diverse biological networks with high target specificity, it can be hypothesized that betulin may eventually become a new lead for drug development because it can modify a variety of pharmacological targets. The summarized research revealed that the diverse beneficial effects of betulin in various diseases can be attributed, at least in part, to its multitarget anti-inflammatory activity. This review focuses on the natural sources, pharmacokinetics, pharmacological activity of betulin, and the multi-target effects of betulin on signaling pathways such as MAPK, NF-κB, and Nrf2, which are important regulators of the response to oxidative stress and inflammation in the body.

Keywords: anti-inflammatory; betulin; hepatoprotective; inflammation; natural products (MAPK, Nrf2, NFκB).

Publication types

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

MeSH terms

  • Betulinic Acid
  • Cytokines / metabolism
  • Humans
  • Inflammation / drug therapy
  • NF-kappa B / metabolism
  • Triterpenes* / pharmacology

Substances

  • betulin
  • Triterpenes
  • Betulinic Acid
  • Cytokines
  • NF-kappa B

Grants and funding

This research was funded by the Ministry of Science and Higher Education of the Russian Federation MEGAGRANT, contract No 075-15-2022-1118, 29 June 2022.