Immunopharmacological Activity of Betulin in Inflammation-associated Carcinogenesis

Anticancer Agents Med Chem. 2018;18(5):645-651. doi: 10.2174/1871520617666171012124820.


This review highlights the multiple properties of the birch bark-derived pentacyclic triterpene betulin with special focus on its pharmacological activity in cancer and inflammation. While less well characterized compared to its hydrophilic derivative, betulinic acid, it exhibits potent anticancer activity described in many publications. Indeed, underinvestigated are its immunomodulatory functions in inflammatory diseases that appeared to enhance innate immune cell activities in an adjuvant-like fashion towards an interleukin-12 driven antitumor immunity. Herein, we like to emphasize the simultaneous and dual function of betulin on the basis of recent investigations of the tumor microenvironment and enlighten the potential use of betulin in the control of inflammation-associated carcinogenesis.

Keywords: Pentacyclic triterpene; betulin; cytostatic; dendritic cell; immunomodulation; inflammation-associated carcinogenesis..

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Carcinogenesis / drug effects*
  • Carcinogenesis / metabolism
  • Humans
  • Immunomodulation
  • Inflammation / drug therapy*
  • Inflammation / metabolism
  • Triterpenes / chemistry
  • Triterpenes / pharmacology*
  • Tumor Microenvironment / drug effects


  • Antineoplastic Agents
  • Triterpenes
  • betulin