Garcinol-A Natural Histone Acetyltransferase Inhibitor and New Anti-Cancer Epigenetic Drug

Int J Mol Sci. 2021 Mar 11;22(6):2828. doi: 10.3390/ijms22062828.

Abstract

Garcinol extracted from Garcinia indica fruit peel and leaves is a polyisoprenylated benzophenone. In traditional medicine it was used for its antioxidant and anti-inflammatory properties. Several studies have shown anti-cancer properties of garcinol in cancer cell lines and experimental animal models. Garcinol action in cancer cells is based on its antioxidant and anti-inflammatory properties, but also on its potency to inhibit histone acetyltransferases (HATs). Recent studies indicate that garcinol may also deregulate expression of miRNAs involved in tumour development and progression. This paper focuses on the latest research concerning garcinol as a HAT inhibitor and miRNA deregulator in the development and progression of various cancers. Garcinol may be considered as a candidate for next generation epigenetic drugs, but further studies are needed to establish the precise toxicity, dosages, routes of administration, and safety for patients.

Keywords: HAT inhibitors; cancer; epigenetic drugs; garcinol; miRNA.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Catalytic Domain
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Enzyme Inhibitors / pharmacology
  • Epigenesis, Genetic / drug effects*
  • Garcinia / chemistry
  • Gene Expression Regulation, Neoplastic
  • Histone Acetyltransferases / antagonists & inhibitors
  • Histone Acetyltransferases / genetics*
  • Histone Acetyltransferases / metabolism
  • Humans
  • MicroRNAs / antagonists & inhibitors
  • MicroRNAs / genetics*
  • MicroRNAs / metabolism
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Plant Extracts / chemistry
  • Terpenes / pharmacology*

Substances

  • Antineoplastic Agents, Phytogenic
  • Enzyme Inhibitors
  • MicroRNAs
  • Plant Extracts
  • Terpenes
  • Histone Acetyltransferases
  • garcinol