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.
Highlights
In H1299 lung cancer and endometrial cancer cell lines, garcinol application resulted in cell cycle arrest and a marked decrease in cyclin-dependent kinase 2 (CDK2) and cyclin-dependent kinase 4 (CDK4) expression [44,46]
This study showed that garcinol affects P300 and TGF-β1 pathways in oesophageal cancer cells [61]
Research confirms that P300/CREB-binding protein (CBP) and P300/CBP-associated factor (PCAF) may prove to be attractive targets of epigenetic therapies
Summary
The current definition of epigenetics is the study of heritable changes in gene expression that occur independently of changes in the original DNA sequence. Epigenetics plays an important role in the modulation of genetic diversity, such as phenotypic variation among genetically identical individuals [2,3]. Acetylation is one of the most important and most common post-translational modifications of proteins, which modulates transcription, chromatin structure, and DNA strand repair [6]. This highly dynamic process induces conformational changes to the nucleosome with consequent activation of transcription.
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