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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Flavonoids Influence Epigenetic-Modifying Enzyme Activity: Structure-Function Relationships and the Therapeutic Potential for Cancer

Author(s): E.R. Gilbert and D. Liu

Volume 17, Issue 17, 2010

Page: [1756 - 1768] Pages: 13

DOI: 10.2174/092986710791111161

Price: $65


Epigenetic modifications result in heritable changes in gene expression without changes to the DNA sequence. The most common forms of epigenetic regulation of gene expression are DNA methylation and histone acetylation or methylation, all of which are associated with chromatin remodeling. Results from recent studies suggest that epigenetic changes are some of the primary contributory factors of tumor-suppressor gene silencing in cancer cells. Compounds that target epigenetic regulators in the body may represent an attractive target for chemoprevention. Flavonoids are polyphenolic phytochemicals that exert a multitude of beneficial effects on human health. In recent years, isoflavones, flavonols and catechins have received much attention due to their ability to influence activity of chromatin-modifying enzymes. Epigallocatechin- 3-gallate, for example, was shown to inhibit activity of histone acetyltransferase and DNA methyltransferase. In this review, we will highlight the structure-function relationship between flavonoids and epigenetic modifications, with an emphasis on the isoflavones, flavonols and catechins, and their potential as anti-cancer agents in this regard.

Keywords: Catechins, DNA methylation, EGCG, epigenetics, flavonoids, genistein, histone, cancer

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