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Differential Methylation and Acetylation as the Epigenetic Basis of Resveratrol’s Anticancer Activity

College of Basic Sciences, King Faisal University, Hofuf 400-Al Ahsa-31982, Saudi Arabia
Department of Medical Laboratory Technology, Faculty of Applied Medical Sciences, University of Tabuk, P.O. Box 741, Tabuk 71491, Saudi Arabia
Department of Psychiatry, University Hospital Limerick, Limerick V94 T9PX, Ireland
Institute of Biomedical and Genetic Engineering (IBGE), Islamabad 44000, Pakistan
Department of Postgraduate Education and Research, Kazakhstan Medical University KSPH, Almaty 050004, Kazakhstan
Organic Chemistry Laboratory, Department of Chemistry, University of Bayreuth, Universitaetsstrasse 30, 95447 Bayreuth, Germany
Department of Oncologic Sciences, Mitchell Cancer Institute, University of South Alabama, Mobile, AL 36604, USA
Author to whom correspondence should be addressed.
Medicines 2019, 6(1), 24;
Received: 11 January 2019 / Revised: 10 February 2019 / Accepted: 11 February 2019 / Published: 13 February 2019
(This article belongs to the Special Issue Natural Compounds as New Cancer Treatments)
PDF [685 KB, uploaded 13 February 2019]


Numerous studies support the potent anticancer activity of resveratrol and its regulation of key oncogenic signaling pathways. Additionally, the activation of sirtuin 1, a deacetylase, by resveratrol has been known for many years, making resveratrol perhaps one of the earliest nutraceuticals with associated epigenetic activity. Such epigenetic regulation by resveratrol, and the mechanism thereof, has attracted much attention in the past decade. Focusing on methylation and acetylation, the two classical epigenetic regulations, we showcase the potential of resveratrol as an effective anticancer agent by virtue of its ability to induce differential epigenetic changes. We discuss the de-repression of tumor suppressors such as BRCA-1, nuclear factor erythroid 2-related factor 2 (NRF2) and Ras Associated Domain family-1α (RASSF-1α) by methylation, PAX1 by acetylation and the phosphatase and tensin homologue (PTEN) by both methylation and acetylation, in addition to the epigenetic regulation of oncogenic NF-κB and STAT3 signaling by resveratrol. Further, we evaluate the literature supporting the potentiation of HDAC inhibitors and the inhibition of DNMTs by resveratrol in different human cancers. This discussion underlines a robust epigenetic activity of resveratrol that warrants further evaluation, particularly in clinical settings. View Full-Text
Keywords: resveratrol; epigenetic; methylation; acetylation resveratrol; epigenetic; methylation; acetylation

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Farhan, M.; Ullah, M.F.; Faisal, M.; Farooqi, A.A.; Sabitaliyevich, U.Y.; Biersack, B.; Ahmad, A. Differential Methylation and Acetylation as the Epigenetic Basis of Resveratrol’s Anticancer Activity. Medicines 2019, 6, 24.

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