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Updated: Jun 13, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Impact on DNA methylation in cancer prevention and therapy by bioactive dietary components
1Department of Biology, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
Abstract:
It is well established that aberrant gene regulation by epigenetic mechanisms can develop as a result of pathological processes such as cancer. Methylation of CpG islands is an important component of the epigenetic code and a number of genes become abnormally methylated during tumorigenesis. Some bioactive food components have been shown to have cancer inhibition activities by reducing DNA hypermethylation of key cancer-causing genes through their DNA methyltransferase (DNMT) inhibition properties. The dietary polyphenols, (-)-epigallocatechin- 3-gallate (EGCG) from green tea, genistein from soybean and possibly isothiocyanates from plant foods, are some examples of these bioactive food components modulated by epigenetic factors. The activity of cancer inhibition generated from dietary polyphenols is associated with gene reactivation through demethylation in the promoters of methylation-silenced genes such as p16INK4a and retinoic acid receptor beta. The effects of dietary polyphenols such as EGCG on DNMTs appear to have their direct inhibition by interaction with the catalytic site of the DNMT1 molecule, and may also influence methylation status indirectly through metabolic effects associated with energy metabolism. Therefore, reversal of hypermethylation-induced inactivation of key tumor suppression genes by dietary DNMT inhibitors could be an effective approach to cancer prevention and therapy. In this analysis, we focus on advances in understanding the effects of dietary polyphenols on DNA methylation modulation during the process of cancer development, which will offer exciting new opportunities to explore the role of diet in influencing the biology of cancer and to understand the susceptibility of the human epigenome to dietary effects.
Insights
Dietary polyphenols like EGCG can inhibit DNA methyltransferases (DNMTs), reversing cancer-promoting gene hypermethylation. This epigenetic modulation by bioactive food components offers a promising avenue for cancer prevention and therapy.
Area of Science:
- Epigenetics
- Nutritional Science
- Cancer Biology
Background:
- Aberrant gene regulation via epigenetic mechanisms, particularly DNA methylation, is a hallmark of cancer development.
- CpG island hypermethylation silences key tumor suppressor genes during tumorigenesis.
- Dietary bioactive compounds show potential in cancer inhibition by influencing epigenetic processes.
Purpose of the Study:
- To review the effects of dietary polyphenols on DNA methylation modulation in cancer.
- To explore the potential of dietary DNA methyltransferase (DNMT) inhibitors for cancer prevention and therapy.
Main Methods:
- Analysis of scientific literature on dietary polyphenols and their impact on DNA methylation.
- Focus on specific compounds like (-)-epigallocatechin-3-gallate (EGCG), genistein, and isothiocyanates.
- Examination of DNMT inhibition mechanisms and gene reactivation through demethylation.
Main Results:
- Dietary polyphenols, including EGCG, genistein, and isothiocyanates, can inhibit DNMTs, reducing aberrant DNA hypermethylation.
- These compounds promote gene reactivation by demethylating silenced tumor suppressor genes (e.g., p16INK4a, retinoic acid receptor beta).
- Polyphenols may inhibit DNMT1 directly or indirectly via metabolic effects.
Conclusions:
- Reversal of hypermethylation-induced gene silencing by dietary DNMT inhibitors is a viable strategy for cancer prevention and treatment.
- Understanding the interplay between diet and the epigenome opens new avenues for cancer research.
- Dietary interventions targeting epigenetic modifications hold significant promise for influencing cancer biology.
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