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Ellagic acid inhibits EZH2: a potential epigenetic therapeutic molecule for cancer

Kirankumar Nalla1, Biji Chatterjee2, Jagadeesha Poyya3

  • 1Department of Plant Sciences, School of Life Sciences, University of Hyderabad, Central University PO, Gachibowli, Hyderabad Telangana 500046.

Cancer Genetics
|September 13, 2025
PubMed
Abstract

Insights

Ellagic acid (EA) effectively inhibits EZH2, a key epigenetic regulator in cancer. This natural compound shows promise for developing new breast cancer therapies by reducing tumor growth and promoting cell death.

Area of Science:

  • Epigenetics and Cancer Biology
  • Natural Product Chemistry
  • Drug Discovery

Background:

  • Epigenetic dysregulation, including aberrant DNA methylation and histone modifications, drives cancer initiation and progression.
  • EZH2 (Enhancer of Zeste homolog 2) mediated H3K27me3 modifications are crucial in altering gene expression for oncogenesis.
  • Targeting epigenetic modifiers like Polycomb Repressive Complex (PRC) components is a promising anti-cancer strategy.

Purpose of the Study:

  • To investigate the molecular interaction between ellagic acid (EA) and EZH2.
  • To evaluate the anti-cancer potential of EA by assessing its effects on cancer cell proliferation, apoptosis, and in vivo tumor growth.

Main Methods:

  • Molecular docking, Surface Plasmon Resonance, and molecular dynamic simulations were used to study EA-EZH2 interactions.
  • In vitro assays (methylation, MTT, EB/AO staining, cell cycle, apoptosis) assessed EA's effects on cancer cells.
  • In vivo mouse xenograft models evaluated EA's anti-tumor efficacy.

Main Results:

  • Ellagic acid (EA) demonstrated strong binding to EZH2's active site, confirmed by molecular docking and SPR studies (KD=3.28E-06).
  • EA inhibited EZH2 activity in vitro, reducing H3K27me3 levels and inducing cancer cell apoptosis and autophagy.
  • Oral administration of EA significantly reduced tumor size in mouse xenografts, decreasing proliferation marker Ki67 and repressive histone marks.

Conclusions:

  • Ellagic acid (EA) acts as a potent EZH2 inhibitor.
  • EA exhibits significant anti-cancer effects, including tumor growth inhibition and induction of cell death.
  • EA represents a potential therapeutic candidate for breast cancer treatment.
Keywords:
Breast cancerEZH2Ellagic acidEpidrugsH3K27me3Natural inhibitor

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