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Apigenin, a Partial Antagonist of the Estrogen Receptor (ER), Inhibits ER-Positive Breast Cancer Cell Proliferation

Thu Ha Pham1, Yann Le Page1, Frédéric Percevault1

  • 1Inserm, EHESP, Irset (Institut de Recherche en Santé, Environnement et Travail)-UMR_S1085, Rennes University, F-35000 Rennes, France.

International Journal of Molecular Sciences
|January 20, 2021
PubMed

Insights

Apigenin shows promise in treating endocrine therapy-resistant breast cancer (BC) by inhibiting the Akt/FOXM1 pathway. This natural compound effectively reduces proliferation in resistant BC cells, offering a potential new therapeutic strategy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Estrogen receptor (ER)-positive breast cancer (BC) often develops resistance to endocrine therapies.
  • Hyperactivation of the Akt signaling pathway is a key mechanism contributing to this endocrine resistance.
  • Apigenin (Api), a plant-derived flavone, has demonstrated anti-cancer properties.

Purpose of the Study:

  • To investigate the therapeutic potential of Apigenin (Api) in ER-positive, endocrine therapy-resistant breast cancer (BC).
  • To evaluate Api's effects on a resistant BC cell model with hyperactivated Akt signaling.

Main Methods:

  • Developed a resistant breast cancer cell line (MCF-7/Akt) by overexpressing constitutively active Akt.
  • Assessed the antiproliferative effects of Apigenin (Api) on MCF-7/Akt cells.
  • Investigated Api's impact on cell cycle progression, apoptosis, and the Akt/FOXM1 signaling pathway.

Main Results:

  • Apigenin (Api) demonstrated significant antiproliferative effects on the endocrine-resistant MCF-7/Akt cells.
  • Api induced G2/M phase cell cycle arrest and apoptosis, counteracting estradiol's proliferative effect.
  • Api inhibited the Akt/FOXM1 pathway by reducing FOXM1 expression and altering downstream gene expression.

Conclusions:

  • Apigenin (Api) exhibits therapeutic potential against endocrine therapy-resistant breast cancer (BC).
  • Api's mechanism involves inhibiting the Akt/FOXM1 pathway and modulating cell cycle-related genes.
  • These findings support further investigation of Apigenin as a treatment for resistant BC.
Keywords:
AktERFOXM1apigeninbreast cancerendocrine resistancephytochemicals

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