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Inhibitory effects of 2'-nitroflavone and apigenin on EGFR signaling in breast cancer cells

Julieta R Cebrón1,2,3, Belén E Berin1,2, Mariana A Bojorge1,2

  • 1Departamento de Química Biológica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, C1113 AAD, Ciudad Autónoma de Buenos Aires, Argentina.

Scientific Reports
|July 17, 2026
PubMed

Insights

Flavonoids like 2'-nitroflavone and apigenin show anticancer effects in breast cancer cells by inhibiting epidermal growth factor receptor (EGFR) signaling. Combining 2'-nitroflavone with gefitinib enhances this effect synergistically.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Epidermal growth factor receptor (EGFR) is a key target in cancer therapy, often dysregulated in breast cancer.
  • Gefitinib, an EGFR tyrosine kinase inhibitor (TKI), is used for lung cancer and shows potential for breast cancer treatment.
  • Combining TKIs with other agents, like flavonoids, may improve efficacy and overcome drug resistance.

Purpose of the Study:

  • To evaluate the anticancer effects of apigenin and 2 itroflavone as monotherapy in breast cancer cells.
  • To investigate the impact of these flavonoids on EGFR signaling pathways.
  • To assess the synergistic potential of combining 2 itroflavone with gefitinib for breast cancer treatment.

Main Methods:

  • Monotherapy treatment of hormone-sensitive (MCF-7) and triple-negative (MDA-MB-231) breast cancer cells with apigenin and 2 itroflavone.
  • Assessment of cell growth inhibition and modulation of EGFR signaling.
  • Evaluation of combined therapy effects using combination index (CI) calculations and apoptosis assays.

Main Results:

  • Both apigenin and 2 itroflavone inhibited breast cancer cell growth and negatively modulated EGFR signaling.
  • 2 itroflavone demonstrated higher potency compared to apigenin.
  • Combined treatment of 2 itroflavone with gefitinib resulted in significantly enhanced cell growth inhibition and apoptosis, with synergistic interactions observed, particularly at lower concentrations.

Conclusions:

  • Apigenin and 2 itroflavone possess antitumor properties against breast cancer cells, partly through EGFR signaling inhibition.
  • The combination of 2 itroflavone with gefitinib exhibits a synergistic growth inhibitory effect.
  • These findings support further investigation of 2 itroflavone and apigenin in preclinical breast cancer models, especially in combination with gefitinib.
Keywords:
2′-NitroflavoneApigeninBreast cancerEGFRGefitinib

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