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Updated: Jun 14, 2025

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Differential Interactions of Flavonoids with the Aryl Hydrocarbon Receptor In Silico and Their Impact on Receptor

Monique Reis de Santana1, Ylanna Bonfim Dos Santos2, Késsia Souza Santos2

  • 1Laboratory of Neurochemistry and Cellular Biology, Institute of Health Sciences, Federal University of Bahia, Salvador 40231-300, Brazil.

Pharmaceuticals (Basel, Switzerland)
|August 29, 2024
PubMed

Insights

Flavonoids show potential anticancer effects by modulating the aryl hydrocarbon receptor (AHR). This study identified specific flavonoids that interact with AHR, offering new avenues for cancer therapy development.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The anticancer mechanisms of flavonoids are not fully understood.
  • The aryl hydrocarbon receptor (AHR) is implicated in cancer progression and is a potential therapeutic target.

Purpose of the Study:

  • To investigate the interaction of hydroxy flavonoids with the aryl hydrocarbon receptor (AHR).
  • To elucidate the molecular mechanisms of flavonoid anticancer activity.
  • To identify selective AHR modulators for potential cancer therapies.

Main Methods:

  • In silico molecular modeling of flavonoid binding to the AHR PAS-B domain.
  • In vitro EROD activity assays using MCF7 human breast cancer cells.
  • Dose-dependent inhibition assays of AHR activity in the presence of an agonist (TCDD).

Main Results:

  • Chrysin, apigenin, naringenin, and quercetin exhibited high AHR binding affinity in silico.
  • All tested flavonoids inhibited AHR activity in a dose-dependent manner in vitro.
  • Naringenin demonstrated novel antagonistic potential against AHR activity.

Conclusions:

  • Flavonoids possess distinct modulatory effects on AHR activity.
  • Understanding these molecular interactions is vital for developing novel flavonoid-based cancer treatments.
  • Naringenin emerges as a promising candidate for further investigation as an AHR modulator.
Keywords:
AHRTCDDantagonistcancer therapynaringeninpolyphenols

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