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Aryl hydrocarbon receptor activation by aminoflavone: new molecular target for renal cancer treatment

Mariana A Callero1, Guadalupe V Suárez, Gabriela Luzzani

  • 1Research Area, Institute of Oncology Ángel H Roffo, University of Buenos Aires, Ciudad de Buenos Aires, Argentina.

International Journal of Oncology
|April 10, 2012
PubMed

Insights

Aminoflavone (AF) exhibits anticancer effects in renal cancer cells by activating the aryl hydrocarbon receptor (AhR). AhR translocation serves as a potential biomarker for AF sensitivity in various renal tumor types.

Area of Science:

  • Pharmacology and Toxicology
  • Oncology
  • Molecular Biology

Background:

  • Aminoflavone (AF) is an investigational anticancer drug demonstrating antiproliferative activity.
  • AF's mechanism involves the aryl hydrocarbon receptor (AhR) and shows promise in renal cancer models.
  • CYP1A1 induction and apoptosis are observed in AF-sensitive renal cells.

Purpose of the Study:

  • To investigate the role of the aryl hydrocarbon receptor (AhR) in mediating the antiproliferative effects of Aminoflavone (AF) in human renal cancer cells.
  • To assess AF's cytotoxicity and apoptosis-inducing potential in various human renal cell lines.
  • To evaluate AhR activation as a predictive marker for AF response.

Main Methods:

  • Cytotoxicity was assessed using MTS assays with and without an AhR inhibitor.
  • AhR nuclear translocation was measured via Western blotting and luciferase reporter assays.
  • Apoptosis was evaluated using specific staining and by quantifying key apoptotic markers (p-P53, P21, caspase 3, PARP cleavage).

Main Results:

  • AF inhibited growth in TK-10, Caki-1, SN12-C, and A498 renal cells, but not ACHN cells.
  • The antiproliferative effect was abolished by an AhR antagonist (α-naphthoflavone) in sensitive cell lines.
  • AF induced apoptosis and AhR nuclear translocation in sensitive renal cancer cells and a papillary tumor cell strain.

Conclusions:

  • The aryl hydrocarbon receptor (AhR) plays a crucial role in Aminoflavone's (AF) antiproliferative and apoptosis-inducing effects in renal cancer.
  • AhR activation and nuclear translocation are key events in AF-sensitive renal cancer cells.
  • AhR translocation can serve as a predictive biomarker for AF sensitivity across different renal tumor histologies in clinical trials.

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