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Diethylstilbestrol-scaffold-based pregnane X receptor modulators.

Žiga Hodnik1, Tihomir Tomašič1, Domen Smodiš1

  • 1University of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, Slovenia.

European Journal of Medicinal Chemistry
|September 27, 2015
PubMed
Summary

Researchers discovered new diethylstilbestrol compounds that modulate the pregnane X receptor (PXR), impacting drug metabolism. Some derivatives activate PXR, while others block its activity, offering potential for drug development.

Keywords:
DiethylstilbestrolMimeticPXR agonistPXR antagonistPregnane X receptorSolomonsterol

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Molecular Biology

Background:

  • The pregnane X receptor (PXR) is a key regulator of drug-metabolizing enzymes and transporters.
  • Understanding PXR modulation is crucial for optimizing drug efficacy and minimizing adverse effects.

Purpose of the Study:

  • To discover novel diethylstilbestrol-based modulators of the pregnane X receptor (PXR).
  • To investigate PXR agonistic and antagonistic activities of synthesized compounds derived from marine steroids and bazedoxifene scaffolds.

Main Methods:

  • Design and synthesis of diethylstilbestrol derivatives.
  • In vitro evaluation of PXR agonistic and antagonistic activities in HepG2 cells.
  • Assessment of PXR-regulated CYP3A4 expression levels.

Main Results:

  • Methylated diethylstilbestrol derivative 1 showed potent PXR agonistic activity (EC50 = 10.5 μM).
  • Diethylstilbestrol (2) and derivatives 3, 4, and 6 exhibited PXR antagonistic effects (IC50 for 6 = 27.4 μM, IC50 for 2 = 14.6 μM).
  • Compound 1 induced PXR-regulated CYP3A4 expression, while compounds 2 and 6 inhibited rifaximin-induced CYP3A4 up-regulation.

Conclusions:

  • Novel diethylstilbestrol derivatives effectively modulate PXR activity, acting as either agonists or antagonists.
  • These findings provide a basis for developing new therapeutic agents targeting PXR for drug metabolism regulation.