The fruit of Cnidium monnieri (L) Cusson is an important traditional medicine employed in
Taiwan and China as the treatments of impotence, sterilization, renal disease, dermatosis, colpitis, inflammation
and gynecological disease. Peroxisome Proliferator-activated Receptor γ (PPARγ) and Farnesoid X
receptor (FXR) are the members of nuclear receptor superfamily that have been targeted for developing
treatments for chronic liver diseases. In this study, the furocoumarins isolated from the fruit of Cnidium
monnieri (L) Cusson were evaluated for their PPARγ and FXR agonism. Indeed, in transient transfection
reporter assays, these furocoumarins transactivated PPARγ and FXR to respectively modulate promoter action
including ABCA1 and SHP promoters in dose-dependent manner. Through the molecular modeling docking studies these
furocoumarins were shown to bind to PPARγ or FXR ligand binding pocket fairly well. All these results indicate that Cnidium
monnieri (L) Cusson might possess therapeutic effects through the activation of PPARγ and FXR pathways.
Keywords: Farnesoid X receptor (FXR), furocoumarin, nuclear receptors, PEPCK, peroxisome proliferator-activated receptor γ
(PPARγ), transient transfection receptor assays.
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