Sesamin: A Naturally Occurring Lignan Inhibits CYP3A4 by Antagonizing the Pregnane X Receptor Activation
Figure 7
Coregulation of SRC-1 and HNF4α with PXR was disrupted by sesamin. HepG2 cells were cotransfected with (a) a vector control (pcDNA3) or PXR expression plasmid (pcDNA3-PXR) and SRC-1 expression plasmid (pCR3.1-SRC-1), or (b) a vector control (pcDNA3) or PXR expression plasmid (pcDNA3-PXR) and HNF4α expression plasmid (pcDNA3-HNF4α), in combination with the CYP3A4 luciferase reporter plasmid and the pRC-CMV-β-galactosidase vector. Subsequently, the transfected cells were exposed to sesamin and/or rifampin for 24 h. Luciferase activity was measured and normalized to the corresponding β-galactosidase activity. The results are expressed as mean ± SD (); ***, as compared to rifampin-treated cells.
