Sesamin: A Naturally Occurring Lignan Inhibits CYP3A4 by Antagonizing the Pregnane X Receptor Activation
Figure 9
Downregulation of CYP3A4 reporter activity on PXR agonist, paclitaxel- and SR12813-mediated induction by sesamin. LS174T cells were cotransfected with a vector control (pcDNA3) or PXR expression plasmid (pcDNA3-PXR), a CYP3A4 luciferase reporter plasmid, and a pRC-CMV-β-galactosidase vector. Subsequently, the transfected cells were exposed to sesamin and/or (a) 2.5 μM paclitaxel or (b) 10 μM SR12813 for 24 h. Luciferase activity was measured and normalized to the corresponding β-galactosidase activity. The results are expressed as mean ± SD (); * and ***, as compared to rifampin-treated cells, as indicated.
