The effect of capsaicin on the expression of CYP3A4

Abstract

Capsaicin (CPS), a constituent of green and red peppers, has been linked with suppression of tumorigenesis and carcinogenesis. However, the influence of CPS on CYP3A4 expression and their mechanisms remain unclear. In this study, we examined the effect of capsaicin on CYP3A4 expression in human hepatoma HepG2 cells and the pharmacokinetic profiles of CYP3A4 substrates in male Sprague-Dawley rats. Capsaicin induced enzyme activity and expression of CYP3A4 in pregnane X receptor (PXR)-transfected HepG2 cells. Additionally, this induction was mediated by the transient receptor potential vanilloid type-1 receptor (TRPV1) in capsaicin-treated HepG2 cells. Capsaicin also induced the activation of CCAAT/enhancer-binding proteinβ (C/EBPβ). Furthermore, capsaicin elevated the level of CYP3A1 in rat liver and significantly increased the biotransformation of nifedipine to dehydronifedipine. Taken together, capsaicin induces CYP3A4 expression in vitro and in vivo and this induction was achieved by the induction of PXR and activation of C/EBPβ.