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Celastrol is a triterpenoid isolated from Tripterygium wilfordii Hook F and may induce apoptosis and autophagy through generating reactive oxygen species (ROS).It has been reported that induction of cytochrome P450s (CYPs) are related with the development of oxidative stress, as well as drug-drug interaction.The induction of CYPs are unsurely mediated by nuclear receptors, such as AhR, PXR and CAR.Thus, by investigating the regulation of CYPs and nuclear receptors after celastrol treatment, our current study attempts to illustrate the possible mechanism of action of celastrol.