This study shows that 1 mg/mL kuhuang injection extract exerts a significant anticholestatic effect, possibly by activating PPAR-γ signalling and reducing the internalization of MRP2 and BSEP caused by oxidative stress-induced disruption of F-actin, thereby alleviating CPZ-induced intrahepatic cholestasis and reducing the expression of DR5 and cell death (Figure 9). This evidence concerns the gene CPZ and intrahepatic cholestasis.