Objective:To investigate the protective effects of resveratrol against α-naphthylisothiocyanate (ANIT)-induced cholestasis and its relationship with the metabolism of bile acid. Methods:The liver injury model rats with cholestasis were established by using ANIT,and then the protective effects of resveratrol were investigated. In sandwich-cultured rat hepatocytes,the effects of resveratrol on hepatocyte bile excretion and the metabolism of bile acid from cholesterol were investigated. The mRNA levels of enzymes and transporters related to bile acid excretion were determined by Q-PCR. Results: Resveratrol significantly decreased the activity of alanine aminotransferase (ALT),aspartate aminotransferase (AST),the serum content of total bilirubin (TBIL),direct bilirubin (DBIL) and indirect bilirubin (IBIL) in ANIT-induced hepatic injury rat models with cholestasis. In sandwich-cultured rat hepatocytes,resveratrol restored ANIT-induced decrease of biliary excretion index(BEI). It also decreased total bile acid and total bilirubin but increased total cholesterol in ANIT-injured hepatocytes. Data from Q-PCR showed that resveratrol made a recovery of ANIT-induced decrease of Bsep,Mrp2,Ntcp,Cyp7a1 and Cyp8b1 mRNA levels in hepatocytes. Conclusion:Resveratrol exerted protective effects against ANIT-induced liver injury and alleviated the cholestasis. The mechanism may be involved in the regulation of metabolism enzymes and transporters related to bile acid excretion.