Objective：To explore the effect and the mechanism of Lidan Tuihuang tang on rats with cholestatic jaundice.Methods：Randomly divided 48 cases of male Wistar rats into six groups，namely the control group，model group，positive medicine group，and the Lidan Tuihuang tang groups of low，middle and high dose，eight cases in each group.In addition to the control group，the other five groups were treated with a one-time gavage of alpha-naphthyliso thiocyanate(ANIT)solution(5 mL/kg)to establish models，inducing the lesion of acute intrahepatic cholestasis in rats.After the models were established for 48 h，the dosage in the Lidan Tuihuang tang groups of low，middle and high dose was 10、20、40 g/(kg·d).respectively；the positive medicine group was given Yinzhihuang granules of 1.6 g/kg by gavage；the control group and model group were give saline by gavage every day.All groups were treated for 7 days of continuous medication.The blood and liver tissues in rats of each group were collected， and the serum markers， protein expression of sodium taurocholate cotransporting polypeptide(NTCP)and bile salt export pump(BSEP)，and expression of mRNA in liver tissues were analyzed，and pathological sections were observed.Results：Compared with the control group，the levels of alanine aminotransferase(ALT)，aspartate aminotrans ferase(AST)， alkaline phosphatase(ALP)， γ-glutamyl transpeptidase(γ-GT)，total bilirubin(TBil)， direct bilirubin(DBil)and total bile acid(TBA)in serum were significantly increased(P＜0.05).Compared with the model group，the serum markers in the Lidan Tuihuang tang groups of low，middle and high dose were significantly decreased(P＜0.05).Compared with the control group，the protein expression of NTCP and BSEP and expression of mRNA in liver tissues in the model group were significantly decreased(P ＜ 0.05).Compared with the model group，the protein expression of NTCP and BSEP，and expression of mRNA in liver tissues in the Lidan Tuihuang tang groups of low，middle and high dose were significantly increased(P ＜ 0.05).From the observation of pathological sections， the rats in the model group showed enlargement，disorderly and irregular arrangement and punctate or focal necrosis of hepatocytes，and the contour was not clear；the rats also showed hyperplasia of cholangiocytes and enlargement of hepatic sinusoid，which can tell the infiltration of a large number of inflammatory cells.The infiltration of inflammatory cells and adipocytes in liver tissue pathology of rats in the Lidan Tuihuang tang groups of low，middle and high dose were decreased；the swelling of hepatocytes was significantly improved；hepatocytes were arranged in a more orderly manner，and the cell size was approximately equal.Compared with the positive medicine group，the pathological improvement of liver tissues in the Lidan Tuihuang tang groups of low，middle and high dose was more obvious，and the levels of ALT，ALP，AST，γ-GT and TBA in serum in these groups were significantly increased(P＜0.05)，while the protein expression of NTCP and expression of mRNA in them were remarkably increased(P＜0.05).Conclusion：Lidan Tuihuang tang can lower and regulate levels of ALT，AST，ALP，TBil，DBil and TBA in serum of rats with cholestatic jaundice induced by ANIT，whose curative effect is superior to that of Yinzhihuang granules.Lidan Tuihuang tang can improve the condition of rats with cholestasis through the mechanism of regulating the expression of NTCP，BSEP and mRNA.