Objective To investigate the inhibitiory effect of tacrolimus(FK506) and adriamycin(ADM) on hepatocellular carcinoma.Methods HepG-2 cells were cultured,and divided into 4 groups,namely(control)、FK506、ADM、FK506+ADM groups,the cells were trated by the drugs for 24 to 48 hours(respectively).The inhibitory rate of the cells was measured by MTT assay,and cell cycle and cell apoptotic rate were detected by flow cytometry(FCM).Results The ability of tumor cell growth were inhibited by FK506 after 48h;the apoptosis ratio was increased when FK506 was below 100?g/L,and when it(exceeded) that value,the apoptosis ratio was decreased.FK506 and ADM significantly prolonged cell G_2 phase;combined tacrolimus and adriamycin had synergistic role effect on arresting the cell in G_2 phase,FK506 combined with adriamycin demonstrated synergistic effect on apoptosis.Conclusions FK506 could inhibit the growth of hepatocellular carcinoma,arrest the cell in G_2 phase,and increase apoptosis.FK506 combined with adriamycin demonstrated synergistic inhibitory effect on hepatocellular carcinoma.