OBJECTIVE: To study the inhibitory effects of emodin on the proliferation of human hepatocellular carcinoma SMMC7721 cells. METHODS: SMMC7721 cells were treated with 0 (negative control), 25, 37.5, 50, 62.5, 75, 87.5, 100 μmol/L emodin solution and 100 μmol/L 5-FU for 24 h, 48 h, 72 h. The optical density value of cells was detected, and inhibition rate was calculated. SMMC7721 cells were treated with 0 (negative control), 25, 50, 75 μmol/L emodin solution and 100 μmol/L 5-FU for 48 h, and cell apoptosis rate, cell cycle and the expression of Bax and Bcl-2 gene were detected. RESULTS: Compared with negative control, the rate of cell proliferation inhibition increased after treated with 25, 37.5, 50, 62.5, 75, 87.5, 100 μmol/L emodin and 100 μmol/L 5-FU, which was positively associated with the concentration and duration. Compared with negative control, the rate of cell apoptosis increased after treated with 25, 50, 75 μmol/L emodin solution and 100 μmol/L 5-FU; the expression of Bax increased and that of Bcl-2 dereased; 50, 75 μmol/L emodin solution and 100 μmol/L 5-FU could arrested cells at G0/G1 phase (P<0.05 or P<0.01). CONCLUSIONS: Emodin can inhibit the proliferation of SMMC7721, promote cell apoptosis and inhibit cell growth.