Objective:To study the effect of Bufalin on the proliferation and cell cycle progression in BEL-7402 human hepatocarcinoma cell line.Methods:Time and dose effects of Bufalin in BEL-7402 human hepatocarcinoma cell line were detected using MTT assay.Cell morphological and ultrastructural changes were observed by light microscope and transmissiion electron microscope.Influence of cell cycle was analyzed by flow cytometry.Results: Treatment of BEL-7402 cells with Bufalin remarkably inhibited cell growth,with a dose and time dependency.The IC_(50) value on BEL-7402 cells at 24,48,72 hour was 6.67,0.348 and 0.228μmol/L respectively.Bufalin can induce G2/M cell cycle arrest and typical cell apoptosis as compared with the control.Conclusion:Inducing G2/M cell cycle arrest may be one of the cytotoxicity mechanisms of Bufalin.