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Objective: The aim of our study was to investigate the effect of Angelica keiskei chalcone (AC) on the expression of Caspase-3 and Bax in mice hepatocarcinoma cells. Methods: Fifty mice inoculated hepatocarcinoma 22 cells were divided into five groups, 10 mice per group. Mice were given 5, 20, 40 mg/kg AC daily by mouth in low, middle and high dose groups respectively. Saline were given to the tumor control group by mouth. Twenty mg/kg cytoxan (CTX) by injection every other day were given to the positive control group. Ten days later, all mice were sacrificed. The levels of the Caspase-3 and Bax protein expression were measured by immunohistochemistry method and the proliferation activity of hepatocarcinoma cells was determined by MTT assay. Results: The expression level of Caspase-3 and Bax protein in tumor control group were 5.00%and 4.68%, respectively, and those of the high-dose group were 38.52% and 35.76%. The differences between two groups were significant (P ＜ 0.05). The cell proliferation activity of tumor control group and high-dose group were 1.135 ± 0.032 and 0.716 ± 0.018. The difference was significant (P ＜ 0.05). Conclusion:AC can increase the expression of Caspase-3 and Bax protein, and inhibit the proliferative activity of mice hepatocarcinoma cells.