Abstract: Objective: : To investigate the effect of Matrine on Human hepatoma cells in vitro and explore the underlying mechanism. Methods : The MTT test and cell death detection ELISA were used to determine the effect ofMatrine on the viability and apoptotic death of human hepatoma cells. And then immunoblot analysis was performed to analyze the expression of Bcl and Bax. Results : Matrine induced apoptotic cell death in Hep G2cells in a time-, and dose-dependent manner. The expression levels of the anti-apoptotic Bcl-2 in matrine-treated cells were decreased in a time-dependent manner. This reduction was coupled to a stable increased expression level of the pro-apoptotic Bax. Furthermore, the Bax was shifted from the cytosol to themitochondria in cells treated with Matrine time-dependently, followed by cleavage of Caspase-3 and Caspase-9. Conclusion : Matrine causes death of liver cancer cells via the mitochondrial apoptotic pathway. Theseeffects are most likely dependent on the regulation of the levels of antiapoptotic and proapoptotic proteins.