[Show abstract][Hide abstract] ABSTRACT: Cinobufacini, a water-soluble preparation of Chinese medicine, is extracted from the skin of Bufo bufo gargarizans Cantor. The present study sought to investigate the effects of Cinobufacini on apoptosis of the hepatocellular carcinoma cell line BEL-7402. Cell viability was measured by methyl thiazolyl tetrazolium assay. Cell morphology was observed by Hoechst 33258 staining. Western blotting analysis was used to detect Bax and Bcl-2 expression. Results indicated that Cinobufacini inhibited the proliferation of BEL-7402 cells in a dose and time-dependent manner. Marked morphological changes indicative of apoptosis were observed after treatment with different concentrations of Cinobufacini. Western blot analysis showed that Bcl-2 expression was down-regulated while Bax expression was upregulated. Thus, Cinobufacini may have a significant apoptosis-inducing effect on BEL-7402 cells, and this could prove useful for further anti-cancer research.