Abstract: AIMTo study the anticancer effect of artesunate and its mechanism. METHODSTo observe the effect of artesunate on the growth of solid tumor and the expression of PCNA, Bcl-2 and Bax genes in mice bearing H₂₂ solid hepatic carcinoma. RESULTSAfter administration of artesunate (ig, 300 mg·kg^-1·d^-1×7 d), growth of solid tumor was obviously inhibited, the tumor inhibitory rates were 49.1%, 48.7% and 46.6% in 3 experiments. The apoptosis of liver cancer cells were increased. Immunohistochemical staining showed that the number of Bcl-2 protein positive cells were decreased, but the number of Bax protein positive cells were increased. The PCNA positive cells were significantly lower than those in the control group. CONCLUSIONArtesunate showed obvious anticancer activity on H₂₂ hepatic carcinoma bearing mice and undergo apoptosis of liver cancer cells. The mechanism of anticancer effect of artesunate may be related to down-regulation of the expression of PCNA and Bcl-2 genes and up-regulation of the expression of Bax gene.