Objective:To investigate the effects of irinotecan(CPT-11)combined with X-ray treatment on the proliferation and apoptosis of human colon cancer cell line HCT-116. Methods:MTT method was used to detect the effects after treatment with different concentrations of CPT-11(10,20,30,40,50 μg/mL)for 24 hours and single dose of X-ray(3,6,9,12,15 Gy)on the proliferation of HCT-116. The proliferation rates of the three groups of cells were detected by clone formation assay,the apoptosis of the three groups was observed by AO/EB staining,and the levels of p53 and p21 protein were detected by Western blot. Results:CPT-11 inhibited the proliferation of HCT-116 cells in a dose-dependent manner in the range of 10~50 μg/mL. After pretreatment with CPT-11 at 10 μmol/L,combined 3,6,9,12 and 15 Gy X-ray irradiation showed that the inhibition rate of proliferation in the combined treatment group was higher than that in the irradiation group,and the difference was statistically significant(P < 0.05);compared with the control group and the irradiation group,the combined treatment group had a dose-dependent inhibition effect on the proliferation of HCT-116 cells. The number of colony formation decreased significantly(P < 0.05);the levels of p21 and p53 in the combined treatment group were significantly higher than those in the other two groups(P < 0.05),and the apoptotic rate also increased significantly(P < 0.05). Conclusion:Iritican combined with X-ray irradiation inhibits the proliferation and induces apoptosis of human colon cancer cell line HCT-116,which may be related to the activation of p53 and p21.