OBJECTIVE: To investigate the effects of curcumin on proliferation and invasion of osteosarcoma cells and its mechanism. METHODS: In in vitro cell assay, osteosarcoma cells were divided into control group(dimethyl sulfoxide), curcumin low-concentration, medium-concentration and high-concentration groups (10, 20, 40 μmol/L) and curcumin high-concentration+endogenous miR-21 simulacrum (agomiR-21) group, curcumin high-concentration+agomiR-21 negative control (NC) group. The proliferation (OD value) and invasion ability (transmembrane cells number) of human osteosarcoma cells U-2OS and MG-63 were detected by CCK-8 and Transwell chamber method; the expression of miR-21 and its target gene PDCD4 protein were detected by real-time fluorescence quantitative PCR and Western blot assay. In in vivo cell assay, MG-63 cells were inoculated in mice, and the mice were divided into blank control group (normal saline), curcumin group (20 mg/kg), curcumin+agomiR-21 NC group (20 mg/kg curcumin solution+50 mg/kg agomiR-21 NC solution), curcumin+agomiR-21 group (20 mg/kg curcumin solution+50 mg/kg agomiR-21 solution) with 8 mice in each group; they were given intratumoral injection of relevant medicine once a day, for consecutive 7 d. The volume changes of the tumor were measured within 20 d after medication, and the expression of miR-21 and PDCD4 protein in tumor tissue were detected on 20th day. RESULTS: Compared with control group, the OD value and transmembrane cells number of U-2OS and MG-63 cells were decreased significantly in curcumin low-concentration, medium-concentration and high-concentration groups (P<0.05 or P<0.01);the expression of miR-21 was weakened significantly in curcumin medium-concentration and high-concentration groups of U-2OS and MG-63 cells (P<0.05 or P<0.01), while the expression of PDCD4 protein was strengthened significantly (P<0.01). Compared with curcumin high-concentration+agomiR-21 NC group, the OD value and transmembrane cells number of U-2OS and MG-63 cells were strengthened significantly in curcumin high-concentration+agomiR-21 group (P<0.01). Compared with blank control group, the tumor volume of mice were decreased significantly in curcumin group and curcumin+agomiR-21 NC group (P<0.05 or P<0.01). The expression of miR-21 was decreased significantly in tumor tissue (P<0.01), while the protein expression of PDCD4 was strengthened significantly (P<0.01). Compared with curcumin+agomiR-21 NC group, the tumor volume of mice were increased significantly in curcumin+agomiR-21 group (P<0.05 or P<0.01). The expression of miR-21 in tumor tissue were strengthened significantly (P<0.01), while the expression of PDCD4 protein were weakened significantly (P<0.01). CONCLUSIONS: Curcumin can inhibit the proliferation and invasion of human osteosarcoma cells U-2OS and MG-63, the mechanism of which may be associated with down-regulating the expression of miR-21.