Abstract: Objective To study the effects of lobaplatin on the proliferation and apoptosis of osteosarcoma MG-63 cells and the mechanism of its function. Methods MG-63 cells in log phase were divided into control group and experimental groups. Experimental groups were treated with different concentrations of lobaplatin (2, 4 and 8μg/ml). MTT colorimetry and fl owcytometry were used to detect the effects of lobaplatin on cellular morphology change, cell growth, cell cycle, and the induction of apoptosis in MG-63 cells. Cell growth curves were studied at different concentrations of lobaplatin. Western blot was used to detect the effects of lobaplatin on the expression of Bcl-2 in MG-63 cells. Results Lobaplatin could inhibit the growth or proliferation and increase the apoptosis of osteosarcoma cell line MG-63 in a dose- and time-dependent manner. Bcl-2 protein level was decreased after lobaplatin treatment. Conclusion The effects of lobaplatin on the proliferation, the apoptosis and changing the cell cycle change of MG-63 cells might be related to its inhibition on Bcl-2 protein expression.