OBJECTIVE To study the growth inhibitory and apoptosis-inducing effect of baicalein and baicalin on human osteosarcoma cell line U2OS and U2OS/MTX300.METHODS U2OS and U2OS/MTX300 cell line were treated with various concentrations of baicalein and baicalin.Their effect of proliferation was determined by MTT test and morphology observation.Flow cytometry were applied to detect the baicalein-induced and baicalin-inducde apoptosis and analyse the cell cycle.RESULTS Baicalein was more effective on a growth inhibitory and apoptosis-inducing of U2OS and U2OS/MTX300 cell than baicalin.CONCLUSION Baicalein has an strong growth inhibitory and apoptosis-inducing effect on U2OS and U2OS/MTX300 cell than baicalin.