AIM: To explore mitochondrial mechanisms of apoptosis induced by artesunate in human leukemia HL60 cells. METHODS: Human leukemia HL60 cell lines were treated by artesunate. The inhibitory effect on cell proliferation was assessed by MTT assay. Electron microscopy and DNA gel electrophoresis was applied to demonstrate the presence of apoptosis. The level of MMP, cell cycle were determined by flow cytometry (FCM). The activity of caspase 3 was observed by colorimetry. RESULTS: Art showed a dose dependent and time dependent manner on the growth of HL60 cells (P