OBJECTIVE：To study the effects of chitosan graphene oxide car rier（CS-GO）loaded with oridonin （CS-GO- oridonin）on the proliferation and apoptosis of human lung cancer A 549 cells. METHODS ：Taking A 549 cells as objects ，the survival rate of cells were detected by CCK- 8 method after treated with different concentrations of CS-GO （3，6，12，24，48 μg/mL）and CS-GO-oridonin loaded with same mass of oridonin （3，6，12，24，48 μg/mL，by the weight of oridonin ，the same below）. IC 50 of CS-GO-oridonin was calculated. The cell morphology were observed by microscope after treated with CS-GO and CS-GO-oridonin（both 32 μg/mL）for 2，4，10，24 h. The uptake of CS-GO ，oridonin，CS-GO-orionin（all 32 μg/mL）by cells was observed with fluorescence labeling method. The apoptosis of cells and the content of ROS were observed by flow cytometry after treated with different concentrations of CS-GO （16，32，64 μg/mL）and CS-GO-oridonin （16，32，64 μg/mL）. The expression of anti-apoptosis related proteins （Mcl-1，Bax and Bak ）were detected by Western blot. RESULTS ：After treated with different concentrations of CS-GO ，the survival rate of cells was still above 90％ ；after treated with different concentrations of CS-GO-oridonin，the survival rate of cells showed a downward trend ，and was significantly lower than that of CS-GO group （P＜ 0.01）；IC50 of CS-GO-oridonin was 32.61 μg/mL. After CS-GO treatment，the cell morphology did not change significantly ；after CS-GO-oridonin treatment ，the cells shrunk and fell off in clusters ，and the suspended matter increased ；the fluorescence of oridonin and CS-GO-orionin taken up by cells was enhanced than CS-GO. Compared with blank group ，there was no significant change in the apoptosis rate ，the content of ROS and the expression of apoptosis-related protein in 16，32，64 μg/mL CS-GO groups（P＞0.05）；apoptosis rate ，the content of ROS ，the protein expression of Bax and Bak in 16，32，64 μg/mL CS- GO-oridonin groups were increased significantly ，while the protein expression of Mcl- 1 were decreased significantly. Above indexes were significantly high er or lower than the same concentration CS-GO group （P＜0.05）. CONCL USIONS：CS-GO dose not affect the proliferation and apoptosis of A 549 cells；CS-GO-oridonin has obvious inhibition and apoptosis promoting effect on cells ，which may be related to increasing ROS production and regulating the expression of apoptosis related proteins.