Objective: To observe the inhibitory effect of artemisinin and its derivatives on non-small cell lung cancer A549 cells.Methods: The TC50(concentration required to cause 50% toxicity compared with controls)of artemisinin,dihydroartemisinin,and artesunate on A549 cells was detemined by MTT assay.The TC10 was selected as the experimental dosage in the proliferation inhibition of A549 assay.Results: The TC50 of artemisinin,dihydroartemisinin,and artesunate were 1.77 mmol/L,58.24 μmol/L,64.33 μmol/L,respectively.Artemisinin had no direct inhibition effect on the proliferation of A549,but dihydroartemisinin and artesunate prolonged the the cell cycle progression by delaying the double proliferation time.Conclusion: Dihydroartemisinin and artesunate may have direct inhibitory effect on the proliferation of A549 cells.