Aim To investigate the effect of deguelin on the proliferation of non-small cell lung cancer cell line A549 and nude mice. Methods CCK-8 assay was used to detect the inhibition of deguelin on proliferation of SH-SY5Y cells; Hoechst stains and Annex-inV-FITC/PI double stained method were employed to observe the apoptotic morphology and apoptotic rate; flow cytometry was applied to determine the effect of deguelin on cell cycle of A549; tumor xenograft experiment and HE staining were conducted to investigate the effect of deguelin on growth of transplanted tumor in nude mice. Results Deguelin inhibited cell proliferation of A549 dose- A nd time-dependently; Hoechst stains and AnnexinV-FITC/PI double stained further confirmed that deguelin could induce the apoptosis of A549 cells, while deguelin blocked A549 cell cycle in G2/M phase in concentration-dependent manner. The nude mice xenograft model and HE staining experiments showed that deguelin significantly inhibited the growth of xenografts in A549 nude npce (P < 0. 01). Conclusions Deguelin has a significant inhibitory effect on non-small cell lung cancer cell line A549, pointing to a basis for the study of the antitumor activity of deguelin.