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AIM Oridonin, a natural tetracycline diterpenoid isolated from Chinese herb Rabdosia rubescens, has been reported to be a potent cytotoxic agent against various cancers.However, the effect of oridonin on highly metastatic breast cancer cells has not been addressed.METHODS AND RESLUTS In this study, we examined the anti-proliferation and anti-metastasis effects of oridonin in breast cancer cells MCF-7 and MDA-MB-231, and found it could induce a potent growth inhibition on them in a time-dependent and dose-dependent manner.Based on the flow cytometric analysis, oridonin suppressed MCF-7 cells growth by cell cycle arrest at the G2/M phase and caused accumulation of MDA-MB-231 cells in sub-G1 phase.The induced apoptosis effect of oridonin was further confirmed by morphologic characteristics assay and TUNEL assay.Immunofluorescent analysis showed that γH2AX-containing nuclear foci were significant in oridonin-treated MDA-MB-231 cells.Meanwhile, oridonin significantly suppressed cell migration and invasion,as well as decreases MMP-2/MMP-9 activation and inhibited the expression of Integrin β1 and FAK in breast cancer cells.CONCLUSION Oridonin inhibited the growth and induced apoptosis in breast cancer cells, which might be related to DNA damage and activation of intrinsic or extrinsic apoptotic pathways.Moreover, oridonin inhibited tumor invasion and metastasis in vitro possibly via decreasing the expression of MMPs and inhibiting the Integrinβ1/FAK pathway in MDA-MB-231 cells.