Genipin, a constituent of Gardenia jasminoides Ellis, is used in the treatment of hepatic disorders and inflammatory diseases in traditional medicine. Although mounting evidence suggests an anti-tumor activity of genipin in several cancer cell systems, the inhibitory effect of genipin on the growth of breast cancer cells has not been reported yet. The present study aimed to investigate the anti-proliferative activity of genipin in MDA-MB-231 human breast cancer cells. Herein, we showed that genipin efficiently induced apoptosis in MDA-MB-231 cells by the down-regulation of Bcl-2, up-regulation of Bax and proteolytic activation of caspase-3. Activation of JNK and p38 MAPK also increased by genipin. Importantly, genipin significantly inhibited invasive and migratory phenotypes of MDA-MB-231 cells. Taken together, this study demonstrates that genipin induces apoptosis and inhibits invasive/migratory abilities of highly invasive MDA-MB-231 human breast cancer cells, suggesting a potential application of genipin as a chemopreventive agent that may prevent or alleviate metastatic breast cancer.