Breast cancer is a severe killer to women worldwide. To find effective therapy, many phyto-chemicals from traditional Chinese medicine were explored. Herein, we have identified 8-methoxyldaphnin from Hydrangea macrophylla and evaluated the inhibitory effects on breast cancer MDA-MB-231 cells. As a result, 8-methoxyldaphnin can inhibit MDA-MB-231 cells through induction of apoptosis. Further investigation has revealed 8-methoxyldaphnin can activate caspase-3, depolarize mitochondrial membrane potential, and down-regulate Bcl-2 mRNA level as well as up-regulate Bax mRNA level. These results veri...