Dioscorealide B is a pharmacologically active compound from the rhizome of the Thai medicinal plant Dioscorea membranacea. Here, we demonstrated that in vitro treatment of
dioscorealide B resulted in a cytotoxic effect on MCF-7 human
breast cancer cells (IC50 = 2.82 microM). To determine whether this compound induces apoptosis in MCF-7, the
Annexin V assay was performed. The data showed that the number of apoptotic cells were increased 7-12 folds over that of the control cells
after treatment with various concentrations of
dioscorealide B (3, 6 and 12 microM) for 24 hours.
Dioscorealide B-induced apoptosis was associated with modulation of the multidomain Bcl-2 family members Bax, Bak and Bcl-2.
After treatment with 3 microM
dioscorealide B, acceleration of the level of proapoptotic
proteins Bax and Bak were observed at 6 hours and 12 hours, respectively, while the decrease in the expression of antiapoptotic
protein Bcl-2 was observed 3 hours after the treatment. These effects of
dioscorealide B might result in the activation of
caspase-8, -9 and -7, which lead to apoptosis in MCF-7 cells. Taken together, the results of this study provide evidence that
dioscorealide B possesses an antitumor property against human
breast cancer cells and thus provide the molecular basis for the further development of
dioscorealide B as a novel chemotherapeutic agent for
breast cancer treatment.