Bufalin is a traditional oriental medicines which induces apoptosis in some lines of human tumor cells. Itconstitutes the major digoxin-like immunoreactive component of Chan Su, obtained from the skin and parotidvenom glands of toads. Bufalin is cardioactive C-24 steroids that exhibits a variety of biological activities, suchas cardiotonic, anaesthetic, blood pressure stimulatory, respiratory and antineoplastic effects. In terms of itsanti-tumor activity, bufalin has been demonstrated to inhibit the growth of tumors, such as endometrial andovarian cancers. This commentary introduces biologic and therapeutic effects of bufalin in treating some cancers.The compound is able to mediate inhibition of cell growth, cell cycle arrest, apoptosis, and expression of genesrelated to the malignant phenotype in human cancer cells.