Abstract: There is a long history of Toad venom in the treatment of cancer in China. Bufalin, extracted from Toad venom, is one of the biologically active compounds of anticancer. We elaborate the molecular mechanism of bufalin on anticancer activity from several aspects such as inducing cell apoptosis and differentiation, inhibitting cell proliferation and angiogenesis, enhancing the sensitivity of chemotherapeutics, which can provide the basis for in-depth study of Toad venom and its development and clinical medication.

Key words: Antineoplastic agents, Molecular mechanisms of pharmacological action, Bufalin