Bufalin is a traditional oriental medicines, originally isolated from the Chinese toad venom. Bufalin is a cardiotonic steroid that has the potential to induce differentiation and apoptosis of tumor cells. Research on bufalin has so far mainly involved leukemia, prostate cancer, gastric cancer and liver cancer, and has been confined to in vitro studies. The bufadienolides bufalin and cinobufagin have been shown to induce apoptosis in a wide spectrum of cancer cell. Bufalin has being shown to be a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1. Bufalin is a component of Huachansu, a Chinese medicine that comes from dried toad venom from the skin glands of Bufo bufo gargarizans Cantor or B.melanotictus Schneider, has been used in the treatment of various cancers in China.

Bufogenin (Resibufogenin) possesses significant pharmacological and toxicological effects, including cardiotonic, anesthetic, antitumor, and cardiotoxic effects. The bufodienolides are a group of steroid compounds that are classified as cardiac glycosides. Resibufogenin (RB), one of the major active compounds of the traditional Chinese medicine Chansu, has displayed great potential as a chemotherapeutic agent in oncology. Resibufogenin has been shown to exhibit the anti-proliferative effect against cancer cells. Although the mechanism of action of bufogenin is still under investigation, this agent is a specific Na+/K+-ATPase inhibitor and has been shown to reduce blood pressure in a rat model of preeclampsia.