arenobufagin

Arenobufagin is a cardiotoxic bufanolide steroid lactone isolated from the venom and skin of toads such as Bufo arenarum, Bufo gargarizans, and Bufo melanostictus. It is a major component of traditional Chinese medicine ("Chan Su") and has been studied for its cardiotonic, analgesic, and notable antitumor activities, particularly against hepatocellular carcinoma and other cancer types. The primary mechanism of action is potent inhibition of the sodium-potassium ATPase (Na+/K+-ATPase) in cardiac myocytes, which is linked to both its cardiotonic and cardiotoxic effects. Arenobufagin also exerts anti-angiogenic effects by inhibiting VEGF-mediated angiogenesis through VEGFR-2 pathway suppression, and induces apoptosis and autophagy in tumor cells via inhibition of signaling in the PI3K/Akt/mTOR pathway. High doses can cause arrhythmia and cardiac dysfunction, making its toxicity a major concern for therapeutic use[1][3][4][5].

Other names

TrobufotoxinArenobufogenin3β,11α,14-Trihydroxy-12-oxo-5β-bufa-20,22-dienolideBufa-20,22-dienolide,3,11,14-trihydroxy-12-oxo-, (3β,5β,11α)-464-74-427R42QLM25