Bufotalin

Bufotalin is a bufadienolide that has been found in toad (B. asiaticus) venom and has cytotoxic and immunomodulatory activities.^1,2 It induces cell cycle arrest at the G₁ phase and apoptosis in Hep3B cells when used at concentrations ranging from 0.13 to 1.13 ?M.¹ Bufotalin (100 ?g/kg) reduces autoantibody production, serum levels of TNF-α, IL-1β, IFN-γ, IL-22, and IL-17, and the number of splenic and lymph node Th17 cells, as well as increases saliva flow rates in a mouse model of experimental Sj?rgren’s syndrome, an autoimmune disease characterized by the reduced secretion of exocrine glands.² It also induces lethality in anesthetized dogs (LD₅₀ = 0.36 mg/kg).³

1.Su, C.-L., Lin, T.-Y., Lin, C.-N., et al.Involvement of caspases and apoptosis-inducing factor in bufotalin-induced apoptosis of Hep 3B cellsJ. Agric. Food Chem.57(1)55-61(2009) 2.Huang, Y., Yang, G., Fei, J., et al.Bufotalin ameliorates experimental Sj?gren's syndrome development by inhibiting Th17 generationNaunyn-Schmiedeberg's Arch. Pharmacol.393(10)1977-1985(2020) 3.Hamet, R.Toxicity of bufotalin administered by oral routeCompt. Rend. Soc. Biol.152571-574(1958)