Bufalin

Isolated from venenum bufonis. Soluble in DMSO (5mg/ml), ethanol (15mg/ml) or DMF (20mg/ml). Bufalin is a cardiotonic steroid with anaesthetic, blood pressure stimulatory and respiratory activities. It is a potent Na+/K+-ATPase transporter inhibitor (Kd = 42, 45, and 40nM for the alpha1, alpha2, and alpha3 subunits, respectively). Bufalin has anticancer effects in a variety of cancer cell lines both in vitro and in vivo. It inhibits cancer cell proliferation, induces cell cycle arrest, induces apoptosis and autophagy, inhibits angiogenesis and neovascularization, induces cell differentiation, inhibits cancer metastasis and invasion, and enhances chemotherapeutic drug sensitivity through multiple kinase targets and also the Na+/K+-ATPase transporter. It also inhibits proteins of the steroid receptor coactivator family, such as SRC-1 and SRC-3 at 5nM. Bufalin has anti-inflammatory effects by modulating nuclear factor-kappaB (NF-kappaB) signaling and down-regulating inflammatory-related genes such as cyclooxygenases, lipoxygenases, inducible nitric oxide synthase (iNOS), and thereby decrease nitric oxide and prostaglandin E2 (PGE2) production.