Gamabufotalin

Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways. In Vitro:Gamabufotalin (0-500 nM, 48 h) inhibits cell viability of human lung cancer A549, H1299, H322 cells, and inhibits colony formation and migration (0-100 nM, 48 h), with no cytotoxicity in human normal lung cell line (HLF cells)^[1].
Gamabufotalin (0-100 nM, 12-48 h) inhibits COX-2 expression and inhibits NF-κB and p300 translocation in A549 cells^[1].
Gamabufotalin (0-100 nM, 12-48 h) induces apoptosis by activating the cytochrome c release and caspase-dependent apoptotic pathway in A549 cells^[1].
Gamabufotalin (0-100 nM, 48 h) induces hyperphosphorylation of p38, increases the expression of ATP1A3 and decreases AQP4 expression in U87 cells^[3].
Gamabufotalin (0-50 nM, 24 h) inhibits VEGF (50 ng/mL)-induced angiogenesis in an HUVECs in vitro angiogenesis tube formation assay^[4].
In Vivo:Gamabufotalin (5 and 20 mg/kg/day, i.p., for 17 days) inhibits tumor growth in the A549-xenografts mice^[1].
Gamabufotalin (1 mg/kg, i.p., three times per week) together with Temozolomide (HY-17364) (20 mg/kg. i.p., three times per week) shows a synergistic antitumor effect, and inhibits tumor growth and prolongs mice survival in mice U87 xenografts^[3].