Resibufogenin

Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma^{[1][2][3][4][5][6][7][8][9]}. In Vitro: Resibufogenin (2-8 µM; 12-48 h) inhibits RPMI8226 cell viability in a dose- and time-dependent manner, with an IC₅₀ value of 7.694 µM at 48 h^[1].
Resibufogenin (10 mM) irreversibly activates mitral cells (MCs) in mouse main olfactory bulb (MOB) slices, evoking a lasting increase in depolarization and firing rate, and some cells die^[2].
Resibufogenin (10-200 nM; 12 h) inhibits the growth activity of Caki-1 cells in a dose-dependent manner, with an IC₅₀ value of 408.2 nM^[3].
Resibufogenin (0.1-10 μM; 24-48 h) decreases the cell viability of HCT116 cells dose-dependently^[4].
Resibufogenin (20 μM; 12 h) inhibits the migration of ES-2 and TOV-21G OCCC cells^[5].
Resibufogenin (2-5 μM; 1-3 days) inhibits the growth of human colon cancer HT-29 cells and induces G1-phase arrest in HT-29 cells^[6].
Resibufogenin (20-80 μM; 1 h) suppresses LPS-induced inflammation via inhibiting NF-κB and AP-1 pathways in RAW264.7 cells^[7].
Resibufogenin (1-10 μM; 24-72 h) inhibits the viability of human pancreatic cancer cells Panc-1 and Aspc^[8].
In Vivo: Resibufogenin (20 mg/kg; i.p.; daily; 21 days) suppresses the growth of TOV-21G cell tumor xenografts in nude mice, as indicated by a significant decrease in tumor volumes and changes in the expression of Ki-67^[5].
Resibufogenin (5-20 mg/kg; i.p.; 30 min before LPS challenge) ameliorates endotoxemia in ICR mice, as indicated by a significant decrease in serum TNF-α, IL-6 and MCP-1 levels^[7].
Resibufogenin (10-20 mg/kg; i.g.; every day; 20 days) suppresses human pancreatic tumor xenograft growth in athymic nude mice without causing systemic toxicity^[8].
Resibufogenin (10 mg/kg/day; i.p.; daily) exerts antitumor effects in BALB/c nude mice with orthotopic P3#GBM tumor xenografts, prolonging the median survival of tumor-bearing mice and suppressing tumor proliferation^[9].