Triptonide

A key bioactive small molecule identified in Tripterygium wilfordii Hook F., has a broad spectrum of biological functions; effectively inhibits canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin; upregulates the expression of IL-37; potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively.(In Vitro):Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells.Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively.Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability.Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells.Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways.(In Vivo):Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice.