Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling , with an IC 50 of 5.92 μΜ.
In Vitro
Ginkgetin (2.5-20 μM; 48 h) inhibits the growth of Daoy and D283 cell lines, and induces G 2 /M cell cycle arrest in Daoy cells. Ginkgetin (20-40 μM; 24 h) significantly activates the apoptosis of osteosarcoma cells in a concentration-dependent manner. Ginkgetin (10-20 μM; 3-24 h) down-regulated the expression of Wnt target genes without affecting the expression of β-catenin in medulloblastoma cells. Ginkgetin (1-10 μM; 24 or 48 h) significantly inhibits the VEGF-induced endothelial cell proliferation, migration, and wound recovery in a concentration-dependent manner. Ginkgetin (5-10 μM; 48 h) induces autophagy responsible for cell death in A549 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Daoy and D283 cell lines Concentration: 2.5, 5, 10, 20 μM Incubation Time: 48 hours Result: Inhibited the cell growth, with IC 50 s of 14.65 and 15.81 μM for Daoy and D283 cells, respectively. Apoptosis AnalysisCell Line: Osteosarcoma cells Concentration: 20, 30, 40 μM Incubation Time: 24 hours Result: Markedly induced the apoptosis of osteosarcoma cells in a concentration-dependent manner. Cell Cycle AnalysisCell Line: Daoy cells Concentration: 2.5, 5, 10, 20 μM Incubation Time: 24 hours Result: Increased G 2 /M phase, compared with that of control, indicating a G 2 /M cell phase arrest. Cell Cycle AnalysisCell Line: Daoy and D283 cell lines Concentration: 10, 20 μM Incubation Time: 3, 6, 12, 24 hours Result: Attenuated the expression of Wnt target genes, Axin2, cyclin D1 and survivin at 20 μM for 24 h in Daoy cells. Unaffected the level of total β-catenin and diminished the level of β-catenin phosphorylation in a time- and concentration-dependent manner.
In Vivo
Ginkgetin (25-100 mg/kg; i.p. 2 hours after the onset of ischemia) exerts anti-inflammatory effects on cerebral ischemia/reperfusion-induced injury in a rat model via the TLR4/NF-κB signaling pathway. Ginkgetin (30 mg/kg; intragastrically once per day for 42 d) suppresses tumor growth in A549 cells bearing nude mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (200-220 g)Dosage: 25, 50, 100 mg/kg Administration: I.p. 2 hours after the onset of ischemia Result: Reduced the neurological deficit score. Suppressed the expression of NF-κB, TLR4 and IκBαin ischemic penumbra cortex, and inhibited the degradation of IκBα. Decreased the expressions of ICAM-1, COX-2, and iNOS. Downregulated downstream inflammatory factor PGE2 and TNF-α expression. Decreased IL-1β, IL-6, IL-8, and IL-10 protein expression.
Form:Solid
