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 IC50 of 5.92 μΜ[1][2][3][4][5].
IC50 & Target[2]
Wnt
5.92 μM (IC50)
体外研究 (In Vitro)
Ginkgetin (2.5-20 μM; 48 h) inhibits the growth of Daoy and D283 cell lines, and induces G2/M cell cycle arrest in Daoy cells[2]. Ginkgetin (20-40 μM; 24 h) significantly activates the apoptosis of osteosarcoma cells in a concentration-dependent manner[3]. 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[2]. 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[1]. Ginkgetin (5-10 μM; 48 h) induces autophagy responsible for cell death in A549[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
Daoy and D283 cell lines
Concentration:
2.5, 5, 10, 20 μM
Incubation Time:
48 hours
Result:
Inhibited the cell growth, with IC50s of 14.65 and 15.81 μM for Daoy and D283 cells, respectively.
Apoptosis Analysis[3]
Cell 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 Analysis[2]
Cell Line:
Daoy cells
Concentration:
2.5, 5, 10, 20 μM
Incubation Time:
24 hours
Result:
Increased G2/M phase, compared with that of control, indicating a G2/M cell phase arrest.
Cell Cycle Analysis[2]
Cell 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.
体内研究 (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[4]. Ginkgetin (30 mg/kg; intragastrically once per day for 42 d) suppresses tumor growth in A549 cells bearing nude mice[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Sprague-Dawley rats (200-220 g)[4]
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.
分子量
566.51
Formula
C32H22O10
CAS 号
481-46-9
中文名称
银杏素；白果双黄酮；银杏双黄酮；银杏黄素
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Hu WH, et, al. Synergy of Ginkgetin and Resveratrol in Suppressing VEGF-Induced Angiogenesis: A Therapy in Treating Colorectal Cancer. Cancers (Basel). 2019 Nov 20;11(12):1828.
[2]. Ye ZN, et, al. Biflavone Ginkgetin, a Novel Wnt Inhibitor, Suppresses the Growth of Medulloblastoma. Nat Prod Bioprospect. 2015 Mar 29;5(2):91-97.
[3]. Xiong M, et, al. Ginkgetin exerts growth inhibitory and apoptotic effects on osteosarcoma cells through inhibition of STAT3 and activation of caspase-3/9. Oncol Rep. 2016 Feb;35(2):1034-40.
[4]. Li Q, et, al. Ginkgetin exerts anti-inflammatory effects on cerebral ischemia/reperfusion-induced injury in a rat model via the TLR4/NF-κB signaling pathway. Biosci Biotechnol Biochem. 2019 Apr;83(4):675-683.
[5]. Lou J, et, al. Ginkgetin induces autophagic cell death through p62/SQSTM1-mediated autolysosome formation and redox setting in non-small cell lung cancer. Oncotarget. 2017 Oct 16;8(54):93131-93148.
