银杏素

生物活性靶点体外研究体内研究银杏素试剂级价格

银杏素

CAS号:481-46-9
英文名:GINKGETIN
中文名:银杏素
CBNumber:CB8350301
分子式:C32H22O10
分子量:566.51
MOL File:481-46-9.mol

银杏素化学性质

熔点 :297 °C(Solv: acetone (67-64-1))
沸点 :863.7±65.0 °C(Predicted)
密度 :1.506±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO:64.0(Max Conc. mg/mL);112.97(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:7):0.12(Max Conc. mg/mL);0.21(Max Conc. mM)
酸度系数(pKa) :6.18±0.40(Predicted)
形态 :powder
颜色 :Light yellow
LogP :4.450 (est)

银杏素性质、用途与生产工艺

生物活性 Ginkgetin 是一种从银杏叶中分离得到的双黄酮。Ginkgetin 具有抗肿瘤，抗炎，神经保护，抗真菌的作用。Ginkgetin 也是一种有效的 Wnt 信号抑制剂，IC50 值为 5.92 μM。
靶点

Wnt

5.92 μM (IC ₅₀ )

体外研究

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.

Cell Viability Assay

Cell 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 Analysis

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

Cell 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 Analysis

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

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.

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.