4',6,7-三羟异黄酮

生物活性靶点体外研究体内研究 4',6,7-三羟异黄酮试剂级价格

4',6,7-三羟异黄酮

CAS号:17817-31-1
英文名:6,7,4'-Trihydroxyisoflavone
中文名:4',6,7-三羟异黄酮
CBNumber:CB8397160
分子式:C15H10O5
分子量:270.24
MOL File:17817-31-1.mol

4',6,7-三羟异黄酮化学性质

熔点 :>280℃
沸点 :587.1±50.0 °C(Predicted)
密度 :1.548±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :soluble in Dimethylformamide
形态 :powder to crystal
酸度系数(pKa) :6.85±0.20(Predicted)
颜色 :Light yellow to Brown to Dark green
LogP :2.170 (est)
CAS 数据库 :17817-31-1(CAS DataBase Reference)

安全信息

安全说明 :22-24/25
WGK Germany :3
F :10
海关编码 :2914.69.9000

4',6,7-三羟异黄酮性质、用途与生产工艺

生物活性 Desmethylglycitein (4',6,7-Trihydroxyisoflavone)，大豆苷元的代谢产物，来源于大豆 Glycine max，具有抗氧化性和抗癌活性。Desmethylglycitein 在体内直接结合 CDK1 和 CDK2，抑制 CDK1 和 CDK2 活性。Desmethylglycitein 是蛋白激酶 C (PKC)α 的直接抑制剂，抑制正常人皮肤成纤维细胞中的太阳紫外线 (sUV) 诱导的基质金属蛋白酶1 (MMP1)。Desmethylglycitein 以 ATP 竞争方式与细胞质中的 PI3K 结合，抑制 PI3K 和下游信号级联的活性，从而抑制 3T3-L1 前脂肪细胞中的脂肪形成。
靶点

CDK1

CDK2

PKC

体外研究

Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppesses anchorage-dependent growth of HCT-116 and DLD1 cells in a dose- and time-dependent manner without cytotoxicity . Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppresses CDK1 activity in a dose-dependent manner and inhibits CDK2 activity in HCT-116 cells. Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) induces cell cycle arrest at the S and G2/M phases, the percentage of cells in S phase is higher in the 100 μM 6,7,4′-THIF-treated group, and the same pattern is observed in G2/M phase (29.5% versus 19.1% ) .

Cell Viability Assay

Cell Line:	HCT-116 cells
Concentration:	0, 12.5, 25, 50 or 100 μM
Incubation Time:	24, 48 or 72 hours
Result:	Inhibited anchorage-dependent and -independent growth of HCT-116 cells.

Western Blot Analysis

Cell Line:	HCT-116 and DLD1 cells
Concentration:	0, 25, 50 or 100 μM
Incubation Time:	48 hours
Result:	Inhibited CDK1,CDK2 expression.

Cell Cycle Analysis

Cell Line:	HCT-116 cells
Concentration:	0, 25, 50 or 100 μM
Incubation Time:	24, 48 or 72 hours
Result:	Induces cell cycle arrest of HCT-116 cells at S and G2/M phases.

体内研究

Desmethylglycitein (4',6,7-Trihydroxyisoflavone) (intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days) suppresses tumor development in mice and serves as an effective anticancer treatment with the potential to inhibit or delay the tumorigenicity of HCT-116 cells in an in vivo system.

Animal Model:	Female athymic nude mice subcutaneously injected with HCT-116 cells
Dosage:	5 or 25 mg/kg
Administration:	Intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days
Result:	Decreased tumor growth, volume and weight of HCT-116 xenografts.