4',6,7-三羟异黄酮

更新时间: 2024-04-30 00:03:41 责编：网友投稿浏览

4',6,7-三羟异黄酮

4',6,7-三羟异黄酮用途与合成方法

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.