- 英文名称
- 6,7,4'-Trihydroxyisoflavone
- 分子式
- C15H10O5
- 分子量
- 270.24
- 中文别名
- 4',6,7'-三羟异黄酮; 4',6,7-三羟基异黄酮; 6,7-二羟基-3-(4-羟基苯基)-4H-苯并吡喃-4-酮; 4'-三羟基异黄酮; 6,7,4'-三羟基异黄酮; 6-羟基大豆苷元; TRIHYDROXYISOFLAVONE, 4',6,7-; DEMETHYLTEXASIN; 6,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one; TRIHYDROXYISOFLAVONE, 4',6,7-(RG); DESMETHYLGLYCITEIN (4',6,7-TRIHYDROXYISOFLAVONE); 6,7-Dihydroxy-3-(4-hydroxyphenyl); Desmethylglycitein; 4H-1-Benzopyran-4-one, 6,7-dihydroxy-3-(4-hydroxyphenyl)-
- 用途
- - 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.
