ThermalShift高通量筛选法快速筛选覆盆子中雌激素样活性化合物

Rapid screening of estrogen-like active compounds from Rubus chingii Hu by Thermal Shift high throughput screening method

[目的]从覆盆子中筛选具有雌激素样活性的化合物。[方法]基于配体=受体理论,以人源雌激素受体亚型的配体结合域(hERα-LBD、hERβ-LBD)为靶点,以17β-雌二醇(E_2)为阳性对照,采用Thermal Shift高通量筛选方法筛选覆盆子中具有雌激素样活性的化合物。[结果]山柰酚明显提高雌激素受体配体结合域的(hERα-LBD、hERβ-LBD)热稳定性。[结论]山柰酚能与hERα-LBD和h ERβ-LBD结合,具有雌激素样活性。

[Objective]To screen estrogen-like active compounds from Rubus chingii Hu.[Methods]The subtypes of human estrogen receptor ligand binding domain(hERα-LBD and hERβ-LBD)were chosen as targets and E2was set as positive control to screen compounds with estrogen-like activity from Rubus chingii Hu by using Thermal Shift high throughput method based on the ligand-receptor theory.[Results]Kaempferol can significantly increase the thermal stability of hERα-LBD and hERβ-LBD.[Conclusion]Kaempferol have an estrogen-like activity,which can bind to hERα-LBD and hERβ-LBD.