摘要: |
[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(E2)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hERβ-LBD结合,具有雌激素样活性。 |
关键词: hERα-LBD hERβ-LBD 覆盆子 配体化合物 雌激素样活性 |
DOI:10.11656/j.issn.1672-1519.2018.03.18 |
分类号:R284.2 |
基金项目:国家自然科学基金青年科学基金项目(81403060);天津市应用基础与前沿技术研究计划项目(14JCYBJC42900);天津市药用植物细胞规模培养企业重点实验室资助项目。 |
|
Rapid screening of estrogen-like active compounds from Rubus chingii Hu by Thermal Shift high throughput screening method |
ZHANG Zhongqun1, ZHANG Jing1, LIU Yongbin2, WANG Yu1, CHAI Xin1
|
1.Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;2.Tianjin Acelbio Biological Technology Co., Ltd., Tianjin 300457, China
|
Abstract: |
[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 E2 was 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. |
Key words: hERα-LBD hERβ-LBD Rubus chingii Hu ligand compound estrogen-like activity |