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Rapid screening of estrogen-like active compounds from Rubus chingii Hu by Thermal Shift high throughput screening method
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DOI   10.11656/j.issn.1672-1519.2018.03.18
Key Words   hERα-LBD;hERβ-LBD;Rubus chingii Hu;ligand compound;estrogen-like activity
Author NameAffiliationE-mail
ZHANG Zhongqun Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China  
ZHANG Jing Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China  
LIU Yongbin Tianjin Acelbio Biological Technology Co., Ltd., Tianjin 300457, China  
WANG Yu Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China  
CHAI Xin Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China chaixinphd@aliyun.com 
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.

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