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

作　　者：张中群 张竞 刘永彬 王彧 柴欣 ZHANG Zhongqun;ZHANG Jing;LIU Yongbin;WANG Yu;CHAI Xin(Tianjin State Key Laboratory of Modern Chinese Medicine, Academy of Traditional Chinese Medical, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;Tianjin Acelbio Biological Technology Co., Ltd., Tianjin 300457, China)

机构地区：[1]天津中医药大学中医药研究院,天津市现代中药重点实验室,天津300193 [2]天津艾赛博生物技术有限公司,天津300457

出　　处：《天津中医药》2018年第3期221-224,共4页Tianjin Journal of Traditional Chinese Medicine

基　　金：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

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(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.

关 键 词：hERα-LBD hERβ-LBD 覆盆子 配体化合物 雌激素样活性 

分 类 号：R284.2[医药卫生—中药学]