羟基茜草素对GPR35受体激动活性的研究  

Study on Purpurin As A G Protein-coupled Receptor-35 Agonist

作　　者：侯滔[1] 丁辉[1] 史丽颖[1] 何牮[2] 王纪霞[2] 魏来[2] 张秀莉[2] 梁鑫淼[2] 

机构地区：[1]大连大学药物研究所,大连116622 [2]中国科学院大连化学物理研究所,大连116023

出　　处：《世界科学技术-中医药现代化》2015年第7期1414-1418,共5页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：国家自然科学基金委面上项目(81473436):基于无标记动态质量重置技术的丹参多靶点作用研究;负责人:张秀莉

摘　　要：目的:羟基茜草素为茜草的代表性成分,研究其作用的分子靶标对阐明茜草药效物质基础及作用机理具有重要意义。方法:本研究采用HT-29细胞培养,以其高表达的GPR35受体为靶标,通过无标记细胞靶点药理学技术检测羟基茜草素对GPR35受体的激动活性。结果:研究结果表明,羟基茜草素在HT-29细胞上能够引起DMR响应,且响应曲线类型与GPR35受体激动剂敏喘宁一致,其EC50值为6.142±0.189μmol·L-1。此外,在HT-29细胞上,羟基茜草素对GPR35受体激动剂敏喘宁有脱敏作用,GPR35受体拮抗剂ML145对羟基茜草素有拮抗作用。结论:由此可以推断羟基茜草素为GPR35受体的激动剂。Purpurin is a common component ofRubia cordifolia L. The study on its molecular target was useful for elucidating the therapeutic material basis and action mechanism ofR. cordifolia. HT-29 cells were used in the cell culture. The highly expressed G Protein-coupled Receptor-35 （GPR35） agonist was used as target. The label-free optical biosensor cellular assay was used to investigate the agonist activity ofpurpurin at an endogenous receptor. The results showed thatpurpurin can cause DMR response in HT-29 cells. And the DMR response curve type was consistent with zaprinast. Its EC50 was 6.142± 0.189μmol＆#183;L-1. In addition,purpurinhad desensitization effect on GPR35 agonist zaprinast in HT-29 cells. GPR35 agonist ML145 blocked the DMR ofpurpurin. It was concluded thatpurpurinwas the GPR35 agonist.

关 键 词：羟基茜草素 GPR35 激动剂 无标记细胞分析 靶点药理学 

分 类 号：R285.5[医药卫生—中药学]