CAJ | 학술논문

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。
목적：간기천초소위천초적대표성성분，연구기작용적분자파표대천명천초약효물질기출급작용궤리구유중요의의。방법：본연구채용HT-29세포배양，이기고표체적GPR35수체위파표，통과무표기세포파점약이학기술검측간기천초소대GPR35수체적격동활성。결과：연구결과표명，간기천초소재HT-29세포상능구인기DMR향응，차향응곡선류형여GPR35수체격동제민천저일치，기EC50치위6.142±0.189μmol·L-1。차외，재HT-29세포상，간기천초소대GPR35수체격동제민천저유탈민작용， GPR35수체길항제ML145대간기천초소유길항작용。결론：유차가이추단간기천초소위GPR35수체적격동제。
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·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.