基于高泌乳素血症探讨麦芽总生物碱中几个单体化合物与多巴胺受体的作用

Study on the effects of the interaction of several monomeric compounds in total malt alkaloids with dopamine receptors based on hyperprolactinemia

目的 基于高泌乳素血症探讨麦芽总生物碱中几个已知的浓度较高的组分即大麦芽碱、辛弗林、芦竹碱和多巴胺D1、D2受体感受器之间的相互作用机理,为进一步探索麦芽的药理作用提供理论基础。方法 选用能稳定表达多巴胺D1受体(DRD1)的中国仓鼠卵巢细胞的K1细胞株(CHO-K1),和能稳定性表达多巴胺D2受体(DRD2)的人胚肾细胞(HEK-293)为试验对象,用CCK-8试剂盒确定3种单体对2种细胞生存状态无不良影响后,采用分子对接法、竞争性受体配体结合实验对3个单体化合物与多巴胺受体的亲和力和调控作用进行研究。结果 大麦芽碱、辛弗林与DRD2间有较强亲和力,但均对DRD1无作用;大麦芽碱、辛弗林、芦竹碱与DRD2间有较强亲和力,且大麦芽碱、辛弗林对DRD2有显著激动作用。结论麦芽总生物碱的3个已知单体化合物中,大麦芽碱、辛弗林对DRD2有显著激动作用,3个单体均对DRD1无显著药理作用。

Objective To investigate the mechanism of action between several known high-content components of malt total alkaloids-hordeline,synephrine,rutabine and dopamine D1,D2 receptors based on hyperprolactinemia,and to provide a theoretical basis for further exploration of the pharmacological effects of malt.Methods The K1 cell line of Chinese Hamster Ovary Cells(CHO-K1)which can stably express dopamine D1 receptor(DRD1)and the human embryonic kidney cells(HEK-293)which can stably express dopamine D2 receptor(DRD2)were selected as the experimental subjects,after determining the effect of different drug concentrations on cell viability with CCK-8 kit,molecular docking method and competitive receptor ligand binding experiments were used to determine the relationship between the three monomer compounds and dopamine receptors.The affinity and regulation of the body were studied.Results Hordetine,synephrine and DRD2 had a significant agonistic effect on DRD2,but all had no effect on DRD1.Conclusion Among the three known monomeric compounds of malt total alkaloids,hordeumine and synephrine have significant agonistic effects on DRD2,and all three monomers have no effect on DRD1.