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目的采用体外实验的方法 ,直接检测活血化瘀中药赤芍有效成分赤芍 80 1与细胞因子内皮素 1(ET 1)间的相互作用 ,探讨其作用的可能的靶点和分子机理。方法应用压电石英晶体生物传感器———石英晶体微天平 (QCM )检测赤芍 80 1与ET 1之间的特异性结合。在QCM金基片表面经活化后接合上亲和素 ,继而将生物素衍生化的ET 1固定于基片表面 ,加入赤芍 80 1,检测赤芍 80 1与ET 1之间的相互作用。每一步结合反应后 ,均用磷酸盐缓冲液 (PBS)冲洗以去除非特异性吸附。结果赤芍 80 1与ET 1发生特异性结合。结论ET 1可能是赤芍 80 1体内作用靶点之一 ,即赤芍 80 1通过与ET 1结合 ,阻碍ET 1与其受体间的结合 ,从而拮抗ET 1的作用 ,扩张血管 ,抑制血小板聚集。
Objective To investigate the interactions between Radix Paeoniae Rubra, an active component of Radix Paeoniae Rubrae, and the endothelin-1 (ET 1), and to explore the possible targets and molecular mechanisms of its action. Methods The specific binding between erythrosine 80 1 and ET 1 was detected by quartz crystal microbalance (QCM) using a piezoelectric quartz crystal biosensor. The surface of the QCM gold substrate was activated and then conjugated with avidin, followed by immobilization of the biotin-derivatized ET 1 on the surface of the substrate and the addition of erythromycin 801 to detect the interaction between erythromycin 80 1 and ET 1 . After each step of the binding reaction, they were washed with phosphate buffered saline (PBS) to remove nonspecific adsorption. Results The specific binding of erythromycin 80 1 to ET 1 occurred. Conclusion ET 1 may be one of the targets in erythropoiesis 80 1 in vivo. That is, erythrosine 80 1 can inhibit the binding of ET 1 and its receptors by binding to ET 1, and thus antagonize the effect of ET 1, dilate blood vessels, and inhibit platelet aggregation. .