心肌细胞膜固定相色谱研究中药川芎提取液与受体的作用

目的 :研究中药川芎提取液与心肌细胞膜受体的作用。方法 :将家兔心肌细胞膜固定在硅胶载体上制成色谱固定相 ,通过川芎水提液和醇提液与心肌细胞膜上已知受体的部分激动剂和拮抗剂在心肌细胞膜色谱柱上保留特性的对比 ,以及流动相中加入心肌细胞膜上已知受体激动剂或拮抗剂时由于竞争结合而产生的对提取液色谱保留特性的影响 ,研究川芎提取液与心肌细胞膜受体的作用。结果 :水提液和醇提液在心肌细胞膜色谱柱上均有保留行为 ;水提液保留特性受α受体阻断剂竞争结合的影响 ,而不受 β₁受体激动剂的影响。结论 :川芎水提液中可能含有与α受体作用的有效成分、不含有与 β₁受体作用的有效成分 ,醇提液中亦含有与心肌细胞膜受体作用的成分。将细胞膜固定在色谱填料上 ,能够进行模仿药物在体内与受体作用的有关过程 ,不仅可以用于药物筛选 ,还可以用于揭示其所作用的受体类型。

Study on the interactions between Ligusticum chuanxiong extract and cardiac muscle membrane receptors by CMSP chromatography

OBJECTIVE: To study the interactions between Ligusticum chuanxiong Hort extract and cardiac muscle membrane receptors. METHOD: The cell membrane of rabbit cardiac muscle was fixed on silicon to make cell membrane stationary phase (CMSP), and then the interactions were studied by comparing the retention characteristics of the extracts from different solvents with those of the antagonists or activators corresponding to known receptors in cardiac muscle membrane, and by competition effect on the retention characteristics of extracts when adding the antagonists or activators into the mobile phase. RESULT: Water extract and ethanol extract both had retentions on CMSP; the retention characteristics of water extract could be affected when water extract was in competition with the antagonists for alpha receptor, and could not be affected when with the activator beta1 receptor. CONCLUSION: It is possible that some components in water extract may combine with alpha receptor and no component with beta1 receptor, and that some components in ethanol extract may combine with cardiac muscle cell membrane. The process between active components and receptors in vivo can be imitated through the interactions between drugs and CMSP. The method provides references for the resolution of two applications: to screen the active components from Chinese medicine, and to figure out the type of receptors involved.