用血管内皮细胞膜色谱模型研究9种药物的生物亲和作用

Chromatographical studies on bio-affinity of nine ligands to human umbilical vein endothelial cell in cell membrane

目的增加细胞膜色谱法的适用范围,构建血管内皮细胞细胞膜固定相,研究药物与血管内皮细胞膜上受体的生物亲和作用。方法培养血管内皮细胞细胞株,制备细胞膜固定相,应用细胞膜色谱法研究九种药物与受体的亲和力。结果九种不同的配体与受体的亲和顺序为:S(+)QNB、哌唑嗪、R(-)QNB、阿托品、育亨宾、BMY7378、(±)美托洛尔、山莨菪碱、东莨菪碱。其容量因子分别为:14.289、13.667、11.121、6.794、4.758、4.386、3.926、2.424、2.412。结论血管内皮细胞膜色谱模型具有高度稳定性,可试用于药物的高效初筛。

Objective To extend the application of cell membrane chromatography （CMC）, the cell membrane stationary phase （CMSP） with human umbilical vein endothelial cell （EVC304） are constructed. The chromatography affinity of drugs to receptors of EVC304 is investigated. Methods We cultured EVC304 strain and constructed EVC304 CMSP. The bio-affinity of nine drugs to receptors was investigated per CMC method. Results The affinity rank order of receptors obtained from CMC for the nine ligands was as follows： S（＋）QNB, prazosion, R（-）QNB, atropine, yohimbine, BMY7378, metoprolol, 654-2, and scopolamine. The related k＇ values were 14.289, 13.667, 11.121, 6.794, 4.758, 4.386, 3.926, 2.424, and 2.412. Conclusion The EVC304 expressed CMSP has high stability and can be used to speed up the initial screening.