【作者】 王凤琴； 张倩； 李春红； 王引珍； 夏之宁； 杨丰庆；

【Author】 WANG Feng-qin;ZHANG qian;LI Chun-hong;WANG Ying-zhen;XIA Zhi-ning;YANG Feng-qing;School of Chemistry and Chemical Engineering, Chongqing University;

【机构】 重庆大学化学化工学院；

【摘要】 目的建立开管亲和电色谱法用于评价小分子和血小板的亲和作用。方法制备不同涂覆长度的涂层毛细管,用漂移法计算小分子在涂层毛细管内的保留因子以及小分子和血小板的结合常数。测定小分子的体外抗血小板聚集活性,分析结合常数和抗血小板聚集活性的关系。结果能诱导血小板聚集的ADP与血小板的亲和作用强,而没有抗血小板聚集活性的3,4-二羟基苯甲酸几乎和血小板没有亲和作用,丹酚酸B、丹参素钠、阿魏酸、绿原酸、咖啡酸、芥子酸等与血小板的结合常数与之体外抗血小板聚集活性成正相关。结论开管血小板亲和电色谱可以用于评价小分子血小板的亲和作用,为药物抗血小板聚集活性预测提供依据。更多还原

【Abstract】 OBJECTIVETo develop an open tubular affinity capillary electro-chromatography(OT-ACEC) method for evaluation of affinity interaction between small molecule and platelet. METHODS prepare plateletcoated capillaries with different coating lengths; calculate retention factors of small molecules and their binding constants with platelet according to peak-shift assay; determine the anti-platelet aggregation activity in vitro to study the relationship between activity and binding constant. RESULTS ADP that can induce aggregation of platelet had high affinity interaction with platelet and protocatechuic acid that had no inhibition on platelet aggregation had no affinity interaction with platelet; small molecules with similar structures had similar affinity interaction with platelet; there was a positive correlation between the anti-platelet aggregation activity of small molecules and their interaction with platelet. CONCLUSION The OT-ACEC method developed in the present study can be a potential method to evaluate affinity interaction between small molecules and platelet, so as to predict the biological activities such as anti-platelet aggregation for the small molecules.更多还原