Siafaka-Kapadai A, Svetlov S, Hanahan D J, Javors M A
Department of Chemistry, University of Athens, Greece.
Life Sci. 1998;63(20):1769-77. doi: 10.1016/s0024-3205(98)00451-2.
The purpose of this study was to investigate the effect of suramin, a polyanionic napthalene sulfonic acid, on human platelet aggregation and Ca2+ mobilization induced by various agonists. Our results show that suramin completely inhibited aggregation by thrombin, platelet activating factor (PAF), alkyllysophosphatidic acid (ALPA), or arachidonic acid in a concentration-dependent manner. The IC50 values of suramin for inhibition of aggregation by PAF, arachidonic acid, and thrombin were 76.7, 239, and 1.49 microg/ml, respectively. Ca2+ mobilization induced by thrombin was inhibited by suramin with an approximate IC50 value of 20 microg/ml. This concentration of suramin had no effect on PAF or oleic acid-induced Ca2+ mobilization. The mechanism by which suramin inhibits aggregation is not clear, but our results suggest that suramin inhibits the ligand-receptor interaction.
本研究的目的是探讨多阴离子萘磺酸苏拉明对各种激动剂诱导的人血小板聚集和Ca2+动员的影响。我们的结果表明,苏拉明以浓度依赖的方式完全抑制凝血酶、血小板活化因子(PAF)、烷基溶血磷脂酸(ALPA)或花生四烯酸诱导的聚集。苏拉明抑制PAF、花生四烯酸和凝血酶诱导聚集的IC50值分别为76.7、239和1.49μg/ml。苏拉明抑制凝血酶诱导的Ca2+动员,其近似IC50值为20μg/ml。该浓度的苏拉明对PAF或油酸诱导的Ca2+动员无影响。苏拉明抑制聚集的机制尚不清楚,但我们的结果表明,苏拉明抑制配体-受体相互作用。