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目的:研究丹酚酸B镁盐(magnesium lithospermateB)对血小板聚集和5-HT释放功能的影响及其作用机制.方法:比浊法评价兔洗涤血小板的聚集反应;荧光分光光度法和放射免疫法观察血小板的5-HT与TXA_2的释放;用Fura 2荧光探针测定血小板胞内钙浓度变化.结果:丹酚酸B镁盐50-800mg/L对凝血酶或花生四烯酸诱导的血小板聚集反应有剂量依赖性的抑制作用,当体系无外Ca~(2+)存在,丹酚酸B镁盐的抑制作用增强,IC_(50)为102 mg/L.药物对血小板的5-HT释放也有剂量依赖性的抑制作用,但对AA激发的TXA_2释放无影响.同时,丹酚酸B镁盐对凝血酶激发的胞内钙升高有明显的抑制作用,并降低静息血小板[Ca~(2+)]_ⅰ.结论:丹酚酸B镁盐对体外洗涤血小板的聚集和5-HT释放反应有明确的抑制作用,可能与影响血小板胞内Ca~(2+)浓度的机制有关.
Objective: To study the effect of magnesium lithospermate B on platelet aggregation and 5-HT release and its mechanism.Methods: Turbidimetric method was used to evaluate the aggregation of washed platelets in rabbit, fluorescence spectrophotometry and radioimmunoassay The release of 5-HT and TXA 2 was observed, and the change of intracellular calcium concentration was measured by Fura 2 fluorescent probe.Results: The concentration of salvianolic acid B 50-800 mg / L on platelet aggregation induced by thrombin or arachidonic acid The inhibitory effect was dose-dependent, and the inhibitory effect of salvianolic acid B magnesium salt was enhanced when there was no Ca 2+ in the system with an IC50 of 102 mg / L. The 5-HT release of platelets But also dose-dependent inhibition, but had no effect on TXA 2 release stimulated by AA.At the same time, salvianolic acid B magnesium salt significantly inhibited thrombin-induced intracellular calcium elevation and decreased resting Ca ~ (2 +)] _ ⅰ. Conclusion: The salvianolic acid B magnesium salt has a clear inhibitory effect on the aggregation of washed platelets and the 5-HT release response in vitro, which may be related to the mechanism of affecting intracellular Ca 2+ concentration on platelets.