In order to develop a series of novel compounds with antiplatelet aggregation activities, 3,15-disuccinate-12-coumarin substituted derivatives were designed and synthesized based on the natural product andrographolide. In vitro antiplatelet aggregation activities were evaluated by the turbidimetric method with thrombin, adenosine diphosphate (ADP), arachidonic acid (AA), and collagen as inducers. The biological evaluation revealed that compound 11k showed significant inhibition activity for thrombin, AA, and collagen-induced platelet aggregation at the same time and exhibited a dose-dependent behavior. Compound 11c showed the highest antiplatelet aggregation activity induced by ADP. Most of the derivatives had no significant cytotoxicity. Therefore, our work proved that 3,15-disuccinate-12-coumarin substituted andrographolide derivatives had the potential to become a novel candidate structure for antiplatelet aggregation and deserved further study.

为了开发一系列具有抗血小板聚集活性的新型化合物，基于天然产物穿心莲内酯设计并合成了3,15-二琥珀酸酯-12-香豆素取代的衍生物。通过比浊法，以凝血酶，二磷酸腺苷（ADP），花生四烯酸（AA）和胶原为诱导剂，通过比浊法评估了体外抗血小板聚集活性。生物学评估表明，化合物11k同时显示出对凝血酶，AA和胶原蛋白诱导的血小板聚集的显着抑制活性，并表现出剂量依赖性行为。化合物11c显示出由ADP诱导的最高的抗血小板聚集活性。大多数衍生物没有明显的细胞毒性。因此，我们的工作证明3,15-二琥珀酸酯-12-香豆素取代的穿心莲内酯衍生物具有成为抗血小板凝集的新型候选结构的潜力，值得进一步研究。