Ivanovska N, Yossifova T, Vassileva E, Kostova I
Department of Immunology, Bulgarian Academy of Sciences, Sofia.
Methods Find Exp Clin Pharmacol. 1994 Oct;16(8):557-62.
Coumarin derivatives are known to possess antiinflammatory and antimetastatic properties due to their direct action on cells, predominantly on macrophages. In the present study the interactions between esculin, esculetin, fraxin, fraxetin, as well as their acetylated and methylated derivatives and non-cell system participating in inflammatory processes, comprised of serum complement proteins, were investigated in vitro. 7-Methylesculin, esculin 5Ac and esculetin 2Ac exhibited good inhibition on classical pathway (CP) activity and scoparone strongly reduced alternative pathway (AP) activity in normal human serum (NHS). Some of the hydroxycoumarins were able to enhance hemolysis. Seven derivatives were tested in C1 and C3 functional assays, as 7-methylesculin appeared to be the strongest inhibitor of both activities. Esculin (En) and scopoletin (St) altered the effect of other complement activators (heat aggregated IgG, suramin, and zymosan) when applied with them simultaneously in vitro.
香豆素衍生物因其对细胞（主要是巨噬细胞）的直接作用而具有抗炎和抗转移特性。在本研究中，体外研究了七叶苷、七叶亭、秦皮苷、秦皮素及其乙酰化和甲基化衍生物与参与炎症过程的非细胞系统（由血清补体蛋白组成）之间的相互作用。7-甲基七叶苷、七叶苷5-乙酸酯和七叶亭2-乙酸酯对正常人血清（NHS）中的经典途径（CP）活性表现出良好的抑制作用，滨蒿内酯强烈降低替代途径（AP）活性。一些羟基香豆素能够增强溶血作用。在C1和C3功能测定中测试了七种衍生物，因为7-甲基七叶苷似乎是这两种活性的最强抑制剂。当七叶苷（En）和东莨菪亭（St）在体外与其他补体激活剂（热聚集IgG、苏拉明和酵母聚糖）同时应用时，会改变它们的作用效果。
