几类天然产物对纤溶系统的作用

The Effect of Some Natural Products on the Fibrinolytic System

在初筛天然来源的小分子PAI - 1抑制剂过程中发现一些天然产物显示出活性苗头 ,进一步试验和选择性试验表明这些化合物都不同程度分别对纤溶系统中存在的不同的酶具有抑制作用。化合物 1(expoxyrolinB)对纤溶酶有一定的抑制 ,化合物 2 (muricatincC)对PAI - 1具有一定的抑制作用且有较好的选择性。化合物 4 (cherimolin - 2 )对纤溶酶较强的抑制。化合物 5(morindone)对凝血酶、胰蛋白酶、纤溶酶均有抑制 ,其中对凝血酶作用最强 ,而同类化合的 6(damnacanthal)则只对纤溶酶有强的抑制 ,对PAI - 1抑制较强。化合物 7( 16α -hy droxy -cleroda - 4 ( 18) ,13 ( 14)Z -dien - 15,16-olide) ,8(hedergenin)对纤溶酶也有较强的抑制。化合物 9(ocetadecanoicacid - 9-yne)在较高浓度时 ( 30 μg/mL)对凝血酶、胰蛋白酶、纤溶酶和PAI- 1均有抑制 ,在低浓度时 ( 1μg/mL)对凝血酶、纤溶酶仍有强的抑制 ,无选择性。

In the course of a screening for inhibitors of PAI-1 from natural products with small molecular weight,preliminay “hits”were found from several natural products.Further investigation and selectivity experiments indicated that compound 1 (expoxyrolin B),compound 4 (cherimolin-2) and compound 6 (damnacanthal) showed some inhibition on plasmin;compound 2 (muricatin C) showed week specific PAI-1 inhibition activity.Compound 5 (morindone) inhibited thrombin,trypsin and plasmin,compound 7 (16α-hydroxy-cleroda-4(18),13(14)Z-dien-15,16-olide),compound 8 (hedergenin) and compound 9 (ocetadecanoic acid-9-yne) inhibited thrombin and plasmin.This report deals with the results of the effect of several natural products on the fibrinolytic system.