Abstract: 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 (16a - 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 re-sults of the effect of several natural products on the fibrinolytic system.

Key words: Natural products

摘要： 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 (expoxyrolin B)对纤溶 酶有一定的抑制，化合物2 (muricatinc C)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-hydroxy-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 (ocetadecanoic acid-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(1 μg/mL)对凝血酶、纤溶酶仍有强的抑制，无选择 性。本文对这些化合物的有关活性实验结果进行了讨论。

关键词: 天然产物, 纤溶作用, PAI-1抑制剂