Fibbi G, Serni U, Pucci M, Caldini R, Magnelli L, Del Rosso M
Dipartimento di Farmacologia Preclinica e Clinica Mario Aiazzi Mancini, Università di Firenze.
Drugs. 1988;35 Suppl 1:9-14. doi: 10.2165/00003495-198800351-00005.
Treatment with tiaprofenic acid appreciably reduced the level of plasminogen activators in the medium of 3T3-Balb mouse fibroblasts, as revealed by both a fibrin plate assay and amidolytic determination with chromogenic substrates. At the same time, tiaprofenic acid was able to inhibit the production of plasminogen activators induced by phorbol myristate acetate, a powerful inflammation and tumour promoter, added to the cell monolayers. By isolating the inhibitors of plasminogen activators it was possible to show that the decrease of fibrinolytic activity produced by tiaprofenic acid is not related to an increase of inhibitors. Rather, a decrease of activators seems to take place. Synovial fluid samples from 4 patients before and after treatment with tiaprofenic acid were also assayed for plasminogen activator activity by the fibrin lysis method. In 3 of the 4 cases a marked decrease after treatment was evident. The one unresponsive patient suffered from a para-neoplastic arthritis.
通过纤维蛋白平板试验和用发色底物进行的酰胺水解测定均显示,用噻洛芬酸处理可显著降低3T3 - Balb小鼠成纤维细胞培养基中纤溶酶原激活剂的水平。同时,噻洛芬酸能够抑制添加到细胞单层中的佛波醇肉豆蔻酸酯乙酸盐(一种强大的炎症和肿瘤促进剂)诱导的纤溶酶原激活剂的产生。通过分离纤溶酶原激活剂的抑制剂,可以表明噻洛芬酸产生的纤溶活性降低与抑制剂的增加无关。相反,似乎发生了激活剂的减少。还用纤维蛋白溶解法对4例患者在使用噻洛芬酸治疗前后的滑液样本进行了纤溶酶原激活剂活性测定。4例中有3例在治疗后明显下降。唯一无反应的患者患有副肿瘤性关节炎。