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苏拉明对补体、血液凝固、纤维蛋白溶解及激肽形成的影响。

Effects of suramin on complement, blood clotting, fibrinolysis and kinin formation.

作者信息

Eisen V, Loveday C

出版信息

Br J Pharmacol. 1973 Dec;49(4):678-87. doi: 10.1111/j.1476-5381.1973.tb08544.x.

Abstract
  1. The inhibition by suramin of complement components, and of blood clotting, fibrinolytic, and plasma kinin forming factors depended on the conditions of the assay and on the substrates used.2. Haemolysis by complement was more effectively inhibited in red blood cell suspensions, than in agarose gel plates. In esterolytic tests, the activation of component 1 (C1) to C1 esterase was significantly inhibited by 0.1-0.3 mM suramin, and the activity of C1 esterase by 0.5 mM suramin.3. Part of the anticoagulant effect of suramin is due to inhibition of the action of thrombin on fibrinogen.4. Suramin did not inhibit fibrin degradation by the fibrinolytic system in plasma. In esterolytic tests, the activation of plasminogen was more potently inhibited than the activity of plasmin.5. Activation of plasma kallikrein, measured either by kinin formation or by esterolysis, was inhibited by 0.1-0.3 mM suramin. Active plasma kallikrein was inhibited by 0.3-0.5 mM suramin. Pancreatic kallikrein was weakly inhibited, and urinary kallikrein not at all.
摘要
  1. 苏拉明对补体成分、凝血、纤维蛋白溶解及血浆激肽形成因子的抑制作用取决于测定条件及所用底物。

  2. 在红细胞悬液中,补体介导的溶血比在琼脂糖凝胶平板中更有效地受到抑制。在酯解试验中,0.1 - 0.3 mM的苏拉明显著抑制成分1(C1)激活为C1酯酶,0.5 mM的苏拉明抑制C1酯酶的活性。

  3. 苏拉明的部分抗凝作用是由于抑制了凝血酶对纤维蛋白原的作用。

  4. 苏拉明不抑制血浆中纤维蛋白溶解系统对纤维蛋白的降解。在酯解试验中,纤溶酶原的激活比纤溶酶的活性受到更有效的抑制。

  5. 通过激肽形成或酯解测定的血浆激肽释放酶的激活受到0.1 - 0.3 mM苏拉明的抑制。活性血浆激肽释放酶受到0.3 - 0.5 mM苏拉明的抑制。胰激肽释放酶受到微弱抑制,而尿激肽释放酶则完全不受抑制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6c2/1776599/d7481a244a36/brjpharm00542-0122-a.jpg

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