Steinmeyer J, Kalbhen D A
Institut für Pharmakologie und Toxikologie, Universität Bonn, Fed. Rep. of Germany.
Arzneimittelforschung. 1990 Feb;40(2 Pt 1):196-200.
The effect of diclofenac-Na, glycosaminoglycanpolysulfate (GAGPS), eglin C and alpha 1-proteinase inhibitor on the activity of elastase from polymorphonuclear granulocytes (PMN-elastase) was tested under various conditions. The synthetic substrate methoxysuccinyl-1-ala-1-pro-1-val-p-nitroaniline was used to measure the activity of the enzyme. The inhibition or activation of PMN-elastase by the test substances was dependent on the type and concentration of buffer, the pH, the presence of a tenside and most notably, the presence of electrolytes. Components of the synovial fluid changed the effects of these electrolytes. Therefore, it is as yet unclear, to what degree the inhibition of PMN-elastase contributes to the therapeutical effects of non-steroidal anti-inflammatory drugs and anti-osteoarthritic drugs.
在不同条件下，测试了双氯芬酸钠、硫酸化糖胺聚糖（GAGPS）、依林C和α1-蛋白酶抑制剂对多形核粒细胞弹性蛋白酶（PMN-弹性蛋白酶）活性的影响。使用合成底物甲氧基琥珀酰-1-丙氨酸-1-脯氨酸-1-缬氨酸-对硝基苯胺来测定该酶的活性。测试物质对PMN-弹性蛋白酶的抑制或激活作用取决于缓冲液的类型和浓度、pH值、表面活性剂的存在，最显著的是电解质的存在。滑液成分改变了这些电解质的作用。因此，目前尚不清楚PMN-弹性蛋白酶的抑制在多大程度上有助于非甾体抗炎药和抗骨关节炎药物的治疗效果。
