蛋白激酶C抑制剂GF 109 203X对人中性粒细胞弹性蛋白酶释放和呼吸爆发的影响。

Effect of the protein kinase C inhibitor GF 109 203X on elastase release and respiratory burst of human neutrophils.

Cabanis A, Gressier B, Brunet C, Dine T, Luyckx M, Cazin M, Cazin J C

Faculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Lille, France.

Gen Pharmacol. 1996 Dec;27(8):1409-14. doi: 10.1016/s0306-3623(96)00053-5.

The effects of bisindolylmaleimide GF 109 203X, reported to be a potent and highly selective inhibitor of protein kinase C (PKC), have been investigated on some human neutrophil functions. 2. GF 109 203X prevented O.2- production by NADPH-oxidase whatever the stimulus used for polymorphonuclear neutrophil (PMN) activation: directs PKC activators like phorbol myristate acetate (PMA) and dioctanoylglycerol, calcium ionophore (A23187), or receptor agonists like fMet-Leu-Phe (fMLP) and opsonized zymosan. 3. The effect of GF 109 203X was also examined on elastase exocytosis by neutrophils. PMA-mediated release was prevented by GF 109 203X. However, GF 109 203X had no effect on exocytosis induced by A23187 and the effect of this compound on the fMLP response changed according to its concentration. 4. These data suggest that PKC might be essential for stimulus-mediated O.2- production and also that PKC plays only a minor role in elastase secretion as compared to the role of the cytosolic calcium level.

据报道，双吲哚马来酰亚胺GF 109 203X是一种强效且高度选择性的蛋白激酶C（PKC）抑制剂，已对其对一些人类中性粒细胞功能的影响进行了研究。2. 无论用于多形核中性粒细胞（PMN）激活的刺激物是什么，GF 109 203X都能阻止NADPH氧化酶产生超氧阴离子（O₂⁻）：直接的PKC激活剂，如佛波醇肉豆蔻酸酯乙酸酯（PMA）和二辛酰甘油，钙离子载体（A23187），或受体激动剂，如N-甲酰甲硫氨酰-亮氨酰-苯丙氨酸（fMLP）和调理酵母聚糖。3. 还研究了GF 109 203X对中性粒细胞弹性蛋白酶胞吐作用的影响。GF 109 203X可阻止PMA介导的释放。然而，GF 109 203X对A23187诱导的胞吐作用没有影响，并且该化合物对fMLP反应的影响根据其浓度而变化。4. 这些数据表明，PKC可能对刺激介导的O₂⁻产生至关重要，并且与胞质钙水平的作用相比，PKC在弹性蛋白酶分泌中仅起次要作用。

Effect of the protein kinase C inhibitor GF 109 203X on elastase release and respiratory burst of human neutrophils.