Maderazo E G, Breaux S P, Woronick C L
J Pharm Sci. 1984 Oct;73(10):1403-6. doi: 10.1002/jps.2600731020.
The stimulation of cell swelling, cell aggregation, polymorphonuclear leukocyte locomotion, and lysosomal enzyme release in response to chemoattractant were all inhibited by ibuprofen, a nonsteroidal anti-inflammatory agent. The dosages needed to induce 50% inhibition (ID50) were 5.9, 7.6, 60, and 95 micrograms/mL, respectively. Aside from the differences in ID50, there was also a difference in the degree of maximum inhibition (Imax) of the complement C5a-stimulated responses observed, so that at achievable serum drug concentrations of 20-50 micrograms/mL, inhibition of 67-78% for cell swelling, 69-82% for cell aggregation, 20-35% for migration response, and 17-38% for lysosomal enzyme release were demonstrated. Also observed were a minor stimulatory effect on nitroblue tetrazolium reduction and an inhibitory effect on the ability to kill Staphylococcus aureus, but only at very high concentrations (approximately 2 mg/mL).
非甾体抗炎药布洛芬可抑制因趋化因子刺激引起的细胞肿胀、细胞聚集、多形核白细胞移动以及溶酶体酶释放。诱导50%抑制率(ID50)所需的剂量分别为5.9、7.6、60和95微克/毫升。除了ID50存在差异外,观察到的补体C5a刺激反应的最大抑制程度(Imax)也存在差异,因此在血清药物浓度达到20 - 50微克/毫升时,细胞肿胀的抑制率为67 - 78%,细胞聚集的抑制率为69 - 82%,迁移反应的抑制率为20 - 35%,溶酶体酶释放的抑制率为17 - 38%。还观察到对硝基蓝四氮唑还原有轻微刺激作用,对杀灭金黄色葡萄球菌的能力有抑制作用,但仅在非常高的浓度(约2毫克/毫升)时出现。