Bustos G, Ferrándiz M L, Sanz M J, Payá M, Alcaraz M J
Departamento de Farmacología, Universidad de Valencia, Facultad de Farmacia, Spain.
Naunyn Schmiedebergs Arch Pharmacol. 1995 Mar;351(3):298-304. doi: 10.1007/BF00233250.
We have evaluated the effects of the novel anti-inflammatory agent florifenine, 2-(1-Pyrrolidinyl)ethyl N-[7-(trifluoromethyl)-4-quinolyl]anthranilate, on topical inflammation in mice, free radical-mediated reactions, arachidonic acid metabolism and some neutrophil functions. Topical administration of florifenine produced dose-related anti-inflammatory activity in 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced ear oedema and with a lower potency, in the response induced by arachidonic acid (AA). Florifenine also inhibited neutrophil migration and PGE2 content in the inflammed ears. In human whole blood, florifenine was a potent and selective inhibitor of TXB2 generation. This anti-inflammatory agent did not exert antioxidant effects but inhibited elastase release in human neutrophils without affecting superoxide anion generation. Florifenine administration to mice dose-dependently inhibited leukocyte migration and PGE2 levels in the air pouch inflammation induced by zymosan. These results demonstrate the topical anti-inflammatory activity of florifenine and provide a basis for understanding the mechanisms involved in the inhibitory effects of this agent on inflammatory responses.
我们评估了新型抗炎药氟立芬宁（2-(1-吡咯烷基)乙基 N-[7-(三氟甲基)-4-喹啉基]邻氨基苯甲酸）对小鼠局部炎症、自由基介导的反应、花生四烯酸代谢及一些中性粒细胞功能的影响。局部给予氟立芬宁在 12-O-十四烷酰佛波醇-13-乙酸酯（TPA）诱导的耳水肿中产生剂量相关的抗炎活性，且在花生四烯酸（AA）诱导的反应中效力较低。氟立芬宁还抑制中性粒细胞迁移及炎症耳部的 PGE2 含量。在人全血中，氟立芬宁是 TXB2 生成的强效选择性抑制剂。这种抗炎药不发挥抗氧化作用，但抑制人中性粒细胞中的弹性蛋白酶释放而不影响超氧阴离子生成。给小鼠施用氟立芬宁剂量依赖性地抑制酵母聚糖诱导的气袋炎症中的白细胞迁移和 PGE2 水平。这些结果证明了氟立芬宁的局部抗炎活性，并为理解该药物对炎症反应抑制作用的机制提供了依据。
