Kaneko M, Suzuki K, Furui H, Takagi K, Satake T
2nd Department of Internal Medicine, Nagoya University School of Medicine, Japan.
Arzneimittelforschung. 1990 Jan;40(1):91-4.
The effect of the new orally active antiallergic compound ethyl 2-(4'-carboxybenzamido)-4-propionamidobenzoate sodium salt (AM-682) and its main metabolite (met-A) were evaluated on respiratory burst in isolated human polymorphonuclear neutrophils (PMN). Both compounds exhibited inhibitory effect with concentration dependency on the n-formyl-methionyl-leucyl-phenylalanine (FMLP)-induced superoxide (O-2) production by human PMN. The inhibitory activity of met-A (IC50 1.1 mumol/l) was higher than that of AM-682 (IC50 85 mumol/l). By contrast, these compounds affected neither PMN O-2 production induced by phorbol 12-myristate 13-acetate (PMA) nor extracellular O-2 generation by the reaction of xanthine oxidase with hypoxanthine. These results indicate that the effects of these compounds act specifically on the generation of O-2 and is not simply a scavenger of O-2. This anti-inflammatory effect may also be beneficial in the treatment of asthma.
新型口服活性抗过敏化合物2-（4'-羧基苯甲酰胺基）-4-丙酰胺基苯甲酸钠盐（AM-682）及其主要代谢产物（met-A）对分离的人多形核中性粒细胞（PMN）呼吸爆发的影响进行了评估。两种化合物均对人PMN由N-甲酰甲硫氨酰-亮氨酰-苯丙氨酸（FMLP）诱导的超氧化物（O₂）产生表现出浓度依赖性抑制作用。met-A的抑制活性（IC₅₀ 1.1 μmol/L）高于AM-682（IC₅₀ 85 μmol/L）。相比之下，这些化合物既不影响佛波醇12-肉豆蔻酸酯13-乙酸酯（PMA）诱导的PMN O₂产生，也不影响黄嘌呤氧化酶与次黄嘌呤反应产生的细胞外O₂。这些结果表明，这些化合物的作用特异性地作用于O₂的产生，而不仅仅是O₂的清除剂。这种抗炎作用在哮喘治疗中可能也有益处。
