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体外抑制脂氧合酶活性的药物的体内抗过敏和抗炎作用

In vivo anti-allergic and anti-inflammatory effects of drugs that inhibit lipoxygenase activity in vitro.

作者信息

Etienne A, Soulard C, Touvay C, Clostre F, Braquet P

出版信息

Int J Tissue React. 1985;7(6):459-62.

PMID:3936815
Abstract

Studies in vitro have already shown that the chemotactic effect of leukotriene LTB4, as well as its pro-aggregatory effect on a suspension of leukocytes, could be inhibited by the lipoxygenase (LO) inhibitor ETYA; moreover a beneficial effect of another LO-inhibitor, diethylcarbamazine, has been shown on experimental asthma. To explore a possible therapeutic application of substances that inhibit 15-LO of soybean in vitro, we have tested several active compounds, namely nordihydroguaiaretic acid (NDGA), phenidone, diethylcarbamazine and mefenamic acid, on the following in vivo inflammation models in the rat: plantar oedema induced by carrageenin; cutaneous vascular hyperpermeability induced by pafacether; pleurisy induced by carrageenin. The correlation between the LO-inhibitor effect of these compounds in vitro and their beneficial effects in the different tests that were performed, as well as the mechanisms of action induced in the different experimental models, are discussed.

摘要

体外研究已经表明,白三烯LTB4的趋化作用及其对白细胞悬液的促聚集作用可被脂氧合酶(LO)抑制剂ETYA抑制;此外,另一种LO抑制剂乙胺嗪对实验性哮喘已显示出有益作用。为了探索体外抑制大豆15-LO的物质的可能治疗应用,我们在大鼠的以下体内炎症模型中测试了几种活性化合物,即去甲二氢愈创木酸(NDGA)、非那宗、乙胺嗪和甲芬那酸:角叉菜胶诱导的足跖水肿;帕法酰基醚诱导的皮肤血管通透性增加;角叉菜胶诱导的胸膜炎。讨论了这些化合物在体外的LO抑制作用与其在不同测试中的有益作用之间的相关性,以及在不同实验模型中诱导的作用机制。

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