中性粒细胞白三烯A4水解酶和白三烯B4受体：白三烯环氧化物及其酶促产物的作用

Neutrophil LTA4 hydrolases and leukotriene B4 receptors: effects of leukotriene epoxides and their enzymatic products.

作者信息

Evans J, Nathaniel D, Charleson S, Léveillé C, Zamboni R, Leblanc Y, Frenette R, Fitzsimmons B J, Leger S, Hamel P

出版信息

Prostaglandins Leukot Med. 1986 Aug;23(2-3):167-71. doi: 10.1016/0262-1746(86)90181-2.

PMID:3020583

Abstract

A selection of inhibitors of rat and human neutrophil LTA4 hydrolases have been studied in vitro using partially purified enzymes. 5(S)trans 5,6 oxido-7,9-trans-11-cis-eicosatrienoic acid (LTA3) and 5(S)trans 5,6 oxido, 7,9-trans, 11,14,17-cis-eicosapentaenoic acid (LTA5) have been shown to inhibit neutrophil LTA4 hydrolases in a time-dependent manner. The products of hydrolysis of LTA3, LTA4 and LTA5 by human and rat neutrophil LTA4 hydrolase have been shown to displace [3H] LTB4 binding to human and rat neutrophil membranes. The order of displacement of [3H] LTB4 is LTB4 = LTB3 greater than LTB5 and this correlated well with their biological potencies for enhancement of neutrophil aggregation and chemokinesis.

摘要

利用部分纯化的酶，在体外对一系列大鼠和人中性粒细胞白三烯A4水解酶抑制剂进行了研究。已证明5(S)反式5,6-环氧-7,9-反式-11-顺式二十碳三烯酸（LTA3）和5(S)反式5,6-环氧、7,9-反式、11,14,17-顺式二十碳五烯酸（LTA5）以时间依赖性方式抑制中性粒细胞白三烯A4水解酶。已证明人及大鼠中性粒细胞白三烯A4水解酶对LTA3、LTA4和LTA5的水解产物可取代[3H]白三烯B4与人及大鼠中性粒细胞膜的结合。[3H]白三烯B4的取代顺序为白三烯B4 = 白三烯B3大于白三烯B5，这与它们增强中性粒细胞聚集和趋化运动的生物学活性密切相关。