Inhibition of lipid mediator biosynthesis in human inflammatory cells by BIRM 270.

T P Parks, A F Hoffman, C A Homon, A G Graham, E S Lazer, F H Chilton, P Borgeat, D Raible, E Schulman, D A Bass
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引用次数: 1

Abstract

BIRM 270 was developed as a potent and enantioselective inhibitor of LTB4 biosynthesis by human neutrophils, and was also found to inhibit LTC4 production by human eosinophils and lung mast cells. BIRM 270 inhibited LTB4 synthesis in neutrophils by preventing arachidonate release from membrane phospholipids, and over the same concentration range, inhibited PAF biosynthesis. BIRM 270 did not directly inhibit acylhydrolases which have been implicated in eicosanoid and PAF biosynthesis, suggesting an indirect mode of action.

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birm270对人炎症细胞脂质介质生物合成的抑制作用
BIRM 270是人类中性粒细胞合成LTB4的一种有效的对体选择性抑制剂,也被发现可以抑制人嗜酸性粒细胞和肺肥大细胞产生LTC4。BIRM 270通过阻止膜磷脂释放花生四烯酸抑制中性粒细胞LTB4的合成,在相同浓度范围内抑制PAF的生物合成。birm270不直接抑制与类二十烷酸和PAF生物合成有关的酰基水解酶,表明其作用方式是间接的。
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