吡利前列素(U-60,257)对人血小板和中性粒细胞功能的抑制作用

J.L. Mehta, P. Mehta, M.B. Ward, D. Lawson
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引用次数: 5

摘要

血小板和中性粒细胞在确定冠状动脉闭塞后心肌损伤程度方面很重要。这些血液元素的有害影响部分是通过花生四烯酸代谢物和氧化物质的释放介导的。一种新的选择性白三烯形成抑制剂,匹利前列素(U-60,257),在实验动物中被观察到可以减少心肌中性粒细胞的积累和冠状动脉结扎后的梗死面积。由于吡利前列素可能有临床应用,我们研究了它对人血小板和中性粒细胞功能的影响。该化合物对肾上腺素诱导的人血小板聚集和TXA2生物合成有明显的抑制作用(IC50为0.04μM)。吡前列素对人中性粒细胞趋化、氧化物质释放、聚集和LTB4合成的抑制作用IC50分别为0.1、0.04、10和14 μM。因此,匹利前列素抑制多种人类血小板和中性粒细胞功能。由于其对人血小板和中性粒细胞功能的抑制作用以及对实验性心肌梗死的保护作用,该药物可能具有临床应用价值。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Inhibition of human platelet and neutrophil function by piriprost (U-60,257)

Platelets and neutrophils are important in determining the extent of myocardial injury following coronary occlusion. The detrimental effects of these blood elements are mediated in part via release of arachidonate metabolites and oxidative species. A new selective inhibitor of leukotriene formation, piriprost (U-60,257), has been observed to decrease both neutrophil accumulation in the myocardium and infarct size following coronary ligation in experimental animals. Since piriprost may have clinical use, we examined its effects on human platelet and neutrophil functions. This compound was found to exert potent inhibitory effects on epinephrine-induced human platelet aggregation and TXA2 biosynthesis (IC50 0.04μM). Piriprost also inhibited human neutrophil chemotaxis, oxidative species release, aggregation, and LTB4 synthesis with IC50 of 0.1, 0.04, 10 and 14 μM, respectively. Thus, piriprost inhibits a variety of human platelet and neutrophil functions. Because of its suppressive effects on human platelet and neutrophil functions and protective effects in experimental myocardial infarction, this agent may have clinical applications.

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