HUMAN-PLATELET AGGREGATION INDUCED BY 1-ALKYL-LYSOPHOSPHATIDIC ACID AND ITS ANALOGS - A NEW GROUP OF PHOSPHOLIPID MEDIATORS
HUMAN-PLATELET AGGREGATION INDUCED BY 1-ALKYL-LYSOPHOSPHATIDIC ACID AND ITS ANALOGS - A NEW GROUP OF PHOSPHOLIPID MEDIATORS
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DOI：
10.1016/s0006-291x(82)80113-7
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发表时间：
1982-01-01
影响因子：
3.1
通讯作者：
DOUSTEBLAZY, L
中科院分区：
文献类型：
--
作者：
SIMON, MF;CHAP, H;DOUSTEBLAZY, L
合成了四种溶血磷脂酸（LPA）的醚类化合物。它们包括1-十六烷基-sn-甘油基-3-磷酸酯（1-Hx-GPA）、1-十六烷基-2-乙酰基-sn-甘油基-3-磷酸酯（1-Hx-2-Ac-GPA）和它们各自的对映异构体。4种化合物均能促进人血小板聚集。1-Hx-GPA比血小板活化因子（PAF-acether）的效力低10倍，但比1-棕榈酰-sn-甘油基-3-磷酸（1-P-GPA）的效力高30倍。4个化合物没有显示出任何强的立体特异性，2-羟基的乙酰化对于完全活性不是必需的。血小板对1-Hx-GPA均表现出特异性脱敏作用，但对PAF-乙酰醚无明显脱敏作用。显然，LPA的醚类似物代表了一组新的强大的磷脂介质，其作用机制与PAF-乙酰醚不同。
Four ether analogs of lysophosphatidic acids (LPA) were prepared. They include 1-hexadecyl-sn-glyceryl-3-phosphate (1-Hx-GPA), 1-hexadecyl-2-acetyl-sn-glyceryl-3-phosphate (1-Hx-2-Ac-GPA) and their respective enantiomers. The 4 compounds promoted human platelet aggregation. 1-Hx-GPA was 10 times less potent than platelet activating factor (PAF-acether), but 30 times more powerful than 1-palmitoyl-sn-glyceryl-3-phosphate (1-P-GPA). The 4 compounds did not display any strong stereospecificity and acetylation of the 2-hydroxyl-group was not essential for full activity. They all displayed specific platelet desensitization to 1-Hx-GPA, but not to PAF-acether. Evidently, ether analogs of LPA represent a new group of powerful phospholipid mediators acting by a mechanism in some way different from that of PAF-acether.