Tence M, Coëffier E, Polonsky J, Benveniste J
Biochim Biophys Acta. 1983 Feb 22;755(3):526-30. doi: 10.1016/0304-4165(83)90260-x.
We have compared for rabbit platelet aggregating and desensitizing activity two different preparations of platelet-activating factor (PAF-acether) (1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine) and of its enantiomer (3-O-alkyl-2-O-acetyl-sn-glycero-1-phosphocholine). After phospholipase A2 treatment, the unnatural enantiomers appeared about 3000-fold less active than PAF-acether, a result which definitively establishes the stereospecificity of the mode of action of this mediator. A new structural analog of PAF-acether, 1-O-hexadecyl-3-O-acetyl-sn-glycero-2-phosphocholine, was isolated and characterized. It was a weak platelet agonist, stressing further the importance for PAF-acether activity of the acetyl group at position 2 of the glycerol.
我们比较了两种不同的血小板激活因子（PAF-乙醚）（1-O-烷基-2-O-乙酰基-sn-甘油-3-磷酸胆碱）及其对映体（3-O-烷基-2-O-乙酰基-sn-甘油-1-磷酸胆碱）对兔血小板聚集和脱敏的活性。经磷脂酶A2处理后，非天然对映体的活性比PAF-乙醚低约3000倍，这一结果明确证实了该介质作用方式的立体特异性。分离并鉴定了一种新的PAF-乙醚结构类似物，即1-O-十六烷基-3-O-乙酰基-sn-甘油-2-磷酸胆碱。它是一种弱血小板激动剂，进一步强调了甘油2位乙酰基对PAF-乙醚活性的重要性。
