Heymans F, Michel E, Borrel M C, Wichrowski B, Godfroid J J, Convert O, Coeffier E, Tence M, Benveniste J
Biochim Biophys Acta. 1981 Nov 23;666(2):230-7. doi: 10.1016/0005-2760(81)90112-0.
A new method of synthesis of octadecyl platelet-activating factor (PAF; 1-O-octadecyl 2-O-acetyl sn-glycero-3-phosphorylcholine) is described. Its advantage is to proceed by way of the 'lyso-PAF' which may be substituted by various groups, while avoiding the inconveniences of the total synthesis already described. Moreover, the intermediates in synthesis are easier to purify, with better yields. The platelet-aggregating activity of synthetic PAF, is enantiomer (3-O-octadecyl) and racemic mixtures were 2.7 . 10(-10), 1.7 . 10(-7) and 2.2 . 10(-10) M, respectively. These results indicate the stereospecificity of platelet activation induced by PAF.
描述了一种合成十八烷基血小板活化因子(PAF;1-O-十八烷基 2-O-乙酰基-sn-甘油-3-磷酸胆碱)的新方法。其优点是通过“溶血 PAF”的方式进行,“溶血 PAF”可被各种基团取代,同时避免了已描述的全合成的不便之处。此外,合成中的中间体更容易纯化,产率更高。合成的 PAF、对映体(3-O-十八烷基)和外消旋混合物的血小板聚集活性分别为 2.7×10⁻¹⁰、1.7×10⁻⁷ 和 2.2×10⁻¹⁰ M。这些结果表明了 PAF 诱导血小板活化的立体特异性。