Söling U, Eibl H, Nagel G A, Unger C
Department of Hematology and Oncology, University of Göttingen, Federal Republic of Germany.
Lipids. 1987 Nov;22(11):868-70. doi: 10.1007/BF02535546.
1-O-Hexadecyl-2-O-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor, PAF) is known to stimulate platelet aggregation and serotonin release in concentrations ranging from 10(-10)-10(-5) M. Since a variety of synthetic PAF analogues are potent antineoplastic agents in vitro and in vivo, it was the aim of this study to examine the PAF-like activity of 15 analogues, including 1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine (ET-18-OCH3) and a thioether analogue. In platelet-rich plasma from human blood, platelet aggregation and serotonin release were studied to compare the effects of PAF and the analogues. Platelet function was controlled by testing their response to adenosine diphosphate, arachidonic acid, collagen and epinephrine. Our results show that only PAF was able to induce platelet aggregation and serotonin release in concentrations from 10(-9) to 10(-5) M, whereas all the tested analogues up to a concentration of 10(-3) M failed to induce these effects.
1-十六烷基-2-乙酰基-sn-甘油-3-磷酸胆碱（血小板活化因子，PAF）已知在浓度范围为10^(-10)-10^(-5)M时能刺激血小板聚集和5-羟色胺释放。由于多种合成PAF类似物在体外和体内都是有效的抗肿瘤药物，本研究的目的是检测15种类似物的PAF样活性，包括1-十八烷基-2-甲基-外消旋甘油-3-磷酸胆碱（ET-18-OCH3）和一种硫醚类似物。在人血富含血小板的血浆中，研究血小板聚集和5-羟色胺释放以比较PAF和类似物的作用。通过测试它们对二磷酸腺苷、花生四烯酸、胶原和肾上腺素的反应来控制血小板功能。我们的结果表明，只有PAF能够在浓度为10^(-9)至10^(-5)M时诱导血小板聚集和5-羟色胺释放，而所有测试的类似物在浓度高达10^(-3)M时都未能诱导这些效应。
