Seyberth H W, Oelz O, Kennedy T, Sweetman B J, Danon A, Frölich J C, Heimberg M, Oates J A
Clin Pharmacol Ther. 1975 Nov;18(5 Pt 1):521-9. doi: 10.1002/cpt1975185part1521.
Ethyl arachidonate was administered orally to 4 healthy male volunteers in a dose of 6 gm daily for a 2 to 3 wk period after 10-day control period. The increased intake of this precursor of the dienoic prostaglandins resulted in significant increases in the relative and absolute amount of arachidonate in plasma triglycerides, phospholipids, and cholesteryl esters. Similar changes in lipid composition were noted in platelets. The excretion of 7alpha-hydroxy-5,11-diketotetranoprostane-1,16-dioic acid, the major urinary metabolite of E prostaglandins in man, was increased by an average of 47% in 3 of the 4 volunteers. Platelet reactivity was assessed by determining the threshold concentration of adenosine diphosphate (ADP) necessary to induce secondary, irreversible aggregation of platelet-rich plasma. This threshold concentration dropped significantly in all volunteers (10% to 60% of control values). It is concluded that the biosynthesis and function of prostaglandins can be augmented in man by oral administration of an esterified precursor fatty acid.
在为期10天的对照期后，向4名健康男性志愿者口服花生四烯酸乙酯，剂量为每日6克，持续2至3周。这种二烯前列腺素前体摄入量的增加导致血浆甘油三酯、磷脂和胆固醇酯中花生四烯酸的相对量和绝对量显著增加。血小板中也观察到了类似的脂质组成变化。人前列腺素E的主要尿液代谢产物7α-羟基-5,11-二酮四氢前列腺素-1,16-二酸的排泄量在4名志愿者中的3名中平均增加了47%。通过测定诱导富含血小板血浆继发性、不可逆聚集所需的二磷酸腺苷（ADP）阈值浓度来评估血小板反应性。所有志愿者的该阈值浓度均显著下降（降至对照值的10%至60%）。结论是，口服酯化前体脂肪酸可增强人体内前列腺素的生物合成和功能。
