Thomas M J, O'Flaherty J T, Cousart S, McCall C E
Prostaglandins. 1982 Feb;23(2):265-72. doi: 10.1016/0090-6980(82)90054-5.
The following racemic hydroxyicosatetraenoic acids were prepared and assayed for their ability to stimulate hexose transport in human polymorphonuclear leukocytes: 15-, 12-, 11-, 9-, 8-, and 5-hydroxyicosatetraenoic acids. The compounds were isolated from reduced, autoxidized arachidonic acid. The results demonstrate that only the 12- and 5-hydroxyicosatetraenoic acids are biologically active inducing half-maximal responses at 820 and 176 nM, respectively. Thus, the bioactions of hydroxicosatetraenoates ae crucially dependent upon the position of the hydroxy residue. Response to both hydroxyicosatetraenoates was effectively blocked by two inhibitors of arachidonic acid metabolism: nordihydroguaiaretic acid and indomethacin. A third arachidonic acid antimetabolite, 5, 8, 11, 14-eicosatetraynoic acid, completely inhibited the response to 12-HETE but caused only partial inhibition of the response to 5-HETE.
制备了以下外消旋羟基二十碳四烯酸，并检测了它们刺激人多形核白细胞中己糖转运的能力：15-、12-、11-、9-、8-和5-羟基二十碳四烯酸。这些化合物是从还原的、自氧化的花生四烯酸中分离出来的。结果表明，只有12-和5-羟基二十碳四烯酸具有生物活性，分别在820和176 nM时诱导出半数最大反应。因此，羟基二十碳四烯酸酯的生物作用关键取决于羟基残基的位置。花生四烯酸代谢的两种抑制剂：去甲二氢愈创木酸和吲哚美辛有效地阻断了对两种羟基二十碳四烯酸酯的反应。第三种花生四烯酸抗代谢物，5,8,11,14-二十碳四炔酸，完全抑制了对12-HETE的反应，但仅部分抑制了对5-HETE的反应。
