Walenga R, Vanderhoek J Y, Feinstein M B
J Biol Chem. 1980 Jul 10;255(13):6024-7.
Serine esterase inhibitors (phenylmethanesulfonyl fluoride, 5-dimethylaminonaphthalene-1-sulfonyl (dansyl) fluoride, 2-nitro-4-carboxyphenyl-N,N-diphenylcarbamate, or p-nitrophenyl anthranilate) blocked the production of malonyldialdehyde by platelets induced with a variety of stimuli (including thrombin, trypsin, collagen, and A23187). These inhibitors did not block malonyldialdehyde production by platelets from exogenous arachidonic acid. Those inhibitors studied in greater detail (phenylmethanesulfonyl fluoride and 2-nitro-4-carboxyphenyl-N,N-diphenylcarbamate) were shown to inhibit the release of [1-14C]arachidonic acid from phosphatidylinositol and phosphatidylcholine in intact platelets but not the conversion of arachidonic acid to thromboxanes, prostaglandins, or hydroxyfatty acids. These inhibitors also blocked the stimulus-induced production of [32P]phosphatidic acid in intact platelets. Both arachidonic acid release from phosphatidylinositol and phosphatidic acid production have been reported to depend on the production of diglyceride by the action on the phosphatidylinositol-specific phospholipase C.f a phosphatidylinositol-specific phospholipase C. That enzyme in the soluble fraction from disrupted platelets was inhibited at concentrations of serine esterase inhibitors which block arachidonic acid release in intact platelets. These results indicate that serine esterase inhibitors block the stimulus-induced mobilization of arachidonic acid in platelets at least in part by their action o
丝氨酸酯酶抑制剂（苯甲基磺酰氟、5-二甲基氨基萘-1-磺酰氟、2-硝基-4-羧基苯基-N,N-二苯基氨基甲酸酯或对硝基苯基邻氨基苯甲酸）可阻断多种刺激物（包括凝血酶、胰蛋白酶、胶原和A23187）诱导的血小板丙二醛生成。这些抑制剂不会阻断外源性花生四烯酸诱导的血小板丙二醛生成。对研究更深入的那些抑制剂（苯甲基磺酰氟和2-硝基-4-羧基苯基-N,N-二苯基氨基甲酸酯）进行检测，结果显示其可抑制完整血小板中花生四烯酸从磷脂酰肌醇和磷脂酰胆碱的释放，但不会抑制花生四烯酸向血栓烷、前列腺素或羟基脂肪酸的转化。这些抑制剂还可阻断完整血小板中刺激诱导的[32P]磷脂酸生成。据报道，磷脂酰肌醇释放花生四烯酸和磷脂酸生成均依赖于磷脂酰肌醇特异性磷脂酶C作用产生甘油二酯。在完整血小板中能阻断花生四烯酸释放的丝氨酸酯酶抑制剂浓度下，可抑制破碎血小板可溶部分中的该酶活性。这些结果表明，丝氨酸酯酶抑制剂至少部分通过其作用阻断刺激诱导的血小板花生四烯酸动员
