Willems C, De Groot P G, Pool G A, Gonsalvez M S, Van Aken W G, Van Mourik J A
Biochim Biophys Acta. 1982 Dec 13;713(3):581-8. doi: 10.1016/0005-2760(82)90318-6.
The effect of acetylsalicylic acid on endothelial prostaglandin synthesis was measured in the presence of exogenous and endogenous substrates. In both types of measurement, a rate of inhibition was found similar to that observed for acetylsalicylic acid inhibition of cyclooxygenase activity in platelets. After withdrawal of acetylsalicylic acid, a rapid restoration of cyclooxygenase activity was observed when exogenous [1-14C]arachidonate was used as a substrate (50% of initial activity at 5 h). However, when endogenous substrate, released after phospholipase activation induced by thrombin treatment of the cells, was used to test cyclooxygenase activity, only partial restoration of enzymic activity was observed (30% after 48 h). Phospholipase activity, measured by the release of free fatty acids, was not inhibited by acetylsalicylic acid. Measurement of turnover times by incubating the cells with cycloheximide revealed a short turnover time for the enzymic activity tested with exogenous [1-14C]arachidonate (2.3 h) and a relatively long turnover time for the cyclooxygenase activity tested with endogenous substrate released after thrombin treatment of the cells (54 h). These results suggest that at least two pools of cycloxygenase are involved in endothelial prostaglandin synthesis.
在存在外源性和内源性底物的情况下,测定了乙酰水杨酸对内皮细胞前列腺素合成的影响。在这两种测量类型中,发现抑制率与在血小板中观察到的乙酰水杨酸对环氧化酶活性的抑制率相似。停用乙酰水杨酸后,当使用外源性[1-14C]花生四烯酸作为底物时,观察到环氧化酶活性迅速恢复(5小时时为初始活性的50%)。然而,当使用经凝血酶处理细胞诱导磷脂酶激活后释放的内源性底物来测试环氧化酶活性时,仅观察到酶活性部分恢复(48小时后为30%)。通过游离脂肪酸释放来测量的磷脂酶活性不受乙酰水杨酸抑制。用环己酰亚胺孵育细胞来测量周转时间,结果显示用外源性[1-14C]花生四烯酸测试的酶活性周转时间较短(2.3小时),而用经凝血酶处理细胞后释放的内源性底物测试的环氧化酶活性周转时间相对较长(54小时)。这些结果表明,内皮细胞前列腺素合成中至少涉及两个环氧化酶池。