Pong S S, Levine L
J Pharmacol Exp Ther. 1976 Jan;196(1):226-30.
Prostaglandin synthetase activities in the microsomal fractions of seven rabbit tissues have been partially characterized. All of the microsomal preparations required arachidonic acid, hydroquinone and reduced glutathione for enzymatic activity. The synthetic systems of the renal medulla were most active followed by microsomal preparations from the renal cortex, lung, brain, spleen, uterus and heart. Three structurally distinct nonsteroidal anti-inflammatory drugs, indomethacin, flufenamic acid and aspirin, inhibited the production of prostaglandins by these microsomes. The effectiveness of these drugs depended on the concentration of substrate. When assayed under identical experimental conditions, the inhibiting activity of each of these drugs for the synthetase of each of the tissues was the same.
已对七种兔组织微粒体部分中的前列腺素合成酶活性进行了部分表征。所有微粒体制剂的酶活性都需要花生四烯酸、对苯二酚和还原型谷胱甘肽。肾髓质的合成系统活性最高,其次是来自肾皮质、肺、脑、脾、子宫和心脏的微粒体制剂。三种结构不同的非甾体抗炎药,吲哚美辛、氟芬那酸和阿司匹林,抑制了这些微粒体产生前列腺素。这些药物的有效性取决于底物浓度。在相同实验条件下进行测定时,这些药物对每种组织合成酶的抑制活性相同。