人类风湿性滑膜微粒体中的前列腺素合成酶活性。“阿司匹林样”药物治疗的影响。
Prostaglandin synthetase activity from human rheumatoid synovial microsomes. Effect of 'aspirin-like' drug therapy.
作者信息
Crook D, Collins A J, Bacon P A, Chan R
出版信息
Ann Rheum Dis. 1976 Aug;35(4):327-32. doi: 10.1136/ard.35.4.327.
Abstract
Using a radiometric technique, prostaglandin synthetase activity was measured in vitro in the microsomal fraction of 19 synovial tissues taken from 17 rheumatoid arthritis patients. The enzyme was inhibited in vitro by low concentrations of several 'aspirin-like' drugs, though paracetamol and salicylic acid were virtually inactive. While the synthetase preparations from patients receiving indomethacin, ibuprofen, or naproxen therapy exhibited considerable activity in vitro, we were unable to show any activity in preparations from patients taking aspirin, even in low doses. These findings suggest that in vivo aspirin may be unique in being an irreversible inhibitor of the enzyme, compared with other 'aspirin-like' drugs.
摘要
采用放射测量技术，对取自17例类风湿性关节炎患者的19个滑膜组织微粒体部分的前列腺素合成酶活性进行了体外测定。低浓度的几种“阿司匹林样”药物在体外可抑制该酶，不过对乙酰氨基酚和水杨酸实际上无活性。虽然接受吲哚美辛、布洛芬或萘普生治疗患者的合成酶制剂在体外表现出相当高的活性，但我们未能在服用阿司匹林患者的制剂中检测到任何活性，即使是低剂量时也未检测到。这些发现表明，与其他“阿司匹林样”药物相比，阿司匹林在体内可能是该酶的一种不可逆抑制剂，具有独特性。
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Prostaglandin synthetase activity from human rheumatoid synovial microsomes. Effect of 'aspirin-like' drug therapy.人类风湿性滑膜微粒体中的前列腺素合成酶活性。“阿司匹林样”药物治疗的影响。
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