阿司匹林和二氟尼柳对人血小板及羊精囊前列腺素合成酶的比较作用
Comparative effects of aspirin and diflunisal on prostaglandin synthetase from human platelets and sheep seminal vesicles.
作者信息
Majerus P W, Stanford N
出版信息
Br J Clin Pharmacol. 1977 Feb;4 Suppl 1(Suppl 1):15S-18S. doi: 10.1111/j.1365-2125.1977.tb04509.x.
Abstract
- We have compared the effects of diflunisal on prostaglandin (PG) synthetase from human platelets and sheep seminal vesicles (SSV) by measuring malonaldehyde, PG products, and rabbit aorta contraction. 2. Aspirin inhibits PG synthetase by covalently acetylating the enzyme. Inhibition is dependent on time and aspirin concentration. Aspirin is 37-fold more potent in inhibiting enzyme in human platelets compared with enzyme from SSV. 3. Diflunisal inhibits PG synthetase from intact human platelets and SSV equally (50% inhibition at 3-5 micronM). The drug does not covalently modify the enzyme, and inhibition is not time dependent. Diflunisal probably acts at a site similar to aspirin since the drug will inhibit acetylation of the enzyme by aspirin. 4. The results suggest that diflunisal is relatively less inhibitory to platelet function than is aspirin.
摘要
- 我们通过测量丙二醛、前列腺素（PG）产物以及兔主动脉收缩情况，比较了双氟尼酸对人血小板和羊精囊（SSV）中前列腺素（PG）合成酶的影响。2. 阿司匹林通过对该酶进行共价乙酰化作用来抑制PG合成酶。抑制作用取决于时间和阿司匹林浓度。与来自SSV的酶相比，阿司匹林抑制人血小板中酶的效力要高37倍。3. 双氟尼酸对完整的人血小板和SSV中的PG合成酶具有同等程度的抑制作用（在3 - 5微摩尔时抑制50%）。该药物不会对酶进行共价修饰，且抑制作用不依赖于时间。双氟尼酸可能作用于与阿司匹林相似的位点，因为该药物会抑制阿司匹林对酶的乙酰化作用。4. 结果表明，与阿司匹林相比，双氟尼酸对血小板功能的抑制作用相对较小。
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