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[阿司匹林和水杨酸的抗炎及镇痛作用方式]

[The modes of anti-inflammatory and analgesic actions of aspirin and salicylic acid].

作者信息

Higuchi S, Osada Y, Shioiri Y, Tanaka N, Otomo S, Aihara H

出版信息

Nihon Yakurigaku Zasshi. 1985 Jan;85(1):49-57. doi: 10.1254/fpj.85.49.

Abstract

The modes of anti-inflammatory and analgesic actions of aspirin and salicylic acid were investigated using some experimental animal models. Anti-inflammatory potencies of aspirin were almost equal to those of sodium salicylate in the carrageenin hind paw edema, the cotton pellet granuloma and the adjuvant arthritis tests in rats. On the other hand, in the ultra-violet ray erythema and the arachidonic acid erythema tests in guinea pigs, aspirin was more potent than sodium salicylate. Aspirin and sodium salicylate exhibited almost the same inhibitions of the rat hind paw edema induced by a mixture of carrageenin and prostaglandin E1. These results suggest that inhibition of cyclo-oxygenase by aspirin does not play any important roles for the prevention of the vascular permeability increment and the granulation in the inflamed tissue. Aspirin may exert its antiinflammatory activity mainly as salicylic acid which is not an inhibitor of prostaglandins biosynthesis in vitro. Aspirin showed about 5 times more potent analgesic action than sodium salicylate in the lameness test using adjuvant arthritic rats. Analgesic potency of aspirin was decreased to the level of sodium salicylate by injection of prostaglandin E2 into the inflamed rat paw in the adjuvant-induced lameness test. On the other hand, analgesic potency of sodium salicylate was not decreased by the same treatment. It is concluded that aspirin has two analgesic effects on the inflammatory pain, one is inhibition of prostaglandins biosynthesis by acetylation of cyclo-oxygenase and the other is an action due to salicylic acid, but the action of salicylic acid was not totally explained by the inhibition of prostaglandins synthetase.

摘要

利用一些实验动物模型研究了阿司匹林和水杨酸的抗炎和镇痛作用方式。在角叉菜胶致大鼠后爪水肿、棉球肉芽肿和佐剂性关节炎试验中,阿司匹林的抗炎效力与水杨酸钠几乎相当。另一方面,在豚鼠紫外线红斑和花生四烯酸红斑试验中,阿司匹林比水杨酸钠更有效。阿司匹林和水杨酸钠对由角叉菜胶和前列腺素E1混合物诱导的大鼠后爪水肿表现出几乎相同的抑制作用。这些结果表明,阿司匹林对环氧化酶的抑制作用在预防炎症组织中的血管通透性增加和肉芽形成方面并不起重要作用。阿司匹林可能主要以水杨酸的形式发挥其抗炎活性,而水杨酸在体外不是前列腺素生物合成的抑制剂。在使用佐剂性关节炎大鼠的跛行试验中,阿司匹林的镇痛作用比水杨酸钠强约5倍。在佐剂诱导的跛行试验中,向发炎的大鼠爪子注射前列腺素E2后,阿司匹林的镇痛效力降至水杨酸钠的水平。另一方面,相同处理并未降低水杨酸钠的镇痛效力。得出的结论是,阿司匹林对炎性疼痛有两种镇痛作用,一种是通过环氧化酶乙酰化抑制前列腺素生物合成,另一种是水杨酸引起的作用,但水杨酸的作用不能完全用抑制前列腺素合成酶来解释。

相似文献

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Anti-inflammatory effects of aspirin and sodium salicylate.阿司匹林和水杨酸钠的抗炎作用。
Eur J Pharmacol. 2002 Jun 28;447(1):1-9. doi: 10.1016/s0014-2999(02)01828-9.

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