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柳氮磺胺吡啶及其代谢产物对前列腺素生物合成的抑制作用。

Inhibition of prostaglandin biosynthesis by sulphasalazine and its metabolites.

作者信息

Collier H O, Francis A A, McDonald-Gibson W J, Saeed S A

出版信息

Prostaglandins. 1976 Feb;11(2):219-25. doi: 10.1016/0090-6980(76)90145-3.

Abstract

Sulphasalazine (SZ) inhibits prostaglandin (PG) biosynthesis in vitro with a potency comparable to that of aceylsalicylate. The metabolites of SZ, sulphapyridine and 5-aminosalicylic acid, were of considerably lower potency as inhibitors of PG biosynthesis in the synthetase preparations used. Th inhibition of prostaglandin production by SZ could at least partly account for the clinical utility of sulphasalazine in ulcerative colitis. Sulphapyridine may help to maintain inhibitory concentrations of SZ by restraining bacterial breakdown of the active drug.

摘要

柳氮磺吡啶(SZ)在体外抑制前列腺素(PG)生物合成,其效力与乙酰水杨酸相当。在所用的合成酶制剂中,SZ的代谢产物磺胺吡啶和5-氨基水杨酸作为PG生物合成抑制剂的效力要低得多。SZ对前列腺素产生的抑制作用至少可以部分解释柳氮磺吡啶在溃疡性结肠炎中的临床效用。磺胺吡啶可能通过抑制活性药物的细菌分解来帮助维持SZ的抑制浓度。

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