Nielsen O H, Ahnfelt-Rønne I
Department of Medical Gastroenterology C, Herlev Hospital, University of Copenhagen, Denmark.
Pharmacol Toxicol. 1988 Apr;62(4):223-6. doi: 10.1111/j.1600-0773.1988.tb01876.x.
5-Aminosalicylic acid seems to be the active moiety of sulfasalazine in the treatment of chronic inflammatory bowel disease. Even if the precise mode of action is obscure, it is assumed that two of the main mechanisms are inhibitory effects on the lipoxygenation of arachidonic acid and interaction with free radicals. As 4-aminosalicylic acid has been claimed to be beneficial in the topical treatment of ulcerative colitis, it was tested whether this drug possesses any influence on the 5-lipoxygenase activity in human neutrophils in vitro or whether it acts as a radical scavenger. The change of the amino residue from carbon-5 to carbon-4 abolished the effect in the two systems tested. The reported clinical observations on 4-aminosalicylic acid in the treatment of chronic inflammatory bowel disease remain to be confirmed and cannot be explained by interference with arachidonic acid metabolism or free oxygen radicals.
5-氨基水杨酸似乎是柳氮磺胺吡啶治疗慢性炎症性肠病的活性部分。即使其确切作用方式尚不清楚,但推测其主要机制有两个,即对花生四烯酸脂氧合作用的抑制作用以及与自由基的相互作用。由于有人声称4-氨基水杨酸在溃疡性结肠炎的局部治疗中有益,因此测试了该药物在体外对人中性粒细胞中5-脂氧合酶活性是否有任何影响,或者它是否作为自由基清除剂起作用。氨基残基从碳-5变为碳-4消除了在两个测试系统中的作用。关于4-氨基水杨酸治疗慢性炎症性肠病的临床观察报告仍有待证实,且无法通过干扰花生四烯酸代谢或游离氧自由基来解释。