文章基本信息

标题：Inhibitory Effect of Flavonoids on N-Acetylation of 5-Aminosalicylic Acid in Cultured Rat Hepatocytes
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作者：Yuri Mizoyama ; Hisashi Takaki ; Narumi Sugihara 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2004
卷号：27
期号：9
页码：1455-1458
DOI：10.1248/bpb.27.1455
出版社：The Pharmaceutical Society of Japan
摘要：5-Aminosalicylic acid (5-ASA) is an effective drug for the treatment of ulcerative colitis and Crohn's disease. A large group of flavonoids was investigated for their inhibitory effects on the N -acetyl-conjugation of 5-ASA in rat hepatocytes and subcellular preparations. When added to cultured hepatocytes, some flavonoids inhibited the production of N -acetyl-5-aminosalicylic acid (5-AcASA) with potencies that depended on the specific structure of flavonoids. Among the flavonols, quercetin, kaempferol and galangin had inhibitory activity with a tendency to be more effective at increasing the number of hydroxyl substitutions in the B-ring. Flavones such as luteolin, apigenin and chrysin were as effective as the corresponding three flavonols above. 7,3′,4′-OH flavone was more effective than other simple flavones such as 7-, 5-, 3-, 7,3-, 7,4′- and 3′,4′-OH flavones. Isoflavones were relatively weak inhibitors. Taxifolin and catechins had little or no inhibitory effect. These data suggest that the presence of C7 hydroxyl substitution on the A-ring and the catechol group on the B-ring in the flavone structure is required for effective inhibitory activity. The inhibitory effect of flavonoids on N -acetyl-conjugation of 5-ASA was also examined by incubating 5-ASA with isolated liver cytosolic preparations. The active flavonoids in the cells inhibited the N -acetylation of 5-ASA in the cell-free enzymatic preparations with a potency comparable to that for cultured rat hepatocytes.
关键词：flavonoid;N-acetylation;5-aminosalicylic acid