頁籤選單縮合
題 名 | Photoproducts of Indomethacin Exhibit Decreased Hydroxyl Radical Scavenging and Xanthine Oxidase Inhibition Activities |
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作 者 | Lien, Gi-shih; Chen, Chien-shu; Chen, Wei-yu; Huang, Shih-hao; Cheng, Kur-ta; Lin, Chun-mao; Chao, Su-hui; | 書刊名 | Journal of Food and Drug Analysis |
卷 期 | 21:3 2013.09[民102.09] |
頁 次 | 頁332-336 |
分類號 | 418.2216 |
關鍵詞 | Electron spin resonance; Hydroxyl radical; Indomethacin; Molecular modeling; Photoproduct; Xanthine oxidase; |
語 文 | 英文(English) |
英文摘要 | Indomethacin (IN) is a widely used nonsteroidal anti-inflammatory drug. In this study, four photoproducts of IN (IN1-IN4) were produced and isolated from photoirradiated IN. This study investigated the abilities of IN and its photoproducts to scavenge hydroxyl radicals and inhibit xanthine oxidase (XO). The hydroxyl radical-scavenging activity was measured in vitro by electron spin resonance spectrometry using 5,5-dimethyl-1-pyrroline-N-oxide as a spin trapping agent. Enzyme activity was measured by continuous monitoring of uric acid formation, using xanthine as a substrate. The results showed that, among all the related products, IN has the strongest hydroxyl radical-scavenging (IC50 = 65 mM) and XO inhibitory (IC50 = 86 mM) effects. To further understand the stereochemistry of the reactions between these IN derivatives and XO, we performed computer-aided molecular modeling. IN was the most potent inhibitor with the most favorable interaction in the reactive site. Various photoproducts exhibited affinity toward XO as a result of the absence of hydrogen bonding with molybdopterin domain. |
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