Photoproducts of Indomethacin exhibit decreased hydroxyl radical scavenging and xanthine oxidase inhibition activities

Gi-Shih Lien, Chien Shu Chen, Wei-Yu Chen, Shih Hao Huang, Kur-Ta Cheng, Chun-Mao Lin, Su Hui Chao

研究成果: 雜誌貢獻文章同行評審

4 引文 斯高帕斯(Scopus)

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 (IC 50 = 65 μM) and XO inhibitory (IC50 = 86 μM) 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.
原文英語
頁(從 - 到)332-336
頁數5
期刊Journal of Food and Drug Analysis
21
發行號3
DOIs
出版狀態已發佈 - 九月 2013

ASJC Scopus subject areas

  • Food Science
  • Pharmacology

指紋 深入研究「Photoproducts of Indomethacin exhibit decreased hydroxyl radical scavenging and xanthine oxidase inhibition activities」主題。共同形成了獨特的指紋。

引用此