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  • 标题:Inhibitory Effects of Amino-Acid Fluids on Drug Binding to Site II of Human Serum Albumin in Vitro
  • 本地全文:下载
  • 作者:Keishi Yamasaki ; Noriyuki Kuga ; Norito Takamura
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2005
  • 卷号:28
  • 期号:3
  • 页码:549-552
  • DOI:10.1248/bpb.28.549
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The effects of amino-acid fluids on ligand binding to human serum albumin (HSA) were investigated by fluorescence and ultrafiltration techniques. Warfarin and dansylsarcosine were used as the site marker fluorescence probes for site I and site II of HSA, respectively. Amino-acid fluids specifically decreased the fluorescence intensity induced by dansylsarcosine-HSA binding without any effects on that induced by warfarin-HSA binding. The ultrafiltration technique clarified that the free fraction of the site II drug, diazepam, in human serum was increased in the presence of amino-acid fluids, while no effect was observed in the free fraction of the site I drug, warfarin. The potencies of the effect on binding to site II, observed by fluorescence and ultrafiltration techniques, correlated well with the L -tryptophan contents in amino-acid fluids or with those in L -tryptophan solutions. Based on the comparison between the effects of amino-acid fluids and L -tryptophan solutions, we confirmed that L -tryptophan in amino-acid fluids specifically inhibits drug binding to site II of HSA.
  • 关键词:protein binding;albumin;parenteral nutrition;binding site;amino acid;drug interaction
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