Structure- Activity Relationships of Folate Derivatives as Inhibitors of Xanthine Oxidase in Vitro

DOI
  • YAMAMOTO Itaru
    Department of Medicinal Biochemistry, Faculty of Pharmaceutical Sciences, Okayama University
  • OKIMURA Tsutomu
    Department of Medicinal Biochemistry, Faculty of Pharmaceutical Sciences, Okayama University
  • KASAHARA Etsuko
    Department of Medicinal Biochemistry, Faculty of Pharmaceutical Sciences, Okayama University
  • NISHIOKA Kusuki
    Rheumatology Division, Department of Medicines, School of Medicine, Mie University
  • MIKANAGI Kiyonobu
    Department of Orthopedics, Jichi Medical School

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Description

A series of 46 folate and the related compounds including those already evaluated as enzyme inhibitors was tested for their inhibition of bovine milk and mouse liver xanthine oxidase in vitro. We have reconfirmed the inhibitory effect of folic acid on this enzyme N10-Formyl folic acid was even stronger inhibitor than folic acid.Reduced forms of folate and its derivatives, namely N5, N10-methenyltetrahydrofolic acid, tetrahydrofolic acid and dihydrofolic acid were also effective inhibitors of this enzyme, indicating that the biological active forms (e.g. one-carbon transfer) are not necessary for the enzyme inhibitory action. Some pteridine compounds including Neopterin, Lumazine were showed to have comparative effects to folic acid, while p-aminobenzoyl glutamic acid and p-aminobenzoic acid and glutamic acid, and their derivatives studied were without significant activity.

Journal

  • Uric acid research

    Uric acid research 3 (2), 198-213, 1979

    Japanese Society of Gout and Nucleic Acid Metabolism

Details 詳細情報について

  • CRID
    1390282679745029120
  • NII Article ID
    130004596466
  • DOI
    10.14867/gnam1977.3.2_198
  • ISSN
    21870098
    03884120
  • Text Lang
    en
  • Data Source
    • JaLC
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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