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

YAMAMOTO Itaru, OKIMURA Tsutomu, KASAHARA Etsuko, NISHIOKA Kusuki, MIKANAGI Kiyonobu

doi:10.14867/gnam1977.3.2_198

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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説明

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.