Cytochrome P-450-dependent oxidative cleavage of 1-(tetrahydro-2-furanyl)-5-fluorouracil to 5-fluorouracil.
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概要
- 論文の詳細を見る
Cytochrome P-450-dependent oxidative cleavage of 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT) was investigated in a reconstituted system containing purified phenobarbital-inducible cytochrome P-450 (P-450<SUB>1</SUB>) or 3-methylcholanthrene-inducible cytochrome P-450 (P-448<SUB>1</SUB>). FT was converted into 5-fluorouracil (5-FU) in the reconstituted system, and its rate was 71 pmol 5-FU formed/min/nmol P-450<SUB>1</SUB> and 45 pmol 5-FU/min/nmol P-448<SUB>1</SUB>. Cytochrome P-450, NADPH-cytochrome P-450 reductase and NADPH were required for 5-FU production. Inhibitors of cytochrome P-450 such as carbon monoxide and metyrapone markedly decreased the rate. FT was found to interact with the purified cytochrome P-450, causing a reverse type I spectral change. From these observations, we concluded that the hepatic microsomal cytochrome P-450-dependent mixed function oxidase system participates in the oxidative cleavage of FT.
- 公益社団法人 日本薬理学会の論文
著者
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Kawata Sumio
Second Department Of Internal Medicine Yamagata University School Of Medicine
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Tarui Seiichiro
Second Department Of Internal Medicine Osaka University Medical School
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MARUNAKA Teruyoshi
Department of Biochemistry, Osaka University Medical School
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OKAMOTO Mitsuhiro
Taiho Pharmaceutical Co. Ltd.
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MINAMI Yuzo
Second Department of Internal Medicine, Osaka University Medical School
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YAMANO Toshio
Taiho Pharmaceutical Co. Ltd.
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