Inhibition of 5'-Deoxy-5-fluorouridine Phosphorolysis by Acyclothymidine in Tumor Cell Homogenates
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概要
- 論文の詳細を見る
The inhibitory effect of acyclothymidine[AcyT, 5-methyl-1-(2'-hydroxyethoxymethyl) uracil], a potent pyrimidine nucleoside phosphorylase (PyNPase) inhibitor, on 5'-deoxy-5-fluorouridine (5'-DFUR) phosphorolysis in human and mouse tumor cell homogenates was measured. Competitive inhibition was observed in MKN-74 and Lewis lung carcinoma (LLC), whereas non-competitive inhibition was observed in HeLa. The strength of the inhibitory effect by AcyT showed the following pattern : HeLa<human normal intestine<mouse normal intestine<Colon 26<LLC<MKN-74<DLD-1. From the kinetic parameter obtained, we simulated the inhibitory effect of AcyT on 5'-DFUR phosphorolysis in tumor cells and the intestine. These data indicated that AcyT was more sensitive in normal mouse intestine than in Colon 26 and LLC, and that orally administered AcyT can reduce the intestinal toxicity of 5'-DFUR without reducing the antitumor effect in the mouse. The present finding may have an important implication for attempts to introduce AcyT, a potent PyNPase inhibitor, into the clinic.
- 公益社団法人日本薬学会の論文
- 1997-08-15
著者
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Hamada Akinobu
熊本大学医学部附属病院 薬剤
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Hamada Akinobu
Kumamoto Univ. Hospital Kumamoto Jpn
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Hamada Akinobu
Department Of Pharmacy Kumamoto University Hospital
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NAKANO Masahiro
Department of Physics, Kyoto University
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長谷川 哲也
城西国際大学 薬学部
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Nakano M
Department Of Information Science University Of Occupational And Environmental Health
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KAWAGUCHI Takeo
Faculty of Pharmaceutical Sciences, Josai University
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SHIMIDZU Satoshi
Faculty of Pharmaceutical Sciences, Josai University
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HASEGAWA Tetsuya
Faculty of Pharmaceutical Sciences, Josai University
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Nakano M
Department Of Biologicalsciences Teikyo University Of Science And Technology
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Hasegawa T
Univ. Tokushima School Of Medicine Tokushima Jpn
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Nakano Masahiro
Department Of Biologicalsciences Teikyo University Of Science And Technology
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Hasegawa Tetsuya
Faculty Of Pharmaceutical Sciences Chiba University
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Hasegawa T
Faculty Of Pharmaceutical Sciences Josai International University
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川口 健夫
城西大学
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Hisayama T
Univ. Tokushima School Of Medicine Tokushima Jpn
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Nakano M
Univ. Occupational And Environmental Health Jpn
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Shimizu Satoshi
Faculty Of Dairy Science Rakuno Gakuen University
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Nakano Masahiro
Deparment Of Physics Kyushu University
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Hasegawa Tetsuya
Faculty Of Pharmaceutical Science Josai International University
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