Inhibition of 5-Deoxy-5-fluorouridine Phosphorolysis by Acyclopyrimidinenucleosides in Intestinal Tissue Homogenates.

• 浜田 哲暢

• 福島 昭二

• 実吉 峯郎

• 川口 健夫

• 中野 眞汎

抄録

This study examined the inhibitory effect of acyclopyrimidinenucleosides on 5'-deoxy-5-fluorouridine (5'-DFUR) phosphorolysis in intestinal tissue derived from rabbit, rat, mouse, and human. 5-Bromoacyclouridine, 5-fluoroacyclouridine, acyclouridine, and 5-nitroacyclouridine showed little or only moderate effect, but acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl) uracil] showed strong inhibitory effect on 5'-DFUR phosphorolysis in intestinal tissue homogenates derived from human. In the absence of inhibitor (acyclothymidine), the V_max of 5'-DFUR phosphorolysis was 2.66 μmol/min and the K_m was 0.57 mM in human intestinal homogenates. The V_max was unaltered by increased inhibitor concentration. The maximal inhibitory effect of acyclothymidine on 5'-DFUR phosphorolysis in rat homogenates was over 90%. The K_i/K_m was 0.63 in human, 2.14 in rabbit, 1.09×10^-2 in rat, and 1.71×10^-2 in mouse. These data show that acyclothymidine is a competitive inhibitor of 5'-DFUR phosphorolysis, and that it can inhibit not only uridine phosphorylase but also thymidine phosphorylase.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 18 (1), 172-175, 1995

  公益社団法人 日本薬学会

キーワード

• 5'-deoxy-5-fluorouridine
• 5-fluorouracil
• acyclothymidine
• thymidine phosphorylase
• uridine phosphorylase
• pyrimidine nucleoside phosphorylase

詳細情報

• CRID: 1390282679599227648
• NII論文ID: 110003640763
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.18.172
• ISSN: 13475215
• ISSN: 09186158
• PubMed: 7735236
• Web Site: http://www.jstage.jst.go.jp/article/bpb1993/18/1/18_1_172/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1995235156
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可