著者

安田 行寛 東郷 常夫 采見 憲男 渡辺 昭治 播磨 耕介 鈴江 崇志

出版者

公益社団法人 日本化学療法学会

雑誌

日本化学療法学会雑誌 (ISSN:00093165)

巻号頁・発行日

vol.21, no.6, pp.1171-1178, 1973

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N<SUB>1</SUB>-(2-Tetrahydrofuryl)-5-fluorouracil (FT-207), a new antimetabolic anticancer agent synthesized in USSR, was studied on antimicrobial activity <I>in vitro</I> and distribution, excretion and metabolism <I>in vivo</I>.<BR>The results obtained were as follows.<BR>1) Antimicrobial activity<BR>FT-207 showed fairly active against <I>Micrococcus flavus</I> ATCC 10240, <I>Sarcina lutea</I> PCI 1001, <I>Staphylococcus epidermidis</I> and <I>Staphylococcus aureus</I> 209 P, but in general the activity was inferior to that of 5-FU.<BR>2) Distribution<BR>By the intravenous administration of FT-207, 400mg/kg, in normal and AH-130 bearing rats, the concentration of FT-207 in serum and tissues maintained measurably until 16-24 hours.<BR>On the other hand, the active substances (5-FU, <I>etc</I>.) from FT-207 detected at 1-4 hours and peaked at 4-16 hours in tissues.<BR>3) Urinary excretion<BR>FT-207 and its active substances were excreted in urine for a long time, and the recoveries of FT-207 for 48 hours in rats, mice and rabbits were 12-18%.<BR>4) Metabolism<BR>In normal and AH-130 bearing rats, the main active substance from FT-207 administrated intravenously was 5-FU.