Mode of Action of 5-Fluorocytidine and 5-Fluoro-2'-deoxycytidine in L5178Y Cells in Vitro

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概要

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• The mode of antiproliferative action of two 5-fluorocytosine nucleosides, 5-fluoro-cytidine (FCR) and 5-fluoro-2'-deoxycytidine (FCdR), was examined using mouse leukemia L5178Y cells in vitro. FCR and FCdR were markedly active against L5178Y cells, though the cells were deficient in cytidine deaminase activity. Both compounds increased the incorporation of ^<14>C-labeled thymidine into the acid-insoluble fraction of L5178Y cells and decreased labeled deoxycytidine incorporation. In reversal studies, the antiproliferative effects of both compounds were almost abolished by simultaneous addition of thymidine or deoxyuridine. Deoxycytidine completely reversed the growth inhibition caused by FCdR, but not that caused by FCR. These results demonstrate that the cytotoxicity of both compounds is due to inhibition of thymidylate synthetase, presumably through formation of 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) after deamination by deoxycytidylate deaminase in the pyrimidine de novo pathway.

• 社団法人日本薬学会の論文
• 1982-03-25

著者

• 星 昭夫

  National Cancer Center Research Institute

• 実吉 峯郎

  Faculty of Pharmaceutical Sciences, Hokkaido University

• 吉田 光二

  National Cancer Center Research Institute

• KURETANI KAZUO

  National Cancer Center Research Institute

• 実吉 峯郎

  Faculty Of Pharmaceutical Sciences Hokkaido University

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