Kozhukhov A N
Vopr Med Khim. 1981 Mar-Apr;27(2):243-7.
Biotransformation of ftorafir (FT) was studied using 2-14C-ftorafur and 2;5'-14C-ftorafur. Both pyrimidine and tetrahydrofurane moieties of the FT underwent degradation to CO2 in rats. The cleavage of the pseudoglycosidic bonds C-N and formation of 5-fluorouracil was one of the steps of the FT metabolism that limited the velocity of the whole biotransformation process. Liver tissue NADPH-linked monooxygenating system was shown to participate in the process. The data obtained suggest that the role of enzymes involved in metabolism of nucleic acids was not significant in the FT metabolism under the conditions studied in vivo.
使用2-¹⁴C-呋喃氟尿嘧啶和2,5'-¹⁴C-呋喃氟尿嘧啶研究了替加氟(FT)的生物转化。在大鼠体内,FT的嘧啶和四氢呋喃部分均降解为二氧化碳。FT代谢过程中限制整个生物转化过程速度的步骤之一是假糖苷键C-N的断裂和5-氟尿嘧啶的形成。研究表明肝脏组织中与NADPH相关的单加氧系统参与了这一过程。获得的数据表明,在所研究的体内条件下,参与核酸代谢的酶在FT代谢中的作用并不显著。