Grant A J, Feinberg A, Chou T C, Watanabe K A, Fox J J, Philips F S
Biochem Pharmacol. 1982 Mar 15;31(6):1103-8. doi: 10.1016/0006-2952(82)90349-5.
The radioactivity of 14C-labeled 2'-fluoro-5-iodo-1-beta-D-arabinofuranosylcytosine ([2-14C]-FIAC), a new and potent antiherpetic agent, was shown previously to be incorporated into the DNA fractions of mammalian and neoplastic tissues. The present work was undertaken to learn the nature of the incorporated moieties. Enzyme degradation of highly purified DNA from the small intestine of mice treated with [2-14C]FIAC and analysis of the resulting nucleosides failed to reveal the presence of unchanged FIAC. Rather, three metabolites were found, namely, the 2'-fluoro-1-beta-D-arabinofuranosyl nucleosides of cytosine (FAC), thymine (FMAU) and 5-iodouracil (FIAU). Labeled metabolites of FIAC were also found in the DNA isolated from P815 leukemic cells in mice given [2-14C]FIAC. It is of interest to note that FMAU, FIAU and FAC are, like FIAC, potent antiherpetic agents.
新型强效抗疱疹剂14C标记的2'-氟-5-碘-1-β-D-阿拉伯呋喃糖基胞嘧啶（[2-14C]-FIAC）的放射性先前已显示可掺入哺乳动物和肿瘤组织的DNA组分中。开展本研究以了解掺入部分的性质。对用[2-14C]FIAC处理的小鼠小肠中高度纯化的DNA进行酶降解，并对所得核苷进行分析，未发现未改变的FIAC存在。相反，发现了三种代谢物，即胞嘧啶（FAC）、胸腺嘧啶（FMAU）和5-碘尿嘧啶（FIAU）的2'-氟-1-β-D-阿拉伯呋喃糖基核苷。在给予[2-14C]FIAC的小鼠的P815白血病细胞分离出的DNA中也发现了FIAC的标记代谢物。值得注意的是，FMAU、FIAU和FAC与FIAC一样，都是强效抗疱疹剂。
