Akulov G P, Kaminskiĭ Iu L, Shestakov A D, Kaiumov V G, Chernysheva L F
Bioorg Khim. 1988 Jan;14(1):37-42.
Chemical and enzymatic syntheses of [5'-3H]adenosine, [5'-3H]guanosine, and [5'-3H]uridine have been developed. The reduction of beta-D-ribo-pentadialdo-1,4-furanosyl derivatives of corresponding bases is used in the chemical synthesis. The maximum molar activity of the labelled products was 220 TBk/mol in reactions with [3H]NaBH4 and 370-740 TBk/mol in reactions with gaseous tritium. The enzymatic synthesis was performed by the rebosylation of heterocyclic bases with nucleoside phosphorylase and [5'-3H]uridine as a ribosyl donor. Nucleoside phosphorylase is proposed to be used in the immobilized form to avoid the decrease of molar activity. Nucleosides labelled with tritium both in ribosyl and heterocyclic moieties were synthesised enzymatically.
已经开发出了[5'-³H]腺苷、[5'-³H]鸟苷和[5'-³H]尿苷的化学合成和酶促合成方法。化学合成中使用相应碱基的β-D-核糖-1,4-呋喃戊二醛衍生物的还原反应。标记产物与[³H]硼氢化钠反应时的最大摩尔活度为220 TBq/mol，与气态氚反应时为370 - 740 TBq/mol。酶促合成是通过用核苷磷酸化酶将杂环碱基与[5'-³H]尿苷作为核糖基供体进行核糖基化反应来进行的。建议使用固定化形式的核苷磷酸化酶以避免摩尔活度降低。通过酶促合成得到了在核糖基和杂环部分都标记有氚的核苷。
