阿拉伯糖基核苷。十二。阿拉伯呋喃糖基胸腺嘧啶对L5178y细胞生长的影响。
Arabinosyl nucleosides. XII. Influence of arabino-furanosylthymine on growth of L5178y cells.
作者信息
Müller W E, Zahn R K, Maidhof A, Beyer R, Arendes J
出版信息
Chem Biol Interact. 1978 Nov;23(2):141-50. doi: 10.1016/0009-2797(78)90001-7.
The antibiotic 1-beta-D-arabinofuranosylthymine (araThd) is a potent inhibitor of the growth of mouse lymphoma cells (L5178y). The ED50 concentration was found to be 9.8 muM. The cells die as a consequence of an unbalanced growth. The cytostatic activity of araThd can be abolished by coincubation with dThd and dUrd but not with Urd. At cytostatic concentrations araThd selectively blocks DNA synthesis; RNA- and protein synthesis are unaffected. Intracellularly araThd is rapidly phosphorylated to araTTP. This enzymic phosphorylation does not influence the synthesis of the naturally occuring, related triphosphate dTTP. AraTMP is incorporated into DNA during DNA synthesis; 1 mol of ara-TMP is incorporated/19,500 molecules of dTMP.
抗生素1-β-D-阿拉伯呋喃糖基胸腺嘧啶（araThd）是小鼠淋巴瘤细胞（L5178y）生长的强效抑制剂。发现其半数有效浓度（ED50）为9.8μM。细胞因生长失衡而死亡。araThd的细胞生长抑制活性可通过与dThd和dUrd共同孵育而消除，但与Urd共同孵育则不能消除。在细胞生长抑制浓度下，araThd选择性地阻断DNA合成；RNA和蛋白质合成不受影响。在细胞内，araThd迅速磷酸化为araTTP。这种酶促磷酸化不影响天然存在的相关三磷酸脱氧胸苷（dTTP）的合成。在DNA合成过程中，araTMP被掺入DNA中；每19,500个dTMP分子掺入1摩尔ara-TMP。
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