Danks M K
J Chromatogr. 1982 Dec 10;233:141-8. doi: 10.1016/s0378-4347(00)81740-5.
Cytosine arabinoside (ara-C) has been used in the treatment of leukemia, but its exact mechanism of cytotoxicity is not yet known. One of the proposed mechanisms for the effectiveness of this drug in treating leukemias suggests that a metabolite of ara-C, i.e., 2'-deoxycytidine 5'-triphosphate (araCTP), competes with cytosine arabinoside 5'-triphosphate (dCTP) for binding to DNA polymerase. The ratio of the drug metabolite to the endogenous nucleotide (araCTP/dCTP) may, therefore, be important in determining the effectiveness of ara-C therapy. This ratio may also play a role in drug resistance. Previously published methods have focused on either araCTP or dCTP, along with metabolites and analogues of one of these compounds. The methods presented here provide two simple, sensitive ways to measure dCTP and araCTP in the same biological sample.
阿糖胞苷（ara-C）已被用于治疗白血病，但其确切的细胞毒性机制尚不清楚。关于该药物治疗白血病有效性的一种推测机制表明，阿糖胞苷的一种代谢产物，即2'-脱氧胞苷5'-三磷酸（araCTP），与胞嘧啶阿拉伯糖苷5'-三磷酸（dCTP）竞争结合DNA聚合酶。因此，药物代谢产物与内源性核苷酸的比例（araCTP/dCTP）可能对确定阿糖胞苷治疗的有效性很重要。该比例也可能在耐药性中起作用。先前发表的方法要么侧重于araCTP，要么侧重于dCTP，以及这些化合物之一的代谢产物和类似物。本文介绍的方法提供了两种简单、灵敏的方法来测量同一生物样品中的dCTP和araCTP。
