Veselý J, Pískala A
Cancer Res. 1984 Nov;44(11):5165-8.
The alpha-D-anomer of 5-aza-2'-deoxycytidine inhibited cell growth in vitro in L1210 mouse leukemic cells (concentration causing 50% inhibition about 1 X 10(-6) M) and was also active in vivo in increasing the life span of mice with L1210 leukemia by 100% after a single i.p. injection (800 to 1000 mg/kg). This effect could be reversed by 2'-deoxycytidine. The alpha-D-anomer produced approximately 100-fold less host toxicity than did 5-aza-2'-deoxycytidine. It was observed that alpha-D-anomer, when kept at 23 degrees for 72 hr, inhibited the uptake of radioactive 2'-deoxycytidine by L1210 cells in vitro as well as the phosphorylation of 2'-deoxycytidine by a cell-free extract from L1210 cells. These effects could not be obtained with the fresh solution of the drug. It is proposed that the action of alpha-D-anomer is due to its conversion to 5-aza-2'-deoxycytidine as shown by high-performance liquid chromatography performed on water solutions of both anomers.
5-氮杂-2'-脱氧胞苷的α-D-异头物在体外对L1210小鼠白血病细胞的生长有抑制作用（引起50%抑制的浓度约为1×10⁻⁶ M），并且在体内单次腹腔注射（800至1000 mg/kg）后，对延长L1210白血病小鼠的寿命也有活性，可使其寿命延长100%。这种作用可被2'-脱氧胞苷逆转。α-D-异头物产生的宿主毒性比5-氮杂-2'-脱氧胞苷小约100倍。据观察，α-D-异头物在23℃保存72小时后，在体外会抑制L1210细胞对放射性2'-脱氧胞苷的摄取，以及L1210细胞无细胞提取物对2'-脱氧胞苷的磷酸化作用。而新鲜的药物溶液则不会产生这些效应。有人提出，α-D-异头物的作用是由于其转化为5-氮杂-2'-脱氧胞苷，这是通过对两种异头物的水溶液进行高效液相色谱分析得出的结果。
