Maruo N, Horiuchi H, Nakabo T, Kondo M, Nakamura T
Hematol Oncol. 1985 Jan-Mar;3(1):39-48. doi: 10.1002/hon.2900030106.
The effects of N4-behenoyl-1-beta-D-arabinofuranosylcytosine (BH-AC) on the cell cycle of murine leukemic cells (L 1210 cells) were compared with those of 1-beta-D-arabinofuranosylcytosine (ara-C), known to be effective for acute leukemia. In a cytokinetic study, a combination of Feulgen microcytofluorometry and tritiated thymidine autoradiography (3H-TdR ARG) was used to measure DNA content and to determine DNA synthesis simultaneously in a single cell. Administration of 200 mg/kg of BH-AC significantly prolonged the survival time of mice bearing L 1210. In addition, the cells in the G1 + S1 phases increased with time, accounting for 94.4 per cent of all cells measured at 48 h after the administration, compared to 73.7 per cent before administration. On the other hand, following the administration of 86 mg/kg of ara-C (equivalent to 200 mg/kg of BH-AC), the percentage of cells in the S1 + S2 phases increased maximally to 75.9 per cent at 18 h. Cytokinetic studies further showed that BH-AC administration blocks DNA synthesis of the cells in the S-phase for a longer period than does ara-C. These results suggest that the prolonged inhibition by BH-AC on DNA synthesis allows cells to accumulate in the S-phase to a greater degree.
将N4-山嵛酰基-1-β-D-阿拉伯呋喃糖基胞嘧啶（BH-AC）对小鼠白血病细胞（L1210细胞）细胞周期的影响与已知对急性白血病有效的1-β-D-阿拉伯呋喃糖基胞嘧啶（ara-C）的影响进行了比较。在细胞动力学研究中，采用福尔根显微细胞荧光测定法和氚标记胸腺嘧啶核苷放射自显影术（3H-TdR ARG）相结合的方法，在单个细胞中同时测量DNA含量并确定DNA合成情况。给予200mg/kg的BH-AC可显著延长荷L1210小鼠的存活时间。此外，G1+S1期的细胞随时间增加，给药后48小时占所有测量细胞的94.4%，而给药前为73.7%。另一方面，给予86mg/kg的ara-C（相当于200mg/kg的BH-AC）后，S1+S2期的细胞百分比在18小时时最大增加到75.9%。细胞动力学研究进一步表明，与ara-C相比，给予BH-AC对S期细胞DNA合成的阻断时间更长。这些结果表明，BH-AC对DNA合成的长期抑制使细胞在S期积累的程度更大。
