Kleinrok Z, Chmielewska B, Czuczwar J S, Kozicka M, Rajtar G, Jarzabek G, Sawiniec Z
Arch Immunol Ther Exp (Warsz). 1986;34(3):263-73.
Comparison of pharmacological properties of commercial racemic Cyclophosphamide and its D- and L-enantiomers was performed in experiments on mice and rats. Acute toxicity, behavioral screening tests and the effects of subchronic treatment (influence on body mass, the increase of the mass of internal organs, mortality, morphology of peripheral blood, biochemical investigations of blood plasma, microscopic evaluation of liver and bladder) were taken into account. Summarized results revealed the most pronounced toxicity of D-cyclophosphamide. L-enantiomer was more toxic when compared with racemate. As several reports in literature confirmed the greatest antineoplastic activity of L-form in animals, the suggestion of further clinical investigation of levorotatory form as a separate preparation has been put forward.
在小鼠和大鼠实验中对市售消旋环磷酰胺及其 D-和 L-对映体的药理特性进行了比较。考虑了急性毒性、行为筛选试验以及亚慢性治疗的效果(对体重的影响、内脏器官重量增加、死亡率、外周血形态、血浆生化检查、肝脏和膀胱的显微镜评估)。汇总结果显示 D-环磷酰胺的毒性最为明显。与消旋体相比,L-对映体毒性更大。由于文献中的几份报告证实了 L 型在动物中具有最大的抗肿瘤活性,因此有人提出将左旋体作为一种单独制剂进行进一步临床研究的建议。