Surya Y A, Rosenfeld J M, Hillcoat B L
Cancer Treat Rep. 1978 Jan;62(1):23-9.
Phosphoramide mustard, formed from cyclophosphamide in vivo and in vitro, may be the active metabolite of this drug. We have found phosphoramide mustard to be at least 100 times more potent than cyclophosphamide in inhibiting growth of two strains of the L1210 lymphoma in culture. Phosphoramide mustard also produced enlargement of cells, an effect not seen with cyclophosphamide. Phosphoramide mustard significantly increased the amount of cross-linked DNA after incubation with intact LM4 cells or nuclei isolated from these cells. Cyclophosphamide had a similar effect only in the isolated nuclei. These findings strengthen the proposed role of phosphoramide mustard as the active metabolite of cyclophosphamide. The effect of cyclophosphamide on nuclei is unexplained.
在体内和体外由环磷酰胺形成的磷酰胺氮芥可能是该药物的活性代谢物。我们发现磷酰胺氮芥在抑制培养中的两株L1210淋巴瘤生长方面比环磷酰胺至少强100倍。磷酰胺氮芥还会使细胞增大，这是环磷酰胺所没有的作用。与完整的LM4细胞或从这些细胞中分离出的细胞核孵育后，磷酰胺氮芥显著增加了交联DNA的量。环磷酰胺仅在分离出的细胞核中具有类似作用。这些发现强化了磷酰胺氮芥作为环磷酰胺活性代谢物的推测作用。环磷酰胺对细胞核的作用尚无法解释。
