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环磷酰胺和异环磷酰胺的 /+/R 及 /-/S 对映体的生物活性比较研究。II. 环磷酰胺和异环磷酰胺对映体的抗增殖活性。

Comparative studies on biological activity of /+/R and /-/S enantiomers of cyclophosphamide and ifosfamide. II. Antiproliferative activity of cyclophosphamide and ifosfamide enantiomers.

作者信息

Paprocka M, Radzikowski C

出版信息

Arch Immunol Ther Exp (Warsz). 1986;34(3):285-91.

PMID:3592932
Abstract

The present studies on antiproliferative activity of cyclophosphamide and ifosfamide /+/R and /-/S enantiomers followed the earlier described differences in their antitumour activity. P-388 leukemic cells in LCFU (Leukemic Colony Forming Units) assay and Lewis lung cells in experimental metastasis assay were used as models of tumour cells. Bone marrow stem cells were applied as models of normal proliferating cells in NCFU-(Normal Colony Forming Units) and RPNCFU (Rapidly Proliferating Normal Colony Forming Units) tests. In all four models /-/S enantiomers exerted higher antiproliferative effect, than their counterparts. Antiproliferative activity of /+/RS cyclophosphamide and ifosfamide appeared to be exactly intermediate between /+/R and /-/S forms. These data, precisely differentiating the effect of /+/R, /-/S and / +/- /RS forms, confirmed the earlier described, higher antitumour effect of /-/S enantiomers of cyclophosphamide and ifosfamide.

摘要

目前关于环磷酰胺和异环磷酰胺 /+/R 和 /-/S 对映体抗增殖活性的研究遵循了此前所描述的它们在抗肿瘤活性方面的差异。在白血病集落形成单位(LCFU)测定中的P - 388白血病细胞以及实验性转移测定中的Lewis肺癌细胞被用作肿瘤细胞模型。在正常集落形成单位(NCFU)和快速增殖正常集落形成单位(RPNCFU)试验中,骨髓干细胞被用作正常增殖细胞模型。在所有这四种模型中,/-/S 对映体比其对应物表现出更高的抗增殖作用。/+ /RS 环磷酰胺和异环磷酰胺的抗增殖活性似乎恰好介于 /+/R 和 /-/S 形式之间。这些数据精确地区分了 /+/R、/-/S 和 /+/- /RS 形式的作用,证实了此前所描述的环磷酰胺和异环磷酰胺的 /-/S 对映体具有更高的抗肿瘤作用。

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