von Schoultz E, Lundgren E, Henriksson R
Department of Oncology, University Hospital, Umeå, Sweden.
Anticancer Res. 1990 May-Jun;10(3):693-6.
Estramustine, a conjugate of estradiol-17 beta and nor-nitrogen mustard currently used in prostatic cancer, was found to exert a dose-dependent antiproliferative effect on the human malignant glioma cell lines U-251 MG and U-105 MG. At equimolar concentrations the inhibitory effects of the estramustine complex were clearly more pronounced than those of estradiol and nor-nitrogen mustard given alone or in combination. Flow cytometric analyses support the concept that estramustine cytotoxicity is mediated via separate mechanisms. The intact estramustine complex may be important for effects related to microtubule function which add to the cytotoxic potential of the alkylating component.
雌莫司汀是一种目前用于前列腺癌治疗的雌二醇 - 17β与去甲氮芥的共轭物，研究发现它对人类恶性胶质瘤细胞系U - 251 MG和U - 105 MG具有剂量依赖性的抗增殖作用。在等摩尔浓度下，雌莫司汀复合物的抑制作用明显比单独使用或联合使用的雌二醇和去甲氮芥更为显著。流式细胞术分析支持了雌莫司汀细胞毒性是通过不同机制介导的这一概念。完整的雌莫司汀复合物对于与微管功能相关的作用可能很重要，这增加了烷化成分的细胞毒性潜力。
