Effects of estramustine and its constituents on human malignant glioma cells.
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.
von Schoultz
E
E
Department of Oncology, University Hospital, Umeå, Sweden.
Lundgren
E
E
Henriksson
R
R
D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004958:Estradiol / Q000494:pharmacology*; D004961:Estramustine / Q000494:pharmacology*; D005434:Flow Cytometry; D005910:Glioma; D006801:Humans; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000166:cytology / Q000187:drug effects*
D009588:Nitrogen Mustard Compounds; D004961:Estramustine; D004958:Estradiol; C004933:nornitrogen mustard