title: Difference in uptake of 3H-estramustine in two human prostatic carcinoma cell lines, LNCaP and LNCaP-r.
abstract: Estramustine, estradiol-3-N-bis(2-chloroethyl)carbamate (EM), has been shown to inhibit growth of the human prostatic carcinoma cell line LNCaP as well as its subline LNCaP-r. The hormone sensitive LNCaP showed greater sensitivity to the drug than the hormoneresistant LNCaP-r. LNCaP has also shown an increasing sensitivity to 10(-7) M EM, when incubated with different concentrations of steroid hormones. We studied whether the increasing sensitivity was caused by increased uptake of EM. 3H-estramustine was added to medium and the cells were incubated 15 min, 30 min, 45 min, 1 h, 1.5 h, 2 h, and 4 h, or 2 h, 4 h, 6 h, and 8 h. No effect of steroids on the uptake of EM was noted, but LNCaP showed a higher uptake of EM compared to LNCaP-r. The uptake of EM in LNCaP increased for eight hours, whereas LNCaP-r reached its maximum uptake after six hours of incubation.
authors.affiliation: Department of Clinical Chemistry I, Karolinska Institute, Huddinge University Hospital, Sweden.
authors.forename: M
authors.initials: M
authors.lastname: Hasenson
mesh_terms: D001693:Biological Transport, Active / Q000187:drug effects; D002460:Cell Line; D004961:Estramustine / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D009376:Neoplasms, Hormone-Dependent / Q000378:metabolism; D009588:Nitrogen Mustard Compounds / Q000493:pharmacokinetics*; D011471:Prostatic Neoplasms / Q000378:metabolism*; D013256:Steroids / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism
chemical_list: D009588:Nitrogen Mustard Compounds; D013256:Steroids; D004961:Estramustine