Hartley-Asp B, Gunnarsson P O
J Urol. 1982 Apr;127(4):818-22. doi: 10.1016/s0022-5347(17)54057-4.
Estramustine at concentrations ranging from 3-40 x 10(-6) M inhibited the cell growth and clonogenic survival of a human prostatic carcinoma cell line (DU 145). This cell line was found to be unresponsive to estradiol and testosterone at concentrations ranging from 10(-9) M to 5 x 10(-5) M. Metabolism studies with estramustine showed that only a few per cent of the ester linkage was cleaved during the exposure period. This small amount of metabolism could possibly lead to the release of nor-nitrogen mustard, which was however found not to be as inhibitory as estramustine in this cell line. The results indicate that estramustine per se causes the cell death of hormone unresponsive human prostatic carcinoma cells in cell culture.
浓度范围为3 - 40×10⁻⁶ M的雌莫司汀抑制了人前列腺癌细胞系(DU 145)的细胞生长和克隆形成存活。发现该细胞系对浓度范围为10⁻⁹ M至5×10⁻⁵ M的雌二醇和睾酮无反应。对雌莫司汀的代谢研究表明,在暴露期间只有百分之几的酯键被裂解。这种少量的代谢可能导致去甲氮芥的释放,然而在该细胞系中发现去甲氮芥的抑制作用不如雌莫司汀。结果表明,在细胞培养中,雌莫司汀本身会导致激素无反应的人前列腺癌细胞死亡。