Roos W, Oeze L, Löser R, Eppenberger U
J Natl Cancer Inst. 1983 Jul;71(1):55-9.
The antiestrogenic action of 3-hydroxytamoxifen [trans-1-(4-beta-dimethylaminoethoxyphenyl)-1-(3-hydroxyphenyl)-2 -phenylbut-1-ene] was characterized in vitro and compared with that of tamoxifen [trans-1-(4-beta-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene]. The relative binding affinities of 3-hydroxytamoxifen to estrogen receptor were 3.3% in cytosol of MCF-7 cells and 1.5% in human mammary carcinoma cytosol compared to values of 0.2 and 0.3% for tamoxifen (the affinity of 17 beta-estradiol considered to be 100%). The concentration of 3-hydroxytamoxifen necessary to suppress the 17 beta-estradiol-induced growth stimulation of MCF-7 cells was about tenfold lower than that for tamoxifen. The induction of progesterone receptor in MCF-7 cells by 17 beta-estradiol was inhibited by 3-hydroxytamoxifen. In the absence of 17 beta-estradiol, 3-hydroxytamoxifen gave rise to a moderate increase in the progesterone receptor levels, which demonstrates the partially estrogenic character of hydroxytamoxifen.
对3-羟基他莫昔芬[反式-1-(4-β-二甲基氨基乙氧基苯基)-1-(3-羟基苯基)-2-苯基丁-1-烯]的抗雌激素作用进行了体外研究，并与他莫昔芬[反式-1-(4-β-二甲基氨基乙氧基苯基)-1,2-二苯基丁-1-烯]进行了比较。与他莫昔芬（17β-雌二醇的亲和力被视为100%）的0.2%和0.3%相比，3-羟基他莫昔芬对雌激素受体的相对结合亲和力在MCF-7细胞胞质溶胶中为3.3%，在人乳腺癌胞质溶胶中为1.5%。抑制17β-雌二醇诱导的MCF-7细胞生长刺激所需的3-羟基他莫昔芬浓度比他莫昔芬低约十倍。3-羟基他莫昔芬抑制了17β-雌二醇诱导的MCF-7细胞中孕酮受体的诱导。在没有17β-雌二醇的情况下，3-羟基他莫昔芬使孕酮受体水平适度增加，这表明羟基他莫昔芬具有部分雌激素特性。
