Sonnenschein C, Papendorp J T, Soto A M
Life Sci. 1985 Jul 29;37(4):387-94. doi: 10.1016/0024-3205(85)90510-7.
Cloned human MCF-7 breast tumor cells were prevented from proliferating when grown in charcoal-dextran stripped human female serum (CDFHS)-supplemented media (40% and 10%); this inhibition was maximally cancelled by estradiol-17, cisTamoxifen, and Metabolite E, whereas Tamoxifen, N-desmethylTamoxifen and Metabolite Y only partially blocked the inhibitory effect of CDFHS. The efficiency of this reversing effect was estradiol-17 greater than Metabolite E greater than cisTAM greater than OHTAM greater than TAM = Metabolite Y. CDFHS at 2% allowed for near maximal cell yield; estradiol-17 at concentrations above 3 X 10(-10) M inhibited cell proliferation whereas at lower concentrations was ineffective. All the triphenylethylenes tested at 2% CDFHS were toxic above 3 X 10(-7) M; beyond these concentrations, these drugs did not significantly affect the cell yield. The proliferative properties of E2 and these triphenylethylenes do not directly correlate with their binding affinities to the intracellular estrophilins. Finally, the control of the proliferation of C7MCF7-173 cells appears to be affected by the interaction among a) estradiol-17 or the triphenylethylenes, b) a specific blood-borne inhibitor of the proliferation of estrogen-sensitive cells (estrocolyones), and c) an inhibitor "receptor"-like structure in these target cells.
克隆的人MCF - 7乳腺肿瘤细胞在添加了经活性炭 - 葡聚糖处理的人女性血清（CDFHS）的培养基（40%和10%）中生长时增殖受到抑制；雌二醇 - 17、顺式他莫昔芬和代谢物E能最大程度地消除这种抑制作用，而他莫昔芬、N - 去甲基他莫昔芬和代谢物Y只能部分阻断CDFHS的抑制作用。这种逆转作用的效率为：雌二醇 - 17＞代谢物E＞顺式他莫昔芬＞OHTAM＞他莫昔芬 = 代谢物Y。2%的CDFHS可使细胞产量接近最大值；浓度高于3×10⁻¹⁰ M的雌二醇 - 17会抑制细胞增殖，而较低浓度时则无效。在2% CDFHS条件下测试的所有三苯乙烯类化合物在浓度高于3×10⁻⁷ M时具有毒性；超过这些浓度后，这些药物对细胞产量没有显著影响。E2和这些三苯乙烯类化合物的增殖特性与其对细胞内雌激素亲和蛋白的结合亲和力没有直接相关性。最后，C7MCF7 - 173细胞增殖的控制似乎受到以下因素相互作用的影响：a）雌二醇 - 17或三苯乙烯类化合物，b）一种血液中特异性的雌激素敏感细胞增殖抑制剂（雌激素裂解素），以及c）这些靶细胞中一种类似抑制剂“受体”的结构。
