Influence of estrogen structure on nuclear binding and progesterone receptor induction by the receptor complex.
Influence of estrogen structure on nuclear binding and progesterone receptor induction by the receptor complex.
复制标题
雌激素结构对核结合和受体复合物诱导孕激素受体的影响。
DOI：
10.1021/bi00078a027
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发表时间：
1993
期刊：
影响因子：
2.9
通讯作者：
Brooks,SC
中科院分区：
文献类型：
--
作者：
VanderKuur,JA;Wiese,T;Brooks,SC
材料和方法类固醇。雌三烯、雌酮、E2、雌三醇、雌二醇-16 a和雌二醇-17 a购自Research Plus，Inc.。（Bayonne，NJ）。在这些研究中使用的所有A-环取代的雌激素都是在我们的实验室中根据公开的程序合成的。已经报道了1-、2-和4-羟基雌三烯-17/3-醇的合成（Palomino等人，1990），雌三烯-17/3-醇和3-羟基雌三烯的合成（Horwitz等人，1986; Dannenberg &科勒，1964）。通过薄层色谱法纯化这些类似物中的每一种，并结晶，直到污染性雌激素（特别是E2）以低于1/10000的水平存在。在TLC板（硅胶）上进行色谱法，其在能够分离E2的系统（用己烷：乙酸乙酯，8：2展开三次）中拆分约1 mg化合物（3-4 μ mol）。将板暴露于I2后，用UV光（254 nm）观察斑点，能够检测到0.1 nmol E2。在这些条件下，TLC板上不存在对应于E2的斑点，这保证了色谱分离的类似物在104份化合物中含有少于1份E2。
MATERIALS AND METHODSSteroids. Estratriene, estrone, E2, estriol, estradiol-16a, and estradiol-17a were purchased from Research Plus, Inc.(Bayonne, NJ). All of the A-ring-substituted estrogens utilized in these studies were synthesized in our laboratory according to published procedures. The syntheses of 1-, 2-, and 4-hydroxyestratrien-17/3-ol have been reported (Palomino et al., 1990), as have the syntheses of estratrien-17/3-ol and 3-hydroxyestratriene (Horwitz et al., 1986; Dannenberg & Kohler, 1964). Each of these analogues was purified by thin-layer chromatography and crystallized until contaminating estrogens (particularly E2) were present at a level less than 1 part in 10 000. Chromatography was carried out on TLC plates (silica gel), which resolved approximately 1 mg of the compounds (3-4^ mol) in a system which was capable of separating E2 (developed three times with hexane: ethylacetate, 8: 2). Visualization of spots with UV light (254 nm), after exposure of the plates to I2, enabled the detection of 0.1 nmol of E2. The absence of a spot corresponding to E2 on the TLC plate under these conditions was assurance that the chromatographed analogue contained less than 1 part E2 in 104 parts of the compound.