3,9 - 二羟基 - 7,12 - 二甲基苯并[a]蒽在大鼠体内的雌激素特性
Estrogenic properties of 3,9-dihydroxy-7,12-dimethylbenz[a]anthracene in rats.
作者信息
Morreal C E, Schneider S L, Sinha D K, Bronstein R E
出版信息
J Natl Cancer Inst. 1979 Jun;62(6):1585-8.
Previously, the 3,9-dihydroxy derivative of benz[a]-anthracene was shown to be weakly estrogenic. The availability of the related diol of the mammary carcinogen dimethylbenz[a]-anthracene, i.e., 3,9-dihydroxy-7,12-dimethylbenz[a]anthracene (3,9-diOHDMBA), prompted a similar study of its estrogenic properties. The competitive binding studies of 3,9-diOHDMBA with 17beta-estradiol in the uterine cytosol of immature SD rats gave a Ka of 1.7 x 10(8) M-1. 17beta-Estradiol (10(-9) M) binding to the 8S binding protein was inhibited by 3,9-diOHDMBA at concentrations similar to those of nafoxidine HCl (1 x 10(-5) M). Bioassay demonstrated that the diol possesses 1/4,464 the activity of 17beta-estradiol.
先前已表明苯并[a]蒽的3,9 - 二羟基衍生物具有弱雌激素活性。乳腺致癌物二甲基苯并[a]蒽的相关二醇，即3,9 - 二羟基 - 7,12 - 二甲基苯并[a]蒽（3,9 - diOHDMBA）的可得性，促使人们对其雌激素特性进行类似研究。在未成熟SD大鼠子宫胞液中，3,9 - diOHDMBA与17β - 雌二醇的竞争性结合研究得出的解离常数Ka为1.7×10⁸ M⁻¹。3,9 - diOHDMBA在与盐酸奈福昔定（1×10⁻⁵ M）相似的浓度下，可抑制17β - 雌二醇（10⁻⁹ M）与8S结合蛋白的结合。生物测定表明该二醇的活性为17β - 雌二醇的1/4464。
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