Rabe T, Bohlmann M K, Rehberger-Schneider S, Prifti S
Department of Obstetrics and Gynecology, Ruprechts-Karls-Universitaet, Heidelberg, Germany.
Gynecol Endocrinol. 2000 Apr;14(2):118-26. doi: 10.3109/09513590009167670.
The cellular action of steroid hormones is mediated by specific receptors. Recently, two different estrogen receptors (ER), alpha and beta, have been cloned with a specific tissue distribution. Active estrogen as well as active progestin are compounds of oral hormonal contraceptives and hormone replacement therapy. To examine the regulation of ER-alpha and -beta activities after treatment with synthetic progestins and synthetic and natural estrogens, COS 7 cells were transfected with the vector expressing ER-alpha and -beta in combination with a luciferase reporter vector. ER-alpha activity was upregulated in the presence of synthetic progestins in a dose-dependent manner. Norethisterone, norethynodrel and desogestrel proved to be the most potent stimulatory agents of ER-alpha expression. On the other hand, not all progestins exhibited a stimulatory action on ER-beta activity. Only norgestrel, levonorgestrel, norethynodrel and norethisterone induced ER-beta-activating functions in a dose-dependent manner. Luciferase activity due to estrogen stimulation served as a positive control. Our results indicate that progestins have different effects on the activities of ER-alpha and -beta.
甾体激素的细胞作用是由特定受体介导的。最近，两种不同的雌激素受体（ER），α和β，已被克隆，且具有特定的组织分布。活性雌激素以及活性孕激素是口服激素避孕药和激素替代疗法的成分。为了研究用合成孕激素以及合成和天然雌激素处理后ER-α和-β活性的调节，将表达ER-α和-β的载体与荧光素酶报告载体一起转染到COS 7细胞中。在合成孕激素存在的情况下，ER-α活性以剂量依赖性方式上调。炔诺酮、异炔诺酮和去氧孕烯被证明是ER-α表达最有效的刺激剂。另一方面，并非所有孕激素都对ER-β活性表现出刺激作用。只有炔诺孕酮、左炔诺孕酮、异炔诺酮和炔诺酮以剂量依赖性方式诱导ER-β激活功能。雌激素刺激引起的荧光素酶活性用作阳性对照。我们的结果表明，孕激素对ER-α和-β的活性有不同影响。
