Chabab A, Sultan C, Fenart O, Descomps B
J Steroid Biochem. 1986 Jul;25(1):165-9. doi: 10.1016/0022-4731(86)90296-7.
In order to study the regulation of aromatase activity by androgens in cultured fibroblasts derived from genital skin of normal prepubertal boys, aromatase activity was evaluated in the presence of various concentrations of non-aromatizable androgen DHT(5 alpha-dihydrotestosterone). The estrogen formation was assayed by an enzymatic method, after 24 h incubation of the cells with 10(-6) M androstenedione. Aromatase activity was stimulated 3- to 20-fold by DHT at concentrations 10(-10) and 10(-9) M. It was necessary to preincubate the cells with DHT for 48 h in order to bring about this stimulation. The stimulatory effect was not significant after preincubation for only 24 h. The basal value of aromatase activity was in the range of 8 +/- 1.2 pmol/mg protein/day (mean +/- SEM), while the maximal stimulation 1043 +/- 46 pmol/mg protein/day was obtained at the concentration of 10(-8) M DHT. This stimulation was partially blocked with cyproterone acetate at level of 20 +/- 4 pmol/mg protein/day; stimulation of aromatase activity by DHT could thus be mediated by the androgen receptor. This stimulatory effect was prevented by incubation of the cells with cycloheximide or actinomycin D, suggesting that DHT acts to increase aromatase activity in cultured fibroblasts by inducing the synthesis of new proteinaceous material. In vitro regulation of aromatase activity by androgens could contribute to a new approach to the extraglandular formation of estrogen.
为了研究雄激素对正常青春期前男孩生殖器皮肤来源的培养成纤维细胞中芳香化酶活性的调节作用，在存在不同浓度的非芳香化雄激素双氢睾酮（5α - 二氢睾酮）的情况下评估了芳香化酶活性。在用10⁻⁶ M雄烯二酮孵育细胞24小时后，通过酶促方法测定雌激素的生成。双氢睾酮在10⁻¹⁰和10⁻⁹ M浓度下可将芳香化酶活性刺激3至20倍。为了产生这种刺激，有必要将细胞与双氢睾酮预孵育48小时。仅预孵育24小时后，刺激作用不显著。芳香化酶活性的基础值在8±1.2 pmol/mg蛋白质/天（平均值±标准误）范围内，而在10⁻⁸ M双氢睾酮浓度下可获得最大刺激值1043±46 pmol/mg蛋白质/天。这种刺激在醋酸环丙孕酮水平为20±4 pmol/mg蛋白质/天时被部分阻断；因此，双氢睾酮对芳香化酶活性的刺激可能是由雄激素受体介导的。用环己酰亚胺或放线菌素D孵育细胞可阻止这种刺激作用，这表明双氢睾酮通过诱导新的蛋白质物质合成来增加培养成纤维细胞中的芳香化酶活性。雄激素对芳香化酶活性的体外调节可能为雌激素的腺外形成提供一种新方法。
