Wouters W, De Coster R, Goeminne N, Beerens D, van Dun J
Department of Life Sciences, Janssen Pharmaceutica, Beerse, Belgium.
J Steroid Biochem. 1988;30(1-6):387-9. doi: 10.1016/0022-4731(88)90128-8.
The aromatase inhibitory properties of the antifungal ketoconazole were compared with those of aminoglutethimide. In rat granulosa cells ketoconazole and aminoglutethimide showed IC50 values for aromatase inhibition of 2 X 10(-6) and 6 X 10(-7) M respectively. In the rat, in vivo, ketoconazole was 5 times less potent than aminoglutethimide. In young women, 400 mg of ketoconazole only marginally lowered plasma levels of estradiol-17 beta. It is concluded that ketoconazole is not a compound of choice for clinical use as an aromatase inhibitor.
将抗真菌药酮康唑的芳香化酶抑制特性与氨鲁米特进行了比较。在大鼠颗粒细胞中，酮康唑和氨鲁米特对芳香化酶抑制的IC50值分别为2×10^(-6) M和6×10^(-7) M。在大鼠体内，酮康唑的效力比氨鲁米特低5倍。在年轻女性中，400毫克酮康唑仅略微降低了血浆中17β-雌二醇的水平。得出的结论是，酮康唑不是临床上作为芳香化酶抑制剂的首选化合物。
