Longcope C
Department of Obstetrics and Gynecology, University of Massachusetts Medical School, Worcester 01605.
Steroids. 1987 Jul-Sep;50(1-3):253-67. doi: 10.1016/0039-128x(83)90076-4.
Using constant infusions of 3H-labeled androgens and 14C-labeled estrogens with measurements of radiolabeled estrogens in blood and/or urine we have carried out studies on the peripheral aromatization of androgens in humans, nonhuman primates, sheep, and rabbits. In the human, aromatization is increased in women as they become postmenopausal, although the mechanism remains uncertain. In humans and cynomolgus monkeys the administration of ACTH and/or glucocorticoids does not increase peripheral aromatization, but results in a slight decrease in the aromatization of androstenedione. The administration of l-thyroxine to cynomolgus monkeys increases peripheral aromatization of androstenedione from basal, 1.16 +/- 0.15%, to 1.71 +/- 0.14% probably due to increased tissue blood flow. The aromatization of testosterone is not affected, probably due to an increase in sex hormone-binding globulin. Peripheral aromatization occurs to a similar degree in humans, rhesus and cynomolgus monkeys, and baboons, but is much lower in sheep and rabbits. The compound 10-(2-propynyl)-estr-4-ene-3,17-dione is an effective inhibitor of the peripheral aromatization of both androstenedione and testosterone.
通过持续输注³H标记的雄激素和¹⁴C标记的雌激素，并测量血液和/或尿液中放射性标记的雌激素，我们对人类、非人灵长类动物、绵羊和兔子体内雄激素的外周芳香化作用进行了研究。在人类中，女性绝经后芳香化作用增强，但其机制尚不清楚。在人类和食蟹猴中，给予促肾上腺皮质激素（ACTH）和/或糖皮质激素不会增加外周芳香化作用，但会导致雄烯二酮的芳香化作用略有下降。给食蟹猴注射左旋甲状腺素会使雄烯二酮的外周芳香化作用从基础水平的1.16±0.15%增加到1.71±0.14%，这可能是由于组织血流量增加所致。睾酮的芳香化作用不受影响，这可能是由于性激素结合球蛋白增加所致。人类、恒河猴、食蟹猴和狒狒的外周芳香化作用程度相似，但在绵羊和兔子中则低得多。化合物10 -（2 - 丙炔基）-雌-4 - 烯-3,17 - 二酮是雄烯二酮和睾酮外周芳香化作用的有效抑制剂。
