Further studies on the androgenic, anti-androgenic, and synandrogenic actions of progestins.
Further studies on the androgenic, anti-androgenic, and synandrogenic actions of progestins.
复制标题
进一步研究孕激素的雄激素、抗雄激素和协同雄激素作用。
作者：
C. Gupta;L. Bullock;C. Bardin
在小鼠的肾近曲小管中，替吉奥使特定蛋白质的活性增加高达50倍。已知几种孕激素通过模拟、抑制或增强雄激素作用来改变这些效应。在本研究中，以肾β-葡萄糖醛酸酶和乙醇脱氢酶活性为终点，检测了一系列C-21和C-18孕激素相对于睾酮的雄激素作用。然后通过使用固定剂量的睾酮（0.1 mg/天）和不同量的孕激素（0.05-1.0 mg/天）来检查这些类固醇的抗雄激素和联雄激素活性。孕酮衍生物的雄激素活性与6α-甲基取代有关。然而，17α-羟基抑制而17α-乙酰氧基增强GO取代类固醇的雄激素活性。所有C-18孕激素（norethynodrel、d-炔诺孕酮和lynestrenol）对小鼠肾脏均具有轻度雄激素性。因为很少有类固醇是抗雄激素的，没有...
Testosterone increases the activity of specific proteins up to 50-fold in the renal proximal convoluted tubule of the mouse. Several progestins are known to modify these effects by mimicking, inhibiting, or potentiating androgen action. In the present study, a series of C-21 and C-18 progestins were examined for their androgenic actions relative to testosterone by using renal β-glucuronidase and alcohol dehydrogenase activities as end points. These steroids were then examined for anti-androgenic and synandrogenic activities by using a fixed dose of testosterone (0.1 mg/day) and varying amounts of progestins (0.05–1.0-mg/day). The androgenic activity of the progesterone derivatives correlated with 6α-methyl substitution. However, a 17α-hydroxyl group inhibited while a 17α-acetoxy group enhanced the androgenic activity of the Go-substituted steroids. All of the C-18 progestins (norethynodrel, d-norgestrel, and lynestrenol) were mildly androgenic on mouse kidney. Because few steroids were anti-androgenic, no...