Serafini P C, Catalino J, Lobo R A
J Steroid Biochem. 1985 Aug;23(2):191-4. doi: 10.1016/0022-4731(85)90236-5.
The effect of spironolactone (S) on genital skin 5 alpha-reductase activity (5 alpha-RA) of hirsute women (HW) in vivo as well as in normal genital skin in vitro was evaluated. Thirteen HW (Ferriman-Gallwey score of 23.3 +/- 2.8) received S 100 mg twice a day for a month. Twenty-three non-hirsute women were selected as controls for the assessment of genital skin 5 alpha-RA. S was added to incubations of genital skin from 9 additional controls in vitro in concentrations from 1.2 X 10(-8) to 10(-5) M. HW had significantly higher conversion ratios (CR) of T to DHT compared to controls (P less than 0.05). Post treatment values for the CR T to DHT were significantly lower than prior to S (17.5 +/- 1.7 and 8.05 +/- 1.2%, P less than 0.05) and the mass of DHT produced also decreased by 37 +/- 9% (P less than 0.05). The CR T to 3 alpha-diol decreased by 30 +/- 9% (P less than 0.05). In 11 of 13 women, a significant reduction of 5 alpha-RA was demonstrated while in 2 patients the activity remained unchanged. The maximum in vitro inhibitory effect of S on the CR T to DHT occurred with a concentration of 1.2 X 10(-5) M (P less than 0.01). In conclusion, S has a direct inhibitory effect on 5 alpha-RA. The beneficial effect of S treatment in HW may be related, in part, to this inhibition of 5 alpha-RA.
评估了螺内酯(S)对多毛症女性(HW)体内生殖器皮肤5α-还原酶活性(5α-RA)以及对正常生殖器皮肤体外5α-还原酶活性的影响。13名多毛症女性(费里曼-高尔韦评分23.3±2.8)每天服用两次100毫克S,持续一个月。选择23名非多毛症女性作为评估生殖器皮肤5α-RA的对照。在体外,将S以1.2×10⁻⁸至10⁻⁵M的浓度添加到另外9名对照的生殖器皮肤孵育物中。与对照相比,多毛症女性中睾酮(T)向双氢睾酮(DHT)的转化率(CR)显著更高(P<0.05)。S治疗后T向DHT的CR值显著低于治疗前(分别为17.5±1.7%和8.05±1.2%,P<0.05),并且产生的DHT量也减少了37±9%(P<0.05)。T向3α-二醇的CR降低了30±9%(P<0.05)。13名女性中有11名显示5α-RA显著降低,而2名患者的活性保持不变。S对T向DHT的CR的最大体外抑制作用发生在浓度为1.2×10⁻⁵M时(P<0.01)。总之,S对5α-RA有直接抑制作用。S治疗多毛症女性的有益效果可能部分与此对5α-RA的抑制有关。