Nguyen Q H, Chen T, Wang X, Chen Y, Chien P
Institute of Chemical Biology, University of San Francisco, CA 94117-1080, USA.
Int J Dermatol. 1995 Oct;34(10):720-5. doi: 10.1111/j.1365-4362.1995.tb04663.x.
The potential role of finasteride in treating androgen related skin disorders was investigated.
Pooled human dermal fibroblasts were used to assess the effect of finasteride on the 5 alpha-reductase activity in skin tissue. Vmax and Km were estimated in the presence of 0, 10, and 200 nM finasteride.
Vmax values remain constant near 1.20 pmol/mg protein/h in the presence of increasing concentrations of finasteride; however, apparent Km increases from 0.27 nM at 0 nM finasteride to 0.31 nM and 0.44 nM at 10 nM and 200 nM finasteride, respectively. This suggests that finasteride competes with testosterone and has a high affinity for same binding site of the 5 alpha-reductase enzyme. Apparent Ki was estimated at 282 nM, indicating that a high concentration of finasteride is required to significantly suppress the enzyme activity.
This study confirms that finasteride inhibits the conversion of testosterone to dihydrotestosterone in human reticular dermal fibroblasts. Finasteride may have therapeutic potential in treating skin disorders influenced by the action of dihydrotestosterone.
研究了非那雄胺在治疗雄激素相关皮肤疾病中的潜在作用。
使用汇集的人真皮成纤维细胞评估非那雄胺对皮肤组织中5α-还原酶活性的影响。在存在0、10和200 nM非那雄胺的情况下估计Vmax和Km。
在非那雄胺浓度增加的情况下，Vmax值在1.20 pmol/mg蛋白质/小时附近保持恒定；然而，表观Km分别从0 nM非那雄胺时的0.27 nM增加到10 nM和200 nM非那雄胺时的0.31 nM和0.44 nM。这表明非那雄胺与睾酮竞争，并且对5α-还原酶的相同结合位点具有高亲和力。表观Ki估计为282 nM，表明需要高浓度的非那雄胺才能显著抑制酶活性。
本研究证实非那雄胺抑制人网状真皮成纤维细胞中睾酮向二氢睾酮 的转化。非那雄胺在治疗受二氢睾酮作用影响的皮肤疾病方面可能具有治疗潜力。
