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FINASTERIDE INHIBITS 5α‐REDUCTASE ACTIVITY IN HUMAN DERMAL FIBROBLASTS: PREDICTION OF ITS THERAPEUTIC APPLICATION IN ANDROGEN‐RELATED SKIN DISEASES
Author(s) -
NGUYEN QUAN H.,
CHEN TAO,
WANG XUESHENG,
CHEN YING,
CHIEN PAUL
Publication year - 1995
Publication title -
international journal of dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.677
H-Index - 93
eISSN - 1365-4632
pISSN - 0011-9059
DOI - 10.1111/j.1365-4362.1995.tb04663.x
Subject(s) - finasteride , dihydrotestosterone , testosterone (patch) , 5 alpha reductase inhibitor , medicine , endocrinology , androgen , enzyme , reductase , pharmacology , chemistry , prostate , biochemistry , hormone , cancer
Background. The potential role of finasteride in treating androgen related skin disorders was investigated. Methods. Pooled human dermal fibroblasts were used to assess the effect of finasteride on the 5α‐reductase activity in skin tissue. V max and K m were estimated in the presence of 0, 10, and 200 nM finasteride. Results. V max values remain constant near 1.20 pmol/mg protein/h in the presence of increasing concentrations of finasteride; however, apparent K m 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 ministered competes with testosterone and has a high affinity for same binding site of the 5α‐reductase enzyme. Apparent K i was estimated at 282 nM, indicating that a high concentration of finasteride is required to significantly suppress the enzyme activity. Conclusions. 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.