Inhibition of 5α-Reductase Activity in SZ95 Sebocytes and HaCaT Keratinocytes In Vitro
Abstract
Inhibition of 5alpha-reductase type 1 has been considered to be a promising target for treatment of androgen-dependent skin disorders, however, currently published clinical results on acne treatment are rather disappointing. In this study, the influence of selective inhibitors of 5alpha-reductase on testosterone metabolism within SZ95 sebocytes and HaCaT keratinocytes IN VITRO was investigated. In both cell types, the isotype 1 inhibitor MK386 completely inhibited the conversion of testosterone to 5alpha-dihydrotestosterone in concentrations higher than 10 (-9) M. Inhibitors of the isotype 2 such as finasteride, dihydrofinasteride, and turosteride, were >100-fold less active, while, as expected, androgen receptor inhibitors did not affect the 5alpha-reductase activity. MK386, but not finasteride, reduced testosterone-stimulated proliferation and slightly reduced the testosterone-induced increase in the amount of SZ95 sebocyte proteins. The androgen receptor inhibitor cyproterone acetate exhibited no effect on testosterone-induced proliferation, but inhibited the 5alpha-dihydrotestosterone-induced sebocyte proliferation. Our experimental findings and the existing clinical results indicate that the inhibition of 5alpha-reductase activity alone may be insufficient to reduce overall sebocyte activity and improve acne lesions.
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- Authors
- Seiffert, K., Seltmann, H., Fritsch, M., & Zouboulis, C.
- ORCID
- Zouboulis, C.
- Venue
- Hormone and Metabolic Research
- Publisher
- Georg Thieme Verlag KG
- Published
- 2007-02
- Volume
- 39
- Issue
- 2
- Pages
- 141-148
- ISSN
- 0018-5043 (ISSN-L)
- 1439-4286
- OpenAlex
- W1975206613
- Cited by
- 28
- References
- 0
- Citations by year
- 2024: 3 · 2022: 3 · 2020: 4 · 2017: 2 · 2016: 1 · 2015: 2 · 2014: 2 · 2013: 1 · 2012: 2
- FWCI
- 2.55
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Hormone and Metabolic Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Dermatology › Acne and Rosacea Treatments and Effects
- Health Sciences › Medicine › Dermatology › Dermatology and Skin Diseases
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Keywords
- 5α-reductase inhibition, 5α-reductase type 1, dihydrotestosterone, testosterone metabolism, sebocytes, keratinocytes, acne, finasteride, cyproterone acetate, androgen receptor
- MeSH terms
- Androgens, Azasteroids, Cells, Cultured, Humans, Sebaceous Glands, Testosterone, Protein Biosynthesis, Keratinocytes, Finasteride, Cholestenone 5 alpha-Reductase, Cell Proliferation, Androgen Receptor Antagonists
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