Original Article

Journal of Investigative Dermatology (1993) 100, 660–662; doi:10.1111/1523-1747.ep12472325

Spironolactone Directly Inhibits Proliferation of Cultured Human Facial Sebocytes and Acts Antagonistically to Testosterone and 5alpha-Dihydrotestosterone In Vitro

Hirohiko Akamatsu, Christos C Zouboulis and Constantin E Orfanos

Department of Dermatology, University Medical Center Steglitz, Free University of Berlin, Berlin, Germany

Received 22 January 1992; Accepted 13 January 1993.

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Abstract

Spironolactone produces antiacne effects and has recently been shown to inhibit 5alpha-dihydrotestosterone (5alpha-DHT) receptors in human sebaceous glands. We applied spironolactone alone and combined with testosterone and 5alpha-DHT to investigate its effects on the proliferation of human sebocyte cultures derived from facial skin. Secondary human facial sebocytes in 96-well culture plates were treated for 10 d by a single or combined application of testosterone (10-8-10-5 M), 5alpha-DHT (10-8-10-5 M), and spironolactone (10-12-10-7 M) in serum-free basal medium. Cell proliferation was assessed in six wells using a fluorometric assay. Testosterone and 5alpha-DHT significantly stimulated sebocyte proliferation in a dose-dependent manner, the effect being strongest with 5alpha-DHT. Spironolactone, on the other hand, caused a dose-dependent inhibition (25% and 50% at 10- 9 and 10-7 M, respectively). Combined treatment of human facial sebocytes with spironolactone and testosterone or 5alpha-DHT resulted in a lower proliferation than with androgens alone. The fact that spironolactone directly and dose dependently inhibits the proliferation of cultured human facial sebocytes and acts antagonistically to testosterone and 5alpha-DHT at the cellular level is indicative of a receptor-mediated effect.

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