Spironolactone directly inhibits proliferation of cultured human facial sebocytes and
acts antagonistically to testosterone and 5 alpha-dihydrotestosterone in vitro.
Author
Akamatsu H; Zouboulis CC; Orfanos CE
Address
Department of Dermatology, University Medical Center Steglitz, Free University of
Berlin, Germany.
Source
J Invest Dermatol, 1993 May, 100:5, 660-2
Abstract
Spironolactone produces antiacne effects and has recently been shown to inhibit 5
alpha-dihydrotestosterone (5 alpha-DHT) receptors in human sebaceous glands. We applied
spironolactone alone and combined with testosterone and 5 alpha-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), 5 alpha-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 5
alpha-DHT significantly stimulated sebocyte proliferation in a dose-dependent manner, the
effect being strongest with 5 alpha-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 5 alpha-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 5 alpha-DHT at the cellular level
is indicative of a receptor-mediated effect.