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Modulation of androgen receptor transcriptional activity by anti-acne reagents

Shigeki Inui1, Toshifumi Nakao, Satoshi Itami

  • 1Department of Dermatology, Course of Molecular Medicine, Graduate School of Medicine, Osaka University, Osaka, 2-2, C5, Yamada-oka, Suita-shi, Osaka 565-0871, Japan. inui@derma.med.osaka-u.ac.jp

Journal of Dermatological Science
|November 3, 2004
PubMed
Abstract

Insights

This study investigated the anti-androgenic effects of common anti-acne medications. Nadifloxacin (NDFX) and roxithromycin (RXM) showed significant suppression of androgen receptor activity, with a synergistic effect observed when used together.

Area of Science:

  • Pharmacology
  • Dermatology
  • Molecular Biology

Background:

  • Previous studies explored roxithromycin's (RXM) anti-androgenic activity using human dermal fibroblasts and the androgen receptor (AR) coactivator ARA55.
  • This research aimed to further investigate RXM and other anti-acne agents for their potential anti-androgenic properties.

Purpose of the Study:

  • To evaluate the anti-androgenic activity of nadifloxacin (NDFX), RXM, all-trans retinoic acid (atRA), and glycolic acid (GA).
  • To utilize CV-1 cells in transient transfection assays as a sensitive system for detecting anti-androgenic effects.

Main Methods:

  • CV-1 cells were transiently transfected for androgen receptor (AR) transcriptional activity assays.
  • Cells were treated with varying concentrations of NDFX, RXM, atRA, and GA, with R1881 used as an inducer.

Main Results:

  • Roxithromycin (RXM) at 5 microg/ml suppressed R1881-induced AR activity by 21.2%.
  • Nadifloxacin (NDFX) at 50 microg/ml suppressed AR activity by 29.8%.
  • A combination of NDFX and RXM demonstrated a synergistic effect, with NDFX (5-50 microg/ml) inhibiting AR transactivity by 32.7-61.0% in the presence of RXM.
  • All-trans retinoic acid (atRA) at 10(-5)M suppressed AR activity by 50%, while glycolic acid (GA) showed no significant effect.

Conclusions:

  • The study demonstrates that commonly used anti-acne agents possess anti-androgenic properties.
  • These findings suggest a potential mechanism for the efficacy of these agents in treating acne through the modulation of androgenic pathways.

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