Dithranol-induced down-regulation of 12(S)-hydroxyeicosatetraenoic acid [12(S)-HETE] receptors in a human epidermal cell line

Arch Dermatol Res. 1991;283(5):333-6. doi: 10.1007/BF00376623.

Abstract

The effects of dithranol and its therapeutically inactive oxidation product, danthrone, on 12(S)-HETE binding to the human epidermal cell line SCL-II were studied. Dithranol (0.25-1 microgram/ml), in contrast to danthrone, induced a substantial decrease in 12(S)-HETE binding in a dose-dependent manner. The inhibition occurred after a latency period of 6 h, reached its maximum at 18-24 h and slowly declined thereafter. At a concentration of 1 microgram/ml, the drug led to an approximately 50% decrease in the number of specific high-affinity 12(S)-HEFE receptors (Bmax), whereas receptor affinity (Kd) showed no change. The down-regulation of 12(S)-HETE receptors on epidermal cells by dithranol may contribute to its antipsoriatic action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid
  • Anthralin / pharmacology*
  • Anthralin / therapeutic use
  • Anthraquinones / pharmacology
  • Cell Line
  • Down-Regulation
  • Epidermis / chemistry*
  • Humans
  • Hydroxyeicosatetraenoic Acids / metabolism*
  • Psoriasis / drug therapy
  • Receptors, Cell Surface / analysis*
  • Receptors, Cell Surface / metabolism
  • Receptors, Eicosanoid*

Substances

  • 12-hydroxyeicosatetraenoic acid receptor
  • Anthraquinones
  • Hydroxyeicosatetraenoic Acids
  • Receptors, Cell Surface
  • Receptors, Eicosanoid
  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid
  • Anthralin
  • danthron