12-hydroxy-5-8-10-14-eicosatetraenoic-acid and danthron

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.

Topics: 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid; Anthralin; Anthraquinones; Cell Line; Down-Regulation; Epidermis; Humans; Hydroxyeicosatetraenoic Acids; Psoriasis; Receptors, Cell Surface; Receptors, Eicosanoid