Kemény L, Gross E, Arenberger P, Ruzicka T
Department of Dermatology, University of Munich, Federal Republic of Germany.
Arch Dermatol Res. 1991;283(5):333-6. doi: 10.1007/BF00376623.
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.
研究了地蒽酚及其治疗无活性的氧化产物丹蒽醌对12(S)-HETE与人表皮细胞系SCL-II结合的影响。与丹蒽醌不同，地蒽酚（0.25 - 1微克/毫升）以剂量依赖方式诱导12(S)-HETE结合显著减少。抑制作用在6小时的潜伏期后出现，在18 - 24小时达到最大值，此后缓慢下降。在浓度为1微克/毫升时，该药物导致特异性高亲和力12(S)-HEFE受体数量（Bmax）下降约50%，而受体亲和力（Kd）无变化。地蒽酚对表皮细胞上12(S)-HETE受体的下调作用可能有助于其抗银屑病作用。
