Metabolism of an aromatic retinoid Ro 10-9359 by cultured human epidermal keratinocytes.
An aromatic retinoid Ro 10-9359 is metabolized after absorption from intestine to form Ro 10-1670 which is an active therapeutic compound. The epidermal keratinocytes, a main target tissue of retinoid therapy in dermatology, was examined in the capacity to metabolize the retinoid. The culture of human epidermal keratinocytes was treated with 10(-6) M Ro 10-9359 and the metabolites released in the medium was analyzed by HPLC. The HPLC profile showed a distinct peak of Ro 10-1670. The human skin fibroblasts, HeLa cells. Chang liver cells and 3T3 cells were less active in metabolizing Ro 10-9359, and only a small amount of Ro 10-1670 was detected in the culture of human skin fibroblasts treated with 10(-6) M Ro 10-9359 for 2 days. When these cells were disrupted by a glass homogenizer, and incubated with Ro 10-9359, no Ro 10-1670 formation was detected.
D017255:Acitretin; D000818:Animals; D002478:Cells, Cultured; D002648:Child; D004817:Epidermis / Q000378:metabolism*; D005050:Etretinate / Q000378:metabolism*; D005260:Female; D005347:Fibroblasts / Q000378:metabolism; D006367:HeLa Cells / Q000378:metabolism; D006801:Humans; D007633:Keratins / Q000096:biosynthesis*; D008099:Liver / Q000378:metabolism; D051379:Mice; D014212:Tretinoin / Q000031:analogs & derivatives* / Q000378:metabolism
D014212:Tretinoin; D005050:Etretinate; D007633:Keratins; D017255:Acitretin