A novel synthetic vitamin-A-like compound (a polyprenoic acid derivative: E-5166) inhibits UVB-stimulated epidermal ornithine decarboxylase activity.
Irradiation of skin with ultraviolet B (UVB) stimulates epidermal activity of ornithine decarboxylase (ODC), a rate limiting polyamine biosynthesing enzyme. The maximum stimulation of ODC activity by UVB was found at 24 after irradiation. Systemic administration of a polyprenoic acid derivative (E-5166) significantly inhibited the UVB-stimulated ODC activity in a dose-dependent manner. The inhibitory effect of E-5166 on the UVB-stimulated ODC activity was found to begin at 5 mg/kg body weight. These results indicate that because it inhibits ODC activity E-5166 can be utilized for the treatment of hyperproliferative skin diseases.
D000818:Animals; D005050:Etretinate / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D051379:Mice; D009955:Ornithine Decarboxylase / Q000528:radiation effects*; D065108:Ornithine Decarboxylase Inhibitors; D012867:Skin / Q000187:drug effects / Q000201:enzymology / Q000528:radiation effects*; D014212:Tretinoin / Q000031:analogs & derivatives* / Q000494:pharmacology; D014466:Ultraviolet Rays
D065108:Ornithine Decarboxylase Inhibitors; D014212:Tretinoin; D005050:Etretinate; C034534:3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid; D009955:Ornithine Decarboxylase