title: Stimulation of epidermal proliferation in mice with 1 alpha, 25-dihydroxyvitamin D3 and receptor-active 20-EPI analogues of 1 alpha, 25-dihydroxyvitamin D3.
abstract: The effects of 1 alpha, 25-dihydroxyvitamin D3 (1 alpha, 25-(OH)2D3) and receptor-active 20-epi vitamin D analogues (MC 1288, 20-epi-1 alpha, 25-(OH)2D3; MC 1301, 20-epi-24a-homo-26,27-dimethyl-1 alpha, 25-(OH)2D3, and KH 1060: 20-epi-22-oxa-24a-homo-26,27-dimethyl-1 alpha, 25-(OH)2D3) on epidermal proliferation in mice were studied in vivo. Single topical applications of all compounds induced epidermal proliferation in a dose-dependent manner. The relative potencies in vivo (KH 1060 > MC1301 > MC1288 > 1 alpha, 25-(OH)2D3) correlated well with the known activities of these compounds to inhibit U 937 cell proliferation in vitro. Vitamin D3 and 1 beta, 25-(OH)2D3, two compounds that do not bind the vitamin D receptor, did not affect epidermal proliferation. Our study shows that vitamin D3 compounds that bind to the vitamin D receptor stimulate epidermal proliferation in mice.
authors.affiliation: Leo Pharmaceutical Products, Ballerup, Denmark.
authors.forename: R
authors.initials: R
authors.lastname: Gniadecki
authors.forename: J
authors.initials: J
authors.lastname: Serup
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000502:physiology; D002455:Cell Division / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D051379:Mice; D008809:Mice, Inbred C3H; D018167:Receptors, Calcitriol / Q000037:antagonists & inhibitors*; D012867:Skin / Q000166:cytology / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D018167:Receptors, Calcitriol; C074279:KH 1060; C092473:MC 1301; D002117:Calcitriol