We. Stumpf et al., DISTRIBUTION OF 1,25-DIHYDROXYVITAMIN D-3[22-OXA] IN-VIVO RECEPTOR-BINDING IN ADULT AND DEVELOPING SKIN, Archives of dermatological research, 287(3-4), 1995, pp. 294-303
Because of the therapeutic potential of oxacalcitriol (OCT, 22-oxa-dih
ydroxyvitamin D-3), in vivo studies were conducted in adult and neonat
al rats to identify the nuclear receptor sites of action in different
tissues of the skin. Results were compared with those for 1,25-dihydro
xyvitamin D-3 (1,25(OH)(2)D-3) and oestradiol from previous studies. A
utoradiograms were prepared from the dorsal skin of adult rats and the
skin of the leg and head regions of neonatal rats 1 or 2 h after the
injection of H-3-OCT, Specific nuclear concentrations of radioactivity
, eliminated by competition with unlabelled OCT or 1,25(OH)(2)D-3, wer
e found in cells of the epidermis, outer hair sheath, hair bulb and se
baceous glands, but were absent or low in most fibroblasts of the derm
is and hypodermis. The strongest nuclear binding of OCT was conspicuou
s in outer hair sheaths, where it was 1.5 to 3.2 times higher than in
keratinocytes of the epidermis. The distribution of nuclear receptors
for OCT was similar to that for 1,25(OH)(2)D-3 but in part dissimilar
to that for oestradiol. Oestradiol binding was found in the epidermis
and hair sheaths, and also predominantly in fibroblasts of the dermis
and hair dermal papillae. The results suggest genomic regulatory effec
ts of OCT, similar to the effects of vitamin D, on proliferation, diff
erentiation and activity of keratinocytes, growth and maintenance of h
air, and proliferation and secretion of sebaceous glands. This may be
utilized therapeutically, since OCT has a lower calcaemic effect than
1,25(OH)(2)D-3.