期刊名称：Journal of Nutritional Science and Vitaminology
印刷版ISSN：0301-4800
电子版ISSN：1881-7742
出版年度：1999
卷号：45
期号：3
页码：239-249
DOI：10.3177/jnsv.45.239
出版社：Center for Academic Publications Japan
摘要：26, 27-Hexafluoro-1α, 25-dihydroxyvitamin D3 [F6-1, 25-(OH)2D3] is more potent than 1α, 25-dihydroxyvitamin D3 [l, 25(OH)2D3] in stimulating bone resorption in vitro and in vivo. The reason why F6-1, 25(OH)2D3 is more active remains unclear. To clarify the relationship between the bone-resorbing activity of each vitamin D3 analogue and the metabolism of each analogue, in the present study, we used an ex vivo method that was established by Reynolds et al ( Calcif Tissue Res , 1974, 15, 333-339). The effect of F6-1, 25(OH)2D3 or 1, 25(OH)2D3 on 45Ca release from parietal bones, prepared at 3, 14 and 24 h after injection of 1.9, 3.8, 7.6 or 15.2 pmol vitamin D analog /g body weight, was examined. F6-1, 25(OH)2D3 was more potent than 1, 25(OH)2D3 during each in vivo time period. 1, 25(OH)2D3 at 3h after the injection was more active compared to the control (no injection of 1, 25(OH)2D3), but not at 14 and 24h. The radioactivity of the bones after the injection of [3H]-F6-, 25(OH)2D3 was retained even at 24h. In the case of [3H]-1, 25(OH)2D3, the radioactivity of bones decreased with an increase in the in vivo period. In a HPLC analysis of the lipid extract of bone homogenate, [3H]-F6-1, 25(OH)2D3 alone was detected at 3 h after the injection and both [3H]-F6-1, 25(OH)2D3 and [3H]-26, 27-hexafluoro-1α, 23S, 25-trihydroxy-vitamin D3 [F6-1, 23, 25(OH)3D3] were detected at 14 and 24h after the injection. [3H]-1, 25(OH)2D3 was highly detected at 3 h after the injection, but it decreased with an increase in the in vivo period. In the ex vivo test, the activity of F6-1, 23, 25(OH)3D3 was less than that of F6-1, 25(OH)2D3 but similar to that of 1, 25(OH)2D3. The present study indicates that F6-1, 25(OH)2D3 is more active and more long-lasting than 1, 25(OH)2D3 in the ex vivo method. A higher potency of F6-1, 25(OH)2D3 is explained, at least partly, by the results that the amounts of both F6-1, 25(OH)2D3 and its active metabolite, F6-1, 23, 25(OH)3D3, in the bones are higher than that of 1, 25(OH)2D3, and that F6-1, 25(OH)2D3 and its metabolite are retained in bones longer than 1, 25(OH)2D3.
关键词：1α,25-dihydroxyvitamin D3;26,27-hexafluoro-1α,25-dihy-droxyvitamin D3;26,27-hexafluoro-lα,23,25-trihydroxyvitamin D3;ex vivo bone resorption;neonatal mouse calvaria
