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Biologic activity of dihydroxylated 19-nor-(pre)vitamin-D(3)

Roger Bouillon, Luis A. Sarandeses, Katrien Allewaert, Jie Zhao, J. Luis Mascareñas, Antonio Mouriño, Sara Vrielynck, Pierre De Clercq (UGent) and Maurits Vandewalle
(1993) JOURNAL OF BONE AND MINERAL RESEARCH. 8(8). p.1009-1015
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Abstract
Vitamin D3 and its hydroxylated metabolites are normally in thermal equilibrium with their previtamin D isomers. To evaluate the biologic activity of 1alpha,25-dihydroxyprevitamin D3, we synthesized 19-nor analogs of 1alpha,25-dihydroxy(pre)vitamin D3 because the absence of a C19 methylene group prevents the isomerization of these analogs. The affinity of 1alpha,25-(OH)2D3-19-nor-D3 for the intestinal vitamin D receptor and plasma vitamin D binding protein was mildly decreased [30 and 20% of the affinity of 1alpha,25-(OH)2D3, respectively], but the affinity of 1alpha,25-(OH)2-19-nor-previtamin D3 was only 1 and 6% of that of 1alpha,25-(OH)2D3 for the receptor and DBP, respectively. The in vitro effects on human promyeloid leukemia (HL-60 cell) differentiation and osteocalcin secretion by human osteosarcoma (MG-63) cells by 1alpha,25-(OH)2-19-nor-D3 were nearly identical to those of 1alpha-25-(OH)2D3, whereas 19-nor-previtamin D3 showed poor activity (2%). The in vivo calcemic effects of both analogs, studied in vitamin D-deficient chicks treated for 10 consecutive days with the analogs, showed no activity of the previtamin D3 analog and reduced calcemic effects (less-than-or-equal-to 10%) of 1alpha,25-(OH)2-19-nor-D3. We conclude that the previtamin D form of 1alpha,25-(OH)2D3 has lost most of its biologic activity in vitro and in vivo.
Keywords
VITAMIN-D ANALOGS, D-BINDING-PROTEIN, INVITRO, SYSTEM

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MLA
Bouillon, Roger, et al. “Biologic Activity of Dihydroxylated 19-nor-(Pre)Vitamin-D(3).” JOURNAL OF BONE AND MINERAL RESEARCH, vol. 8, no. 8, 1993, pp. 1009–15.
APA
Bouillon, R., Sarandeses, L. A., Allewaert, K., Zhao, J., Mascareñas, J. L., Mouriño, A., … Vandewalle, M. (1993). Biologic activity of dihydroxylated 19-nor-(pre)vitamin-D(3). JOURNAL OF BONE AND MINERAL RESEARCH, 8(8), 1009–1015.
Chicago author-date
Bouillon, Roger, Luis A. Sarandeses, Katrien Allewaert, Jie Zhao, J. Luis Mascareñas, Antonio Mouriño, Sara Vrielynck, Pierre De Clercq, and Maurits Vandewalle. 1993. “Biologic Activity of Dihydroxylated 19-nor-(Pre)Vitamin-D(3).” JOURNAL OF BONE AND MINERAL RESEARCH 8 (8): 1009–15.
Chicago author-date (all authors)
Bouillon, Roger, Luis A. Sarandeses, Katrien Allewaert, Jie Zhao, J. Luis Mascareñas, Antonio Mouriño, Sara Vrielynck, Pierre De Clercq, and Maurits Vandewalle. 1993. “Biologic Activity of Dihydroxylated 19-nor-(Pre)Vitamin-D(3).” JOURNAL OF BONE AND MINERAL RESEARCH 8 (8): 1009–1015.
Vancouver
1.
Bouillon R, Sarandeses LA, Allewaert K, Zhao J, Mascareñas JL, Mouriño A, et al. Biologic activity of dihydroxylated 19-nor-(pre)vitamin-D(3). JOURNAL OF BONE AND MINERAL RESEARCH. 1993;8(8):1009–15.
IEEE
[1]
R. Bouillon et al., “Biologic activity of dihydroxylated 19-nor-(pre)vitamin-D(3),” JOURNAL OF BONE AND MINERAL RESEARCH, vol. 8, no. 8, pp. 1009–1015, 1993.
@article{202554,
  abstract     = {{Vitamin D3 and its hydroxylated metabolites are normally in thermal equilibrium with their previtamin D isomers. To evaluate the biologic activity of 1alpha,25-dihydroxyprevitamin D3, we synthesized 19-nor analogs of 1alpha,25-dihydroxy(pre)vitamin D3 because the absence of a C19 methylene group prevents the isomerization of these analogs. The affinity of 1alpha,25-(OH)2D3-19-nor-D3 for the intestinal vitamin D receptor and plasma vitamin D binding protein was mildly decreased [30 and 20% of the affinity of 1alpha,25-(OH)2D3, respectively], but the affinity of 1alpha,25-(OH)2-19-nor-previtamin D3 was only 1 and 6% of that of 1alpha,25-(OH)2D3 for the receptor and DBP, respectively. The in vitro effects on human promyeloid leukemia (HL-60 cell) differentiation and osteocalcin secretion by human osteosarcoma (MG-63) cells by 1alpha,25-(OH)2-19-nor-D3 were nearly identical to those of 1alpha-25-(OH)2D3, whereas 19-nor-previtamin D3 showed poor activity (2%). The in vivo calcemic effects of both analogs, studied in vitamin D-deficient chicks treated for 10 consecutive days with the analogs, showed no activity of the previtamin D3 analog and reduced calcemic effects (less-than-or-equal-to 10%) of 1alpha,25-(OH)2-19-nor-D3. We conclude that the previtamin D form of 1alpha,25-(OH)2D3 has lost most of its biologic activity in vitro and in vivo.}},
  author       = {{Bouillon, Roger and Sarandeses, Luis A. and Allewaert, Katrien and Zhao, Jie and Mascareñas, J. Luis and Mouriño, Antonio and Vrielynck, Sara and De Clercq, Pierre and Vandewalle, Maurits}},
  issn         = {{0884-0431}},
  journal      = {{JOURNAL OF BONE AND MINERAL RESEARCH}},
  keywords     = {{VITAMIN-D ANALOGS,D-BINDING-PROTEIN,INVITRO,SYSTEM}},
  language     = {{eng}},
  number       = {{8}},
  pages        = {{1009--1015}},
  title        = {{Biologic activity of dihydroxylated 19-nor-(pre)vitamin-D(3)}},
  volume       = {{8}},
  year         = {{1993}},
}
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