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Title: The biological-activity of 23-oxa-dihydroxyvitamin-d-3, 23-oxa-24-oxo-dihydroxyvitamin-d-3, and 23-thia-dihydroxyvitamin-d-3
Authors: Allewaert, K
Convents, R
Tan, Bk
Marcelis, S
Zhao, J
Zhao, Xy
Declercq, P
Vandewalle, M
Bouillon, Roger #
Issue Date: Dec-1994
Publisher: Butterworth-heinemann
Series Title: Steroids vol:59 issue:12 pages:686-690
Abstract: Three analogs of 1 alpha,25-(OH)(2)D-3 with an oxygen ol another heteroatom at position 23 were synthesized in search of separating the cell-differentiating from the calcemic effects of the vitamin D hormone. Their ability to induce superoxide production in human myeloid leukemia cells (HL-60) was 1 alpha,25-(OH)(2)D-3 > 23-oxa-24-oxo-1 alpha,25-(OH)(2)D-3 > 23-thia-1 alpha,25-(OH)(2)D-3 > 23-oxa-1 alpha,25-(OH)(2)D-3. 23-oxa-24-oxo-1 alpha,25(OH)(2)D-3 was slightly more potent than 1 alpha,25-(OH)(2)D-3 in inhibiting cell proliferation in MCF-7 cells and 23-thia- and 23-oxa-1 alpha,25(OH)(2)D-3 were less potent. Their in vitro potency to produce osteocalcin in MG-63 cells was 1 alpha,25-(OH)(2)D-3 > 23-oxa-24-oxo-1 alpha,25-(OH)(2)D-3 > 23-thia-1 alpha,25-(OH)(2)D-3 = 23-oxa-1 alpha,25-(OH)(2)D-3. All three analogs had reduced receptor and DBP affinity compared to 1 alpha,25-(OH)(2)D-3. When these analogs were injected in rachitic chicks, only little calcemic effects were observed. The introduction of a heteroatom in carbon 23 of 1 alpha,25-(OH)(2)D-3 thus creates analogs with dissociated action on cell differentiation and calcium homeostasis.
ISSN: 0039-128X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Clinical and Experimental Endocrinology
# (joint) last author

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