THE CHEMISTRY AND CONFORMATIONAL AND BIOLOGICAL ANALYSIS OF VITAMIN D3, ITS METABOLITES AND ANALOGUES |
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| Authors: | ANTHONY W. NORMAN R. LORNE JOHNSON TERRY W. OSBORN DANA A. PROSAL STEPHEN C. CAREY MILTON L. HAMMOND MANINDARAN N. MITRA MARCEL R. PIRIO ALBERT REGO RICHARD M. WING WILLIAM H. OKAMURA |
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| Affiliation: | Department of Biochemistry and Chemistry, University of Californaiam Riverside, California, U.S.A. |
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| Abstract: | The chemical properties, sterochemical relationships and solution confromation, as assessed in part by proton NMR spectroscopy, for vitamin D3, its major metabolites [including 1α, 25-(OH)2 D3, its hormonally active form] and a number of A-ring and side chain analogues are evaluated and discussed in relation ot their biological activity. In particular the relative ability of many of these seco-steroids to compet both with 25-OHD3 for its chick serum binding protein and 1α, 25-(OH)2-D3 for its chick intenstinal cytosol-chromation receptor systme was quantitated, in vitro , Further, the relative effectiveness of all these metabolites and analogues to mediate in vivo intestinal calcium absorption and bone calcium mobilization was determined. Collectiveily these chemical and bilogical studies constitute a 'systems analysis'of the various steroid structural parameters both required and tolerated by the multi-stepped endocrine system associated with the bilogical actions of vitamin D. |
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