In Vitro Biological Activities of a Series of 2β-Substituted Analogues of 1α, 25-Dihydroxyvitamin D_3
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概要
- 論文の詳細を見る
Biological activities of a series of 2β-substituted analogues of 1α, 25-dihydroxyvitamin D_3 [1α, 25(OH)_2D_3] were evaluated in vitro in terms of their binding affinity with regard to calf thymus cytosolic vitamin D receptor (VDR) and rat plasma vitamin D-binding protein (DBP). Additionally, reporter gene luciferase activities using either a rat 25-hydroxyvitamin D_3-24-hydroxylase gene promoter, including two vitamin D-responsive elements (VDREs), in transfected rat osteoblast-like ROS17/2.8 cells, or a human VDR-GAL4 modified two-hybrid system in transfected human epitheloid carcinoma, cervix HeLa cells were examined. Binding affinity for VDR, transactivation potency on the target gene and VDR-mediated gene ergulation of the hydroxyalkyl and hydroxyalkoxy 2β-substituted analogues were almost comparable to those of 1α, 25(OH)_2D_3,while the alkyl and alkenyl analogues were much les active than 1α, 25(OH)_2D_3. This study investigated the biological evaluation of a series of 2β-substituted analogues at the molecular level, with regard to the structural differences of alkyl, alkenyl, hydroxyalkyl, hydroxyalkoxy, alkoxy, hydroxy and chloro substituents at the 2β-position of 1α, 25(OH)_2D_3.
- 社団法人日本薬学会の論文
- 2000-01-01
著者
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TSUGAWA Naoko
Department of Hygienic Sciences, Kobe Pharmaceutical University
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OZONO Keiichi
Department of Developmental Medicine (Pediatrics), Osaka University Graduate School of Medicine
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Okano Toshio
Department Of Hygienic Sciences Kobe Women's College Of Pharmacy
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NAKAGAWA Kimie
Department of Hygienic Science, Kobe Pharmaceutical University
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Okano Toshio
Department Of Hygienic Science Kobe Pharmaceutical University
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KUBODERA Noboru
Chugai Pharmaceutical Co. Ltd.
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Ono Yoshiyuki
Chugai Pharmaceutical Co. Ltd.
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Kubodera N
Chugai Pharmaceutical Co. Ltd. Tokyo Jpn
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KUROBE Mayuko
Department of Hygienic Sciences, Kobe Pharmaceutical University
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津川 尚子
神戸薬大
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Kurobe Mayuko
Department Of Hygienic Sciences Kobe Pharmaceutical University
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Tsugawa Naoko
Department Of Hygienic Sciences Kobe Pharmaceutical University
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Kubodera Noboru
Chugai Pharmaceutical Co.
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Ozono Keiichi
Department Of Developmental Medicine (pediatrics) D-5 Osaka University Graduate School Of Medicine
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