Biological activity of 1,25-dihydroxyvitamin D2 and 24-epi-1,25-dihydroxyvitamin D2

H. F. DeLuca, R. R. Sicinski, Y. Tanaka, P. H. Stern and C. M. Smith Department of Biochemistry, University of Wisconsin-Madison 53706. The biological activity of 1,25-dihydroxyvitamin D2 [1,25(OH)2D2] and 24-epi-1,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2] has been determined in vitamin D-deficien...

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Veröffentlicht in:American journal of physiology: endocrinology and metabolism 1988-04, Vol.254 (4), p.E402-E406
Hauptverfasser: DeLuca, H.F, Sicinski, R.R, Tanaka, Y, Stern, P.H, Smith, C.M
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container_end_page E406
container_issue 4
container_start_page E402
container_title American journal of physiology: endocrinology and metabolism
container_volume 254
creator DeLuca, H.F
Sicinski, R.R
Tanaka, Y
Stern, P.H
Smith, C.M
description H. F. DeLuca, R. R. Sicinski, Y. Tanaka, P. H. Stern and C. M. Smith Department of Biochemistry, University of Wisconsin-Madison 53706. The biological activity of 1,25-dihydroxyvitamin D2 [1,25(OH)2D2] and 24-epi-1,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2] has been determined in vitamin D-deficient rats. The biological effectiveness of 1,25(OH)2D2 is equal to that reported previously for 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] (15) in intestinal calcium transport, mineralization of bone, mobilization of bone calcium, and elevation of plasma inorganic phosphorus of rachitic rats. However, 24-epi-1,25(OH)2D2 is at best one-half as active as 1,25(OH)2D2 in stimulating intestinal calcium transport and in the mineralization of rachitic bone. The 24-epi-1,25(OH)2D2 is one-third as active as 1,25(OH)2D3 in binding to the chick intestinal receptor for 1,25(OH)2D3. Thus receptor discrimination may account for the twofold difference in intestinal calcium transport activity. 24-Epi-1,25(OH)2D2 appeared inactive in in vivo mobilization of bone calcium or bone phosphorus. On the other hand, in fetal rat bone in culture, the epi compound was only five times less active than 1,25(OH)2D2 in inducing resorption. Short-term experiments on bone mineral mobilization in vivo show that the 24-epi-1,25(OH)2D2 does induce bone calcium mobilization but that its activity in this respect is short lived. It is suggested that 24-epi-1,25(OH)2D2 and, as a result, it shows preferential activity on intestine whose response to a single dose of 1,25(OH)2D2 remains for several days, whereas the short-lived bone system does not remain stimulated during the 24-h period between doses.
doi_str_mv 10.1152/ajpendo.1988.254.4.E402
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F. DeLuca, R. R. Sicinski, Y. Tanaka, P. H. Stern and C. M. Smith Department of Biochemistry, University of Wisconsin-Madison 53706. The biological activity of 1,25-dihydroxyvitamin D2 [1,25(OH)2D2] and 24-epi-1,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2] has been determined in vitamin D-deficient rats. The biological effectiveness of 1,25(OH)2D2 is equal to that reported previously for 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] (15) in intestinal calcium transport, mineralization of bone, mobilization of bone calcium, and elevation of plasma inorganic phosphorus of rachitic rats. However, 24-epi-1,25(OH)2D2 is at best one-half as active as 1,25(OH)2D2 in stimulating intestinal calcium transport and in the mineralization of rachitic bone. The 24-epi-1,25(OH)2D2 is one-third as active as 1,25(OH)2D3 in binding to the chick intestinal receptor for 1,25(OH)2D3. Thus receptor discrimination may account for the twofold difference in intestinal calcium transport activity. 24-Epi-1,25(OH)2D2 appeared inactive in in vivo mobilization of bone calcium or bone phosphorus. On the other hand, in fetal rat bone in culture, the epi compound was only five times less active than 1,25(OH)2D2 in inducing resorption. Short-term experiments on bone mineral mobilization in vivo show that the 24-epi-1,25(OH)2D2 does induce bone calcium mobilization but that its activity in this respect is short lived. 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F. DeLuca, R. R. Sicinski, Y. Tanaka, P. H. Stern and C. M. Smith Department of Biochemistry, University of Wisconsin-Madison 53706. The biological activity of 1,25-dihydroxyvitamin D2 [1,25(OH)2D2] and 24-epi-1,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2] has been determined in vitamin D-deficient rats. The biological effectiveness of 1,25(OH)2D2 is equal to that reported previously for 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] (15) in intestinal calcium transport, mineralization of bone, mobilization of bone calcium, and elevation of plasma inorganic phosphorus of rachitic rats. However, 24-epi-1,25(OH)2D2 is at best one-half as active as 1,25(OH)2D2 in stimulating intestinal calcium transport and in the mineralization of rachitic bone. The 24-epi-1,25(OH)2D2 is one-third as active as 1,25(OH)2D3 in binding to the chick intestinal receptor for 1,25(OH)2D3. Thus receptor discrimination may account for the twofold difference in intestinal calcium transport activity. 24-Epi-1,25(OH)2D2 appeared inactive in in vivo mobilization of bone calcium or bone phosphorus. On the other hand, in fetal rat bone in culture, the epi compound was only five times less active than 1,25(OH)2D2 in inducing resorption. Short-term experiments on bone mineral mobilization in vivo show that the 24-epi-1,25(OH)2D2 does induce bone calcium mobilization but that its activity in this respect is short lived. It is suggested that 24-epi-1,25(OH)2D2 and, as a result, it shows preferential activity on intestine whose response to a single dose of 1,25(OH)2D2 remains for several days, whereas the short-lived bone system does not remain stimulated during the 24-h period between doses.</description><subject>ABSORCION</subject><subject>ABSORPTION</subject><subject>Animals</subject><subject>BONE DISEASES</subject><subject>Bone Resorption - drug effects</subject><subject>CALCIO</subject><subject>Calcitriol - pharmacology</subject><subject>CALCIUM</subject><subject>Calcium - metabolism</subject><subject>Chickens</subject><subject>ENFERMEDADES OSEAS</subject><subject>Ergocalciferols - analogs &amp; derivatives</subject><subject>Ergocalciferols - metabolism</subject><subject>Ergocalciferols - pharmacology</subject><subject>Intestinal Absorption - drug effects</subject><subject>Intestines - metabolism</subject><subject>Kinetics</subject><subject>Male</subject><subject>NUTRITIVE VALUE</subject><subject>OSTEOPATHIE</subject><subject>Rats</subject><subject>Receptors, Calcitriol</subject><subject>Receptors, Steroid - metabolism</subject><subject>Reference Values</subject><subject>Space life sciences</subject><subject>VALEUR NUTRITIVE</subject><subject>VALOR NUTRITIVO</subject><subject>VITAMIN D</subject><subject>Vitamin D Deficiency - metabolism</subject><subject>VITAMINA D</subject><subject>VITAMINE D</subject><issn>0002-9513</issn><issn>0193-1849</issn><issn>2163-5773</issn><issn>1522-1555</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kE1P4zAQhi20CMrHH0BC5MRpHTxjO3aPC8uXVIlD4Ww5jtMapXWIW9j8-01phcSBkzWeZ94ZPYRcAMsBJF7Z19Yvq5jDWOscpchFfisY7pERQsGpVIr_IiPGGNKxBH5IjlJ6HUqQXByQA9ScA9MjMr0OsYmz4GyTWbcK72HVZ7HO4DdKWoV5X3XxXz_82kVYZn8xs8sqQ0F9G-hPzAnZr22T_OnuPSYvd7fPNw908nT_ePNnQh0KvqKWlXVVghfOKe4QEIfbfIEFQ6w4eC0YcObqsnSlkrUv5ACqGpWE0o11xY_J5Ta37eLb2qeVWYTkfNPYpY_rZJSGAoDJAVRb0HUxpc7Xpu3Cwna9AWY2Os1Op9noNINOI8xG5zB5vluxLhe--prb-Rv6dNufh9n8I3TetPM-fSrtv0K_5Z1t-dpGY2ddSOZlqjVXfCz4f5dSidQ</recordid><startdate>198804</startdate><enddate>198804</enddate><creator>DeLuca, H.F</creator><creator>Sicinski, R.R</creator><creator>Tanaka, Y</creator><creator>Stern, P.H</creator><creator>Smith, C.M</creator><scope>FBQ</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>198804</creationdate><title>Biological activity of 1,25-dihydroxyvitamin D2 and 24-epi-1,25-dihydroxyvitamin D2</title><author>DeLuca, H.F ; Sicinski, R.R ; Tanaka, Y ; Stern, P.H ; Smith, C.M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c243t-a0bfdb1e4cc73c2122534e626022d31e840130cfbbcb75fe65cc77f2751bc98d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1988</creationdate><topic>ABSORCION</topic><topic>ABSORPTION</topic><topic>Animals</topic><topic>BONE DISEASES</topic><topic>Bone Resorption - drug effects</topic><topic>CALCIO</topic><topic>Calcitriol - pharmacology</topic><topic>CALCIUM</topic><topic>Calcium - metabolism</topic><topic>Chickens</topic><topic>ENFERMEDADES OSEAS</topic><topic>Ergocalciferols - analogs &amp; derivatives</topic><topic>Ergocalciferols - metabolism</topic><topic>Ergocalciferols - pharmacology</topic><topic>Intestinal Absorption - drug effects</topic><topic>Intestines - metabolism</topic><topic>Kinetics</topic><topic>Male</topic><topic>NUTRITIVE VALUE</topic><topic>OSTEOPATHIE</topic><topic>Rats</topic><topic>Receptors, Calcitriol</topic><topic>Receptors, Steroid - metabolism</topic><topic>Reference Values</topic><topic>Space life sciences</topic><topic>VALEUR NUTRITIVE</topic><topic>VALOR NUTRITIVO</topic><topic>VITAMIN D</topic><topic>Vitamin D Deficiency - metabolism</topic><topic>VITAMINA D</topic><topic>VITAMINE D</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>DeLuca, H.F</creatorcontrib><creatorcontrib>Sicinski, R.R</creatorcontrib><creatorcontrib>Tanaka, Y</creatorcontrib><creatorcontrib>Stern, P.H</creatorcontrib><creatorcontrib>Smith, C.M</creatorcontrib><collection>AGRIS</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>American journal of physiology: endocrinology and metabolism</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>DeLuca, H.F</au><au>Sicinski, R.R</au><au>Tanaka, Y</au><au>Stern, P.H</au><au>Smith, C.M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biological activity of 1,25-dihydroxyvitamin D2 and 24-epi-1,25-dihydroxyvitamin D2</atitle><jtitle>American journal of physiology: endocrinology and metabolism</jtitle><addtitle>Am J Physiol</addtitle><date>1988-04</date><risdate>1988</risdate><volume>254</volume><issue>4</issue><spage>E402</spage><epage>E406</epage><pages>E402-E406</pages><issn>0002-9513</issn><issn>0193-1849</issn><eissn>2163-5773</eissn><eissn>1522-1555</eissn><abstract>H. F. DeLuca, R. R. Sicinski, Y. Tanaka, P. H. Stern and C. M. Smith Department of Biochemistry, University of Wisconsin-Madison 53706. The biological activity of 1,25-dihydroxyvitamin D2 [1,25(OH)2D2] and 24-epi-1,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2] has been determined in vitamin D-deficient rats. The biological effectiveness of 1,25(OH)2D2 is equal to that reported previously for 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] (15) in intestinal calcium transport, mineralization of bone, mobilization of bone calcium, and elevation of plasma inorganic phosphorus of rachitic rats. However, 24-epi-1,25(OH)2D2 is at best one-half as active as 1,25(OH)2D2 in stimulating intestinal calcium transport and in the mineralization of rachitic bone. The 24-epi-1,25(OH)2D2 is one-third as active as 1,25(OH)2D3 in binding to the chick intestinal receptor for 1,25(OH)2D3. Thus receptor discrimination may account for the twofold difference in intestinal calcium transport activity. 24-Epi-1,25(OH)2D2 appeared inactive in in vivo mobilization of bone calcium or bone phosphorus. On the other hand, in fetal rat bone in culture, the epi compound was only five times less active than 1,25(OH)2D2 in inducing resorption. Short-term experiments on bone mineral mobilization in vivo show that the 24-epi-1,25(OH)2D2 does induce bone calcium mobilization but that its activity in this respect is short lived. It is suggested that 24-epi-1,25(OH)2D2 and, as a result, it shows preferential activity on intestine whose response to a single dose of 1,25(OH)2D2 remains for several days, whereas the short-lived bone system does not remain stimulated during the 24-h period between doses.</abstract><cop>United States</cop><pmid>2833108</pmid><doi>10.1152/ajpendo.1988.254.4.E402</doi></addata></record>
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subjects ABSORCION
ABSORPTION
Animals
BONE DISEASES
Bone Resorption - drug effects
CALCIO
Calcitriol - pharmacology
CALCIUM
Calcium - metabolism
Chickens
ENFERMEDADES OSEAS
Ergocalciferols - analogs & derivatives
Ergocalciferols - metabolism
Ergocalciferols - pharmacology
Intestinal Absorption - drug effects
Intestines - metabolism
Kinetics
Male
NUTRITIVE VALUE
OSTEOPATHIE
Rats
Receptors, Calcitriol
Receptors, Steroid - metabolism
Reference Values
Space life sciences
VALEUR NUTRITIVE
VALOR NUTRITIVO
VITAMIN D
Vitamin D Deficiency - metabolism
VITAMINA D
VITAMINE D
title Biological activity of 1,25-dihydroxyvitamin D2 and 24-epi-1,25-dihydroxyvitamin D2
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