羟基维生素D3衍生物对体外培养的大鼠胎儿骨骼45Ca释放的影响。

Effect of hydroxy-vitamin D3 derivatives on 45Ca release from rat fetal bones in vitro.

作者信息

Mahgoub A, Sheppard H

机构信息

Department of Cell Biology, Roche Research Center, Hoffmann-La Roche, Inc., Nutley, New Jersey 07110.

出版信息

Endocrinology. 1977 Mar;100(3):629-34. doi: 10.1210/endo-100-3-629.

DOI:10.1210/endo-100-3-629

PMID:401017

Abstract

Several hydroxy vitamin D3 (OH-D3) derivatives were tested for biological activity by measuring 45Ca release from prelabeled rat fetal bones, in vitro. In a 72 h continuous culture, 1 alpha,25-(OH)2-D3 produced a significant effect at 10 pg/ml. A similar effect was produced by 50 ng/ml of either 25-OH-D3 or 5,6-trans-25-OH-D3, and by 500 pg of 3 deoxy-1 alpha,25-(OH)2-D3. 24R,25-(OH)2-D3 was more active than 24S,25-(OH)2-D3, and the R isomer had activity that more closely resembled the biosynthetic compound. 3-deoxy-1 alpha-OH-D3 was inactive at a concentration of up to 1 microgram/ml. Using a 24 h preincubation period with no added vitamin D3 derivative, a steep dose-response curve could be obtained with 1 alpha,25-(OH)2-D3 over a range of 2-10 pg/ml during a subsequent 96 h incubation period, and 1 alpha,25-(OH)2-D3 was found to have about 5000 times the activity of 25-OH-D3.

摘要

通过在体外测量预先标记的大鼠胎儿骨骼中45Ca的释放，对几种羟基维生素D3（OH-D3）衍生物的生物活性进行了测试。在72小时的连续培养中，1α,25-(OH)2-D3在10 pg/ml时产生了显著效果。50 ng/ml的25-OH-D3或5,6-反式-25-OH-D3以及500 pg的3-脱氧-1α,25-(OH)2-D3也产生了类似的效果。24R,25-(OH)2-D3比24S,25-(OH)2-D3更具活性，且R异构体的活性更类似于生物合成化合物。3-脱氧-1α-OH-D3在浓度高达1微克/毫升时无活性。在不添加维生素D3衍生物的情况下进行24小时预孵育，随后在96小时孵育期内，1α,25-(OH)2-D3在2-10 pg/ml范围内可获得陡峭的剂量反应曲线，并且发现1α,25-(OH)2-D3的活性约为25-OH-D3的5000倍。