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24-表-1α-羟基维生素D2和24-表-1α,25-二羟基维生素D2的骨吸收活性

Bone-resorbing activities of 24-epi-1 alpha-hydroxyvitamin D2 and 24-epi-1 alpha,25-dihydroxyvitamin D2.

作者信息

Yokoyama K, Miyahara T, Matsumoto M, Hashimoto K, Komiyama H, Miyanishi A, Kotera N, Maruyama F, Kozuka H

机构信息

Department of Toxicology, Hikone Research Laboratories, Maruho Co., Ltd., Shiga, Japan.

出版信息

Calcif Tissue Int. 1995 Jan;56(1):49-53. doi: 10.1007/BF00298744.

Abstract

Bone-resorbing activities of 24-epi-1 alpha-hydroxyvitamin D2 [24-epi-1 alpha(OH)D2], 24-epi-1 alpha,25-dihydroxyvitamin D2 [24-epi-1,25(OH)2D2], and 1 alpha,24S,25-trihydroxyvitamin D2 [1,24S,25(OH)3D2], which might be a metabolite of 24-epi-1,25(OH)2D2, were investigated. In an in vitro bone resorption test, the activity of 24-epi-1 alpha(OH)D2 was similar to that of 1 alpha-hydroxyvitamin D3 [1 alpha(OH)D3] at 10(-9) M-10(-6) M. The activity of 24-epi-1,25(OH)2D2 was weaker than that of 1 alpha,25-dihydroxyvitamin D3 [1,25(OH)2D3] at 10(-11) M-10(-8) M. On the other hand, the activity of 1,24S,25(OH)3D2 was similar to that of 24-epi-1,25(OH)2D2 at 10(-11) M-10(-9) M. In the formation assay of osteoclast-like cells, the activity of 24-epi-1 alpha(OH)D2 was weaker than that of 1 alpha(OH)D3 at 10(-7) M. The activity of 24-epi-1,25(OH)2D2 was almost similar to that of 1,25(OH)2D3 at 10(-11) M-10(-7) M. The activity of 1,24S,25(OH)3D2 was significantly weaker than that of 24-epi-1,25(OH)2D2 at 10(-11) M-10(-9) M. In the two experiments, the potencies of 24-epi-1,25(OH)2D2 were about 100 times higher than those of 24-epi-1 alpha(OH)D2. In an in vivo/in vitro bone resorption test, the activity of 24-epi-1 alpha(OH)D2 was almost similar to those of 1 alpha(OH)D3 and 1,25(OH)2D3 and higher than those of 24-epi-1,25(OH)2D2 and 1,24S,25(OH)3D2. 24-epi-1 alpha-(OH)D2 and 1 alpha(OH)D3 were longer lasting than 24-epi-1,25(OH)2D2 and 1,25(OH)2D3 in this experiment.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

对24-表-1α-羟基维生素D2 [24-表-1α(OH)D2]、24-表-1α,25-二羟基维生素D2 [24-表-1,25(OH)2D2]以及1α,24S,25-三羟基维生素D2 [1,24S,25(OH)3D2](可能是24-表-1,25(OH)2D2的一种代谢产物)的骨吸收活性进行了研究。在体外骨吸收试验中,在10(-9) M - 10(-6) M浓度下,24-表-1α(OH)D2的活性与1α-羟基维生素D3 [1α(OH)D3]相似。在10(-11) M - 10(-8) M浓度下,24-表-1,25(OH)2D2的活性弱于1α,25-二羟基维生素D3 [1,25(OH)2D3]。另一方面,在10(-11) M - 10(-9) M浓度下,1,24S,25(OH)3D2的活性与24-表-1,25(OH)2D2相似。在破骨细胞样细胞形成试验中,在10(-7) M浓度下,24-表-1α(OH)D2的活性弱于1α(OH)D3。在10(-11) M - 10(-7) M浓度下,24-表-1,25(OH)2D2的活性与1,25(OH)2D3几乎相似。在10(-11) M - 10(-9) M浓度下,1,24S,25(OH)3D2的活性明显弱于24-表-1,25(OH)2D2。在这两个实验中,24-表-1,25(OH)2D2的效力比24-表-1α(OH)D2高约100倍。在体内/体外骨吸收试验中,24-表-1α(OH)D2的活性与1α(OH)D3和1,25(OH)2D3几乎相似,且高于24-表-1,25(OH)2D2和1,24S,25(OH)3D2。在本实验中,24-表-1α-(OH)D2和1α(OH)D3的作用持续时间比24-表-1,25(OH)2D2和1,25(OH)2D3更长。(摘要截短于250字)

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