1α,25 - 二羟基维生素D衍生物——24 - 表 - 1α,25 - 二羟基维生素D - 2和1α,25 - 二羟基维生素D - 7的生物活性
Biological activity of 1 alpha, 25-dihydroxyvitamin D derivatives--24-epi-1 alpha, 25-dihydroxyvitamin D-2 and 1 alpha,25-dihydroxyvitamin D-7.
作者信息
Sato F, Okamoto Y, Ouchi Y, Kaneki M, Nakamura T, Ikekawa N, Orimo H
机构信息
Department of Geriatrics, Faculty of Medicine, University of Tokyo, Japan.
出版信息
Biochim Biophys Acta. 1991 Jan 31;1091(2):188-92. doi: 10.1016/0167-4889(91)90060-b.
Biological activity of 24-epi-1 alpha,25-dihydroxyvitamin D-2 (24-epi-1,25(OH)2D2) and 1 alpha,25-dihydroxyvitamin D-7 (1,25(OH)2D7), the 22,23-dihydro derivative of the former compound, was investigated. Both of the vitamin D derivatives stimulated intestinal calcium transport and calcium mobilization from bones in rats; however, the effect was about 50% of that of 1 alpha,25-dihydroxyvitamin D-3 (1,25(OH)2D3). On the other hand, 24-epi-1,25(OH)2D2 and 1,25(OH)2D7 inducement of HL-60 human leukemia cell differentiation was comparable to that of 1,25(OH)2D3. Accordingly, the differentiation-inducing activity of 24-epi-1,25(OH)2D2 and 1,25(OH)2D7 was much greater than their ability to stimulate calcium metabolism. In contrast to 1,25(OH)2D3, 24-epi-1,25(OH)2D2 and 1,25(OH)2D7 exerted little hypercalcemic activity in mice. These results suggest that both vitamin D derivatives will be useful as anti-tumor agents.
对24-表-1α,25-二羟基维生素D-2（24-表-1,25(OH)2D2）及其22,23-二氢衍生物1α,25-二羟基维生素D-7（1,25(OH)2D7）的生物活性进行了研究。这两种维生素D衍生物均能刺激大鼠肠道钙转运和骨钙动员；然而，其作用约为1α,25-二羟基维生素D-3（1,25(OH)2D3）的50%。另一方面，24-表-1,25(OH)2D2和1,25(OH)2D7诱导HL-60人白血病细胞分化的能力与1,25(OH)2D3相当。因此，24-表-1,25(OH)2D2和1,25(OH)2D7的诱导分化活性远大于其刺激钙代谢的能力。与1,25(OH)2D3不同，24-表-1,25(OH)2D2和1,25(OH)2D7在小鼠中几乎没有高钙血症活性。这些结果表明，这两种维生素D衍生物有望作为抗肿瘤药物。
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