用1α,25-二羟基维生素D3和1α,25-二羟基维生素D3的受体活性20-表位类似物刺激小鼠表皮增殖。
Stimulation of epidermal proliferation in mice with 1 alpha, 25-dihydroxyvitamin D3 and receptor-active 20-EPI analogues of 1 alpha, 25-dihydroxyvitamin D3.
作者信息
Gniadecki R, Serup J
机构信息
Leo Pharmaceutical Products, Ballerup, Denmark.
出版信息
Biochem Pharmacol. 1995 Mar 1;49(5):621-4. doi: 10.1016/0006-2952(94)00482-2.
The effects of 1 alpha, 25-dihydroxyvitamin D3 (1 alpha, 25-(OH)2D3) and receptor-active 20-epi vitamin D analogues (MC 1288, 20-epi-1 alpha, 25-(OH)2D3; MC 1301, 20-epi-24a-homo-26,27-dimethyl-1 alpha, 25-(OH)2D3, and KH 1060: 20-epi-22-oxa-24a-homo-26,27-dimethyl-1 alpha, 25-(OH)2D3) on epidermal proliferation in mice were studied in vivo. Single topical applications of all compounds induced epidermal proliferation in a dose-dependent manner. The relative potencies in vivo (KH 1060 > MC1301 > MC1288 > 1 alpha, 25-(OH)2D3) correlated well with the known activities of these compounds to inhibit U 937 cell proliferation in vitro. Vitamin D3 and 1 beta, 25-(OH)2D3, two compounds that do not bind the vitamin D receptor, did not affect epidermal proliferation. Our study shows that vitamin D3 compounds that bind to the vitamin D receptor stimulate epidermal proliferation in mice.
在体内研究了1α,25 - 二羟基维生素D3（1α,25-(OH)2D3）和具有受体活性的20 - 表维生素D类似物（MC 1288，20 - 表 - 1α,25-(OH)2D3；MC 1301，20 - 表 - 24a - 高 - 26,27 - 二甲基 - 1α,25-(OH)2D3，以及KH 1060：20 - 表 - 22 - 氧杂 - 24a - 高 - 26,27 - 二甲基 - 1α,25-(OH)2D3）对小鼠表皮增殖的影响。所有化合物单次局部应用均以剂量依赖性方式诱导表皮增殖。体内相对效力（KH 1060 > MC1301 > MC1288 > 1α,25-(OH)2D3）与这些化合物在体外抑制U 937细胞增殖的已知活性密切相关。维生素D3和1β,25-(OH)2D3这两种不与维生素D受体结合的化合物，不影响表皮增殖。我们的研究表明，与维生素D受体结合的维生素D3化合物可刺激小鼠表皮增殖。
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