1,24(R)‐Dihydroxyvitamin D3, a Novel Active Form of Vitamin D3 with High Activity for Inducing Epidermal Differentiation but Decreased Hypercalcemic Activity
1,24(R)‐Dihydroxyvitamin D3, a Novel Active Form of Vitamin D3 with High Activity for Inducing Epidermal Differentiation but Decreased Hypercalcemic Activity
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1,24(R)-二羟基维生素 D3，维生素 D3 的一种新型活性形式，具有诱导表皮分化的高活性，但可降低高钙血症活性
DOI：
10.1111/j.1346-8138.1990.tb01614.x
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发表时间：
1990
期刊：
影响因子：
--
通讯作者：
Toshio Kuroki
中科院分区：
文献类型：
--
作者：
T. Matsunaga;Masaru Yamamoto;H. Mimura;T. Ohta;M. Kiyoki;T. Ohba;T. Naruchi;J. Hosoi;Toshio Kuroki
1二羟基维生素D3(1，25(α)2D3，1，25(OH)2D3)是一种具有激素活性的维生素D3，可调节细胞内外钙水平，促进髓系细胞和表皮角质形成细胞的分化。我们发现1，24(R)-二羟基维生素D3(1，24(α)2D3，1，24(OH)2D3)是维生素D3的一种新的合成衍生物，也具有调节表皮角质形成细胞分化的活性。1，24(OH)2D3与1，25(OH)2D3对从新生小鼠表皮分离的受体具有相同的亲和力。小鼠表皮角质形成细胞与1，24(OH)2D3孵育后以时间和剂量依赖的方式诱导分化，表现为角化包膜的形成和转谷氨酰胺酶活性的增加。1，24(OH)2D3抑制表皮角质形成细胞DNA合成，并使细胞内钙离子水平升高。1，24(OH)2D3的这些作用与生理活性的1，25(OH)2D3相似，或者更确切地说，比生理活性1，25(OH)2D3的作用更大。然而，静脉注射1，24(OH)2D3引起的高血钙较1，25(OH)2D3少，提示其对银屑病有潜在的治疗价值。
1α,25‐Dihydroxyvitamin D3 (1,25(OH)2D3) is known to be a hormonally active form of vitamin D3 in the regulation of intracellular and extracellular calcium levels and of differentiation of myeloid cells and epidermal keratinocytes. We found that 1α,24(R)‐dihydroxyvitamin D3 (1,24(OH)2D3), a novel synthetic derivative of vitamin D3, is also active in regulating the differentiation of epidermal keratinocytes. 1,24(OH)2D3 had the same affinity as 1,25(OH)2D3 for a receptor isolated from the epidermis of newborn mice. The incubation of mouse epidermal keratinocytes with 1,24(OH)2D3 induced their differentiation in a time‐ and dose‐dependent manner, as determined by the formation of a cornified envelope and an increase in the activity of transglutaminase. 1,24(OH)2D3 inhibited DNA synthesis of epidermal keratinocytes and also increased their cytosolic calcium level. These effects of 1,24(OH)2D3 were similar to, or rather more than, those of physiologically active 1,25(OH)2D3. However, 1,24(OH)2D3 was found to cause less hypercalcemia than 1,25(OH)2D3 when administrated intravenously to rats, suggesting its possible therapeutic value in psoriasis.
DOI：
10.1016/s0021-9258(18)60729-x
发表时间：
1988-04
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
S. Pillai;D. Bikle;P. Elias
通讯作者：
S. Pillai;D. Bikle;P. Elias
大鼠皮肤中 1,25-二羟基维生素 D3 受体样蛋白的表征。
DOI：
10.1073/pnas.77.10.5822
发表时间：
1980
影响因子：
11.1
作者：
Simpson,RU;DeLuca,HF
通讯作者：
DeLuca,HF
小鼠皮肤和肠道1,25-(OH)2-D3受体浓度的检测和发育变化。
DOI：
10.1111/1523-1747.ep12272358
发表时间：
1985
期刊：
The Journal of investigative dermatology
影响因子：
--
作者：
Horiuchi,N;Clemens,TL;Schiller,AL;Holick,MF
通讯作者：
Holick,MF