Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate; 25(OH)D3) is a potent ligand for the vitamin D receptor (VDR) with gene regulatory and anti-proliferative properties, and functions as a vitamin D supplement and a VDR antagonist. As a precursor hormone in the vitamin D endocrine system (VDES), calcifediol undergoes hydroxylation in the liver to form the active hormone, calcitriol. This form of vitamin D can rapidly increase serum vitamin D levels [1-3].
Calcifediol monohydrate (100nM; 24h) decreased amyloid-β (Aβ)-production and increased Aβ-degradation in neuroblastoma cells. Effects were mediated by affecting the Aβ-producing enzymes BACE1 and γ-secretase [4]. Calcifediol monohydrate(10−5M) can induce a rapid increase in Ca2+ levels in hADMSCs cells in vitro [5].
Calcifediol monohydrate (5µg/kg, 100µL; 7 times; i.p)significantly protected mice against DNCB-induced AD. Calcifediol monohydrate may reduce inflammatory cell infiltration and chemokines by inhibiting the phosphorylation of STAT3 and may restore skin barrier function through the downregulation of AQP3 protein expression and inhibition of cell proliferation in In AD mouse model [6]. After viral attack, mice supplemented with Calcifediol monohydrate(125mg/kg; p.o; 7 weeks) stimulated the production of both anti-inflammatory and pro-inflammatory cytokines [7].
References:
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[3]. Lou YR, Molnár F, Peräkylä M, Qiao S, Kalueff AV, St-Arnaud R, Carlberg C, Tuohimaa P. 25-Hydroxyvitamin D(3) is an agonistic vitamin D receptor ligand. J Steroid Biochem Mol Biol. 2010 Feb 15;118(3):162-70. doi: 10.1016/j.jsbmb.2009.11.011. Epub 2009 Nov 26. PMID: 19944755.
[4]. Grimm MOW, Thiel A, Lauer AA, Winkler J, Lehmann J, Regner L, Nelke C, Janitschke D, Benoist C, Streidenberger O, Stötzel H, Endres K, Herr C, Beisswenger C, Grimm HS, Bals R, Lammert F, Hartmann T. Vitamin D and Its Analogues Decrease Amyloid-β (Aβ) Formation and Increase Aβ-Degradation. Int J Mol Sci. 2017 Dec 19;18(12):2764. doi: 10.3390/ijms18122764. PMID: 29257109; PMCID: PMC5751363.
[5]. Donati S, Palmini G, Romagnoli C, Aurilia C, Miglietta F, Falsetti I, Marini F, Zonefrati R, Galli G, Marcucci G, Iantomasi T, Brandi ML. In Vitro Non-Genomic Effects of Calcifediol on Human Preosteoblastic Cells. Nutrients. 2021 Nov 25;13(12):4227. doi: 10.3390/nu13124227. PMID: 34959778; PMCID: PMC8707877.
[6]. Lu R, Peng Z, Lian P, Wazir J, Gu C, Ma C, Wei L, Li L, Pu W, Liu J, Wang H, Su Z. Vitamin D attenuates DNCB-induced atopic dermatitis-like skin lesions by inhibiting immune response and restoring skin barrier function. Int Immunopharmacol. 2023 Sep;122:110558. doi: 10.1016/j.intimp.2023.110558. Epub 2023 Jun 30. PMID: 37393836.
[7]. Hayashi H, Okamatsu M, et,al. Oral Supplementation of the Vitamin D Metabolite 25(OH)D3 Against Influenza Virus Infection in Mice. Nutrients. 2020 Jul 5;12(7):2000. doi: 10.3390/nu12072000. PMID: 32635656; PMCID: PMC7400405.
Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate; 骨化二醇)是维生素D受体（VDR）的配体，具有基因调控和抗增殖特性，可作为维生素D补充剂和VDR拮抗剂。作为维生素D内分泌系统(VDES)的前体激素，Calcifediol在肝脏中发生羟基化作用，形成活性激素骨化三醇。这种形式的维生素D可以迅速提高血清维生素D水平[1-3]。
Calcifediol monohydrate (100nM; 24h)在神经母细胞瘤细胞中减少了淀粉样β(Aβ)产生并增加了Aβ的降解。其作用是通过影响Aβ生成酶BACE1和γ-分泌酶介导的[4]。Calcifediol monohydrate(10−5M)可以在体外诱导人脂肪来源的间充质干细胞（hADMSCs）中钙离子(Ca²⁺)水平的快速升高[5]。
Calcifediol monohydrate (5µg/kg, 100µL; 7 times; i.p)显著保护特应性皮炎小鼠免受DNCB诱导的特应性皮炎(AD)影响。Calcifediol monohydrate可能通过抑制STAT3的磷酸化减少炎症细胞的浸润和趋化因子的生成，并通过下调AQP3蛋白表达和抑制细胞增殖来恢复皮肤屏障功能[6]。在病毒攻击后，补充Calcifediol monohydrate(125mg/kg; p.o; 7 weeks)的小鼠能够刺激抗炎和促炎细胞因子的产生[7]。