In Vitro Non-Genomic Effects of Calcifediol on Human Preosteoblastic Cells

Nutrients. 2021 Nov 25;13(12):4227. doi: 10.3390/nu13124227.

Abstract

Several recent studies have demonstrated that the direct precursor of vitamin D3, the calcifediol [25(OH)D3], through the binding to the nuclear vitamin D receptor (VDR), is able to regulate the expression of many genes involved in several cellular processes. Considering that itself may function as a VDR ligand, although with a lower affinity, respect than the active form of vitamin D, we have assumed that 25(OH)D3 by binding the VDR could have a vitamin's D3 activity such as activating non-genomic pathways, and in particular we selected mesenchymal stem cells derived from human adipose tissue (hADMSCs) for the in vitro assessment of the intracellular Ca2+ mobilization in response to 25(OH)D3. Our result reveals the ability of 25(OH)D3 to activate rapid, non-genomic pathways, such as an increase of intracellular Ca2+ levels, similar to what observed with the biologically active form of vitamin D3. hADMSCs loaded with Fluo-4 AM exhibited a rapid and sustained increase in intracellular Ca2+ concentration as a result of exposure to 10-5 M of 25(OH)D3. In this work, we show for the first time the in vitro ability of 25(OH)D3 to induce a rapid increase of intracellular Ca2+ levels in hADMSCs. These findings represent an important step to better understand the non-genomic effects of vitamin D3 and its role in endocrine system.

Keywords: calcifediol; calcitriol; intracellular Ca2+; non-genomic effects; vitamin D3.

MeSH terms

  • Calcifediol / pharmacokinetics*
  • Calcium / metabolism*
  • Calcium Signaling / drug effects*
  • Humans
  • In Vitro Techniques
  • Ligands
  • Mesenchymal Stem Cells
  • Receptors, Calcitriol / metabolism
  • Signal Transduction / drug effects*
  • Vitamins / pharmacokinetics*

Substances

  • Ligands
  • Receptors, Calcitriol
  • Vitamins
  • Calcifediol
  • Calcium