Vitamin K2 induces phosphorylation of protein kinase A and expression of novel target genes in osteoblastic cells

J Mol Endocrinol. 2007 Oct;39(4):239-47. doi: 10.1677/JME-07-0048.

Abstract

Vitamin K is known as a critical nutrient required for bone homeostasis and blood coagulation, and it is clinically used as a therapeutic agent for osteoporosis in Japan. Besides its enzymatic action as a cofactor of vitamin K-dependent gamma-glutamyl carboxylase (GGCX), we have previously shown that vitamin K(2) is a transcriptional regulator of bone marker genes and extracellular matrix-related genes, by activating the steroid and xenobiotic receptor (SXR). To explore a novel action of vitamin K in osteoblastic cells, we identified genes up-regulated by a vitamin K(2) isoform menaquinone-4 (MK-4) using oligonucleotide microarray analysis. Among these up-regulated genes by MK-4, growth differentiation factor 15 (GDF15) and stanniocalcin 2 (STC2) were identified as novel MK-4 target genes independent of GGCX and SXR pathways in human and mouse osteoblastic cells. The induction of GDF15 and STC2 is likely specific to MK-4, as it was not exerted by another vitamin K(2) isoform MK-7, vitamin K(1), or the MK-4 side chain structure geranylgeraniol. Investigation of the involved signaling pathways revealed that MK-4 enhanced the phosphorylation of protein kinase A (PKA), and the MK-4-dependent induction of both GDF15 and STC2 genes was reduced by the treatment with a PKA inhibitor H89 or siRNA against PKA. These results suggest that vitamin K(2) modulates its target gene expression in osteoblastic cells through the PKA-dependent mechanism, which may be distinct from the previously known vitamin K signaling pathways.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bone Morphogenetic Proteins / genetics
  • Bone Morphogenetic Proteins / metabolism
  • Carbon-Carbon Ligases / genetics
  • Carbon-Carbon Ligases / metabolism
  • Cells, Cultured
  • Cyclic AMP-Dependent Protein Kinases / metabolism*
  • Gene Expression Profiling
  • Gene Expression Regulation / drug effects*
  • Glycoproteins / genetics
  • Glycoproteins / metabolism
  • Growth Differentiation Factor 15
  • Humans
  • Intercellular Signaling Peptides and Proteins / genetics
  • Intercellular Signaling Peptides and Proteins / metabolism
  • Mice
  • Oligonucleotide Array Sequence Analysis
  • Osteoblasts / drug effects*
  • Osteoblasts / metabolism*
  • Phosphorylation / drug effects
  • Pregnane X Receptor
  • Receptors, Steroid / genetics
  • Receptors, Steroid / metabolism
  • Vitamin K 2 / analogs & derivatives
  • Vitamin K 2 / pharmacology*

Substances

  • Bone Morphogenetic Proteins
  • GDF15 protein, human
  • Gdf15 protein, mouse
  • Glycoproteins
  • Growth Differentiation Factor 15
  • Intercellular Signaling Peptides and Proteins
  • Pregnane X Receptor
  • Receptors, Steroid
  • STC2 protein, human
  • Vitamin K 2
  • menatetrenone
  • Cyclic AMP-Dependent Protein Kinases
  • Carbon-Carbon Ligases
  • glutamyl carboxylase