A Novel H2S-releasing Amino-Bisphosphonate which combines bone anti-catabolic and anabolic functions

Sci Rep. 2017 Sep 20;7(1):11940. doi: 10.1038/s41598-017-11608-z.

Abstract

Bisphosphonates (BPs) are the first-line treatment of bone loss resulting from various pathological conditions. Due to their high affinity to bone they have been used to develop conjugates with pro-anabolic or anti-catabolic drugs. We recently demontrated that hydrogen sulfide (H2S), promotes osteogenesis and inhibits osteoclast differentiation. Here we developed an innovative molecule, named DM-22, obtained from the combination of alendronate (AL) and the H2S-releasing moiety aryl-isothiocyanate. DM-22 and AL were assayed in vitro in the concentration range 1-33 μM for effects on viability and function of human osteoclasts (h-OCs) and mesenchymal stromal cells (h-MSCs) undergoing osteogenic differentiation. Amperometric measures revealed that DM-22 releases H2S at a slow rate with a thiol-dependent mechanism. DM-22 significantly inhibited h-OCs differentiation and function, maintaining a residual h-OCs viability even at the high dose of 33 μM. Contrary to AL, in h-MSCs DM-22 did not induce cytotoxicity as revealed by LDH assay, significantly stimulated mineralization as measured by Alizarin Red staining and increased mRNA expression of Collagen I as compared to control cultures. In conclusion, DM-22 is a new BP which inhibits h-OCs function and stimulate osteogenic differentiation of h-MSCs, without cytotoxicity. DM-22 is an ideal candidate for a novel family of osteoanabolic drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alendronate / metabolism
  • Bone Density Conservation Agents / chemical synthesis
  • Bone Density Conservation Agents / metabolism*
  • Cell Differentiation / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Diphosphonates / chemical synthesis
  • Diphosphonates / metabolism*
  • Humans
  • Hydrogen Sulfide / metabolism*
  • Isothiocyanates / metabolism
  • Mesenchymal Stem Cells / drug effects
  • Osteoclasts / drug effects
  • Osteogenesis / drug effects*

Substances

  • Bone Density Conservation Agents
  • Diphosphonates
  • Isothiocyanates
  • isothiocyanic acid
  • Alendronate
  • Hydrogen Sulfide