In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds

ChemMedChem. 2018 Dec 6;13(23):2484-2487. doi: 10.1002/cmdc.201800601. Epub 2018 Nov 27.

Abstract

The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2 ] (NHC=N-heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet-activating factor (PAF)-induced platelet aggregation was probed. All complexes were found to possess anti-aggregatory properties in vitro with [IPr*⋅H][AuCl2 ] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti-inflammatory drugs.

Keywords: N-heterocyclic carbenes; anti-atherogenic activity; atheromatosis; aurates; platelet-activating factor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Humans
  • Methane / analogs & derivatives*
  • Methane / chemistry
  • Methane / pharmacology
  • Models, Molecular
  • Organogold Compounds / chemistry*
  • Organogold Compounds / pharmacology*
  • Platelet Activating Factor / antagonists & inhibitors
  • Platelet Activating Factor / metabolism
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemistry*
  • Platelet Aggregation Inhibitors / pharmacology*

Substances

  • Anti-Inflammatory Agents
  • Organogold Compounds
  • Platelet Activating Factor
  • Platelet Aggregation Inhibitors
  • carbene
  • Methane