Anti-inflammatory actions of a taurine analogue, ethane β-sultam, in phagocytic cells, in vivo and in vitro

Biochem Pharmacol. 2011 Mar 15;81(6):743-51. doi: 10.1016/j.bcp.2010.12.030. Epub 2011 Jan 11.

Abstract

The ability of a taurine prodrug, ethane β-sultam, to reduce cellular inflammation has been investigated, in vitro, in primary cultures of alveolar macrophages and an immortilised N9 microglial cell line and in vivo in an animal model of inflammation and control rats. Ethane β-sultam showed enhanced ability to reduce the inflammatory response in alveolar macrophages, as assayed by the lipopolysaccharide-stimulated-nitric oxide release, (LPS stimulated-NO), in comparison to taurine both in vitro (10 nM, 50 nM) and in vivo (0.15 mmol/kg/day by gavage). In addition, ethane β-sultam, (50, 100 and 1000 nM) significantly reduced LPS-stimulated glutamate release from N9 microglial cells to a greater extent than taurine. The anti-inflammatory response of taurine was shown to be mediated via stabilisation of IkBα. The use of a taurine prodrug as therapeutic agents, for the treatment of neurological conditions, such as Parkinson's and Alzheimer's disease and alcoholic brain damage, where activated phagocytic cells contribute to the pathogenesis, may be of great potential.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Line, Transformed
  • Cells, Cultured
  • Ethane / analogs & derivatives
  • Ethane / pharmacology*
  • Inflammation Mediators / chemistry
  • Inflammation Mediators / pharmacology
  • Macrophages, Alveolar / drug effects
  • Macrophages, Alveolar / metabolism
  • Male
  • Mice
  • Phagocytes / drug effects*
  • Phagocytes / metabolism
  • Prodrugs / chemistry
  • Prodrugs / pharmacology
  • Rats
  • Rats, Wistar
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*
  • Taurine / analogs & derivatives*
  • Taurine / pharmacology*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Inflammation Mediators
  • Prodrugs
  • Sulfonamides
  • beta-sultam
  • Taurine
  • Ethane