Iron chelators that form redox-inactive complexes are important inhibitors of the Fenton reaction mediated by hydrogen peroxide, an important cellular pathway for the generation of hydroxyl radical and oxidative stress. However, iron chelators promote cytotoxicity after prolonged exposure, caused by cellular iron depletion. New pro-chelators (BSIH, SIHB) have been designed which are inactive as iron chelators, but are activated in the presence of hydrogen peroxide. Therefore, the chelators accumulate only in cellular sites with high concentration of hydrogen peroxide, and not throughout the cell. The pro-chelators were synthesized by condensation, and characterized by 1H-NMR, 13C-NMR, UV and IR spectrophotometry. Activation by hydrogen peroxide was confirmed by UV-spectrophotometry. The pro-chelators were not toxic to HepG2 cells even at high micromolar concentrations, suggesting their usefulness as iron pro-chelators in hepatocytes.

Effect of new iron chelators on hydrogen peroxide-mediated cell damage

243rd National Meeting (2012)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.