Inhibition of the hepatotoxicity of paracetamol and its irreversible binding to rat liver microsomal protein

Abstract

Dithiocarb and (+)-cyanidanol-3 prevented paracetamol-induced liver injury in rats in vivo. Both, as well as two other antihepatotoxic agents, deanol and DMSO, inhibited covalent binding of [³H]-paracetamol to rat liver microsomal proteins in vitro. Dithiocarb and (+)-cyanidanol-3 were the most effective inhibitors. The concentrations of the antidotes yielding 50% inhibition (I₅₀) valued 1 · 8 × 10⁻⁵ M for dithiocarb and 2 · 1 × 10⁻⁵ M for (+)-cyanidanol-3.