PGE2-regulated wnt signaling and N-acetylcysteine are synergistically hepatoprotective in zebrafish acetaminophen injury

Proc Natl Acad Sci U S A. 2010 Oct 5;107(40):17315-20. doi: 10.1073/pnas.1008209107. Epub 2010 Sep 20.

Abstract

Acetaminophen (APAP) toxicity is the most common drug-induced cause of acute liver failure in the United States. The only available treatment, N-acetylcysteine (NAC), has a limited time window of efficacy, indicating a need for additional therapeutic options. Zebrafish have emerged as a powerful tool for drug discovery. Here, we developed a clinically relevant zebrafish model of APAP toxicity. APAP depleted glutathione stores, elevated aminotransferase levels, increased apoptosis, and caused dose-dependent hepatocyte necrosis. These outcomes were limited by NAC and conserved in zebrafish embryos. In a targeted embryonic chemical screen, prostaglandin E2 (PGE2) was identified as a potential therapeutic agent; in the adult, PGE2 similarly decreased APAP-associated toxicity. Significantly, when combined with NAC, PGE2 extended the time window for a successful intervention, synergistically reducing apoptosis, improving liver enzymes, and preventing death. Use of a wnt reporter zebrafish line and chemical genetic epistasis showed that the effects of PGE2 are mediated through the wnt signaling pathway. Zebrafish can be used as a clinically relevant toxicological model amenable to the identification of additional therapeutics and biomarkers of APAP injury; our data suggest combinatorial PGE2 and NAC treatment would be beneficial for patients with APAP-induced liver damage.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetaminophen / toxicity*
  • Acetylcysteine* / pharmacology
  • Acetylcysteine* / therapeutic use
  • Analgesics, Non-Narcotic / toxicity
  • Animals
  • Animals, Genetically Modified
  • Chemical and Drug Induced Liver Injury* / drug therapy
  • Chemical and Drug Induced Liver Injury* / metabolism
  • Chemical and Drug Induced Liver Injury* / pathology
  • Dinoprostone / metabolism*
  • Genes, Reporter
  • Glutathione / metabolism
  • Liver / drug effects
  • Liver / metabolism
  • Liver / pathology
  • Liver Failure, Acute* / drug therapy
  • Liver Failure, Acute* / metabolism
  • Liver Failure, Acute* / pathology
  • Proteome / analysis
  • Signal Transduction / physiology*
  • Zebrafish* / anatomy & histology
  • Zebrafish* / physiology

Substances

  • Analgesics, Non-Narcotic
  • Proteome
  • Acetaminophen
  • Glutathione
  • Dinoprostone
  • Acetylcysteine