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

TE North, IR Babu, LM Vedder… - Proceedings of the …, 2010 - National Acad Sciences
TE North, IR Babu, LM Vedder, AM Lord, JS Wishnok, SR Tannenbaum, LI Zon, W Goessling
Proceedings of the National Academy of Sciences, 2010National Acad Sciences
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 …
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.
National Acad Sciences