Positive feedback between histone H4K16 lactylation and glycolysis promotes MAFLD progression

Hepatol Int. 2026 Jun;20(3):646-663. doi: 10.1007/s12072-025-10978-1. Epub 2025 Dec 2.

Abstract

Background/aims: Metabolic-associated fatty liver disease (MAFLD) is a progressive metabolic disorder characterized by hepatic steatosis, inflammation, and fibrosis. Emerging evidence suggests that lactate-driven histone lactylation may contribute to its pathogenesis, but mechanisms remain unclear.

Methods: C57BL/6 mice were fed HFD or CDHFD, and hepatocytes were treated with OAPA. Histone lactylation was assessed by IF and WB. CUT&Tag and RNA-seq identified downstream targets, while H4K16R mutation, PDK4 knockdown, and dichloroacetic acid (DCA) inhibition were applied in vitro and in vivo.

Results: Histone lactylation, especially H4K16la, was elevated in murine and human MASH and correlated with steatosis, inflammation, and fibrosis. H4K16la directly activated PDK4 transcription, forming a lactate-H4K16la-PDK4 feedback loop that exacerbated MAFLD. Genetic or pharmacologic inhibition reduced lactate, lipid accumulation, and liver injury.

Conclusions: We identify a lactate-H4K16la-PDK4 axis that drives metabolic reprogramming and MAFLD progression. Targeting PDK4 may represent a therapeutic strategy for MAFLD/MASH.

Keywords: Glycolysis; Histone lactylation; Lactate; MAFLD; PDK4.

MeSH terms

  • Animals
  • Disease Progression
  • Fatty Liver* / metabolism
  • Fatty Liver* / pathology
  • Feedback, Physiological
  • Glycolysis*
  • Hepatocytes / metabolism
  • Histones* / metabolism
  • Humans
  • Lactic Acid* / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Pyruvate Dehydrogenase Acetyl-Transferring Kinase* / genetics
  • Pyruvate Dehydrogenase Acetyl-Transferring Kinase* / metabolism

Substances

  • Histones
  • Lactic Acid
  • Pyruvate Dehydrogenase Acetyl-Transferring Kinase
  • Pdk4 protein, mouse