Nesfatin-1 Reduces Cholic Acid-Induced Intrahepatic Cholestasis of Pregnancy by Regulating the General Control Nonderepressible 2/Eukaryotic Initiation Factor 2α Pathway

Chem Biol Drug Des. 2025 Jun;105(6):e70147. doi: 10.1111/cbdd.70147.

Abstract

Intrahepatic cholestasis of pregnancy (ICP) is a liver disorder that significantly impacts pregnancy outcomes, with oxidative stress (OS) playing a crucial role in its pathogenesis. The animal model was constructed using 8-10-week-old CD-1 mice, which were administered cholic acid (CA) orally from gestational day (GD) 12-GD17 to induce placental injury. Nesfatin-1 (NF-1) was administered intraperitoneally to assess its protective effects. Our study found that NF-1 effectively attenuated placental dysfunction by reducing glucocorticoid (GC) production and boosting 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2) expression, a key enzyme for GC inactivation. Furthermore, NF-1 reduced OS markers such as malondialdehyde (MDA) and reactive oxygen species (ROS) in both placental tissue and HTR8/SVneo cells. The protective effects of NF-1 were correlated with the suppression of the general control nonderepressible 2 (GCN2)/eukaryotic initiation factor 2α (eIF2α) signaling pathway, which became activated under OS conditions. Notably, halofuginone, a GCN2 agonist, abolished the beneficial effects of NF-1, further confirming the involvement of the GCN2/eIF2α pathway. These results suggest that NF-1 may serve as a potential therapeutic agent for managing ICP and related stress-induced pregnancy complications by modulating GC metabolism and mitigating OS.

Keywords: 11β‐HSD2; GCN2/eIF2α pathway; glucocorticoids; intrahepatic cholestasis of pregnancy; nesfatin‐1; oxidative stress.

MeSH terms

  • Animals
  • Calcium-Binding Proteins* / metabolism
  • Cell Line
  • Cholestasis, Intrahepatic* / chemically induced
  • Cholestasis, Intrahepatic* / drug therapy
  • Cholestasis, Intrahepatic* / metabolism
  • Cholestasis, Intrahepatic* / pathology
  • Cholic Acid*
  • Disease Models, Animal
  • Eukaryotic Initiation Factor-2* / metabolism
  • Female
  • Humans
  • Mice
  • Nucleobindins / metabolism
  • Oxidative Stress / drug effects
  • Placenta / drug effects
  • Placenta / metabolism
  • Placenta / pathology
  • Pregnancy
  • Pregnancy Complications* / chemically induced
  • Pregnancy Complications* / drug therapy
  • Pregnancy Complications* / metabolism
  • Pregnancy Complications* / pathology
  • Reactive Oxygen Species / metabolism
  • Signal Transduction / drug effects

Substances

  • Nucleobindins
  • Cholic Acid
  • Eukaryotic Initiation Factor-2
  • Reactive Oxygen Species
  • Calcium-Binding Proteins

Supplementary concepts

  • Intrahepatic Cholestasis of Pregnancy