LXRα agonists ameliorates acute rejection after liver transplantation via ABCA1/MAPK and PI3K/AKT/mTOR signaling axis in macrophages

Mol Med. 2025 Mar 14;31(1):99. doi: 10.1186/s10020-025-01153-1.

Abstract

Introduction: Liver X receptor α (LXRα) plays an important role in inflammatory immune response induced by hepatic ischemia-reperfusion injury (IRI) and acute rejection (AR). Macrophage M1-polarization play an important role in the occurrence and development of AR. Although the activation of LXR has anti-inflammatory effects, the role of LXRα in AR after liver transplantation (LT) has not been elucidated.

Objective: We aimed to investigate LXRα anti-inflammatory and macrophage polarization regulation effects and mechanisms in acute rejection rat models.

Methods: LXRα anti-inflammatory and liver function protective effects was initially measured in primary Kupffer cells and LT rat models. Subsequently, a flow cytometry assay was used to detect the regulation effect of LXRα in macrophage polarization. HE staining, TUNEL and ELISA were used to evaluate the co-treatment effects of TO901317 and tacrolimus on hepatic apoptosis and liver acute rejection after LT.

Results: In this study, we found that LPS can inhibit the expression of LXRα and activate MAPK pathway and PI3K/AKT/mTOR. We also found that LXRα agonist (TO901317) could improve liver function and rat survival after LT by activating the level of ABCA1 and inhibiting MAPK. TO901317 could inhibit macrophage M1-polarization by activating PI3K/AKT/mTOR signal pathway to improve the liver lesion of AR rats after liver transplantation. Additionally, co-treatment with TO901317 and tacrolimus more effectively alleviated the damaging effects of AR following LT than either drug alone.

Conclusion: Our results suggest that the activation of LXRα can improve liver function and rat survival after LT by regulate ABCA1/MAPK and PI3K/AKT/mTOR signaling axis in macrophages.

Keywords: Acute rejection; Inflammation; LXRα; Liver transplantation; M1 polarization; Macrophage.

MeSH terms

  • ATP Binding Cassette Transporter 1 / metabolism
  • Animals
  • Apoptosis / drug effects
  • Benzenesulfonamides
  • Disease Models, Animal
  • Fluorocarbons
  • Graft Rejection* / drug therapy
  • Graft Rejection* / etiology
  • Graft Rejection* / metabolism
  • Graft Rejection* / pathology
  • Hydrocarbons, Fluorinated / pharmacology
  • Kupffer Cells / drug effects
  • Kupffer Cells / metabolism
  • Liver Transplantation* / adverse effects
  • Liver X Receptors* / agonists
  • Liver X Receptors* / metabolism
  • Macrophages* / drug effects
  • Macrophages* / metabolism
  • Male
  • Mitogen-Activated Protein Kinases / metabolism
  • Phosphatidylinositol 3-Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • Rats
  • Signal Transduction* / drug effects
  • Sulfonamides / pharmacology
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • Liver X Receptors
  • ATP Binding Cassette Transporter 1
  • Proto-Oncogene Proteins c-akt
  • Phosphatidylinositol 3-Kinases
  • TOR Serine-Threonine Kinases
  • T0901317
  • Hydrocarbons, Fluorinated
  • Sulfonamides
  • Abca1 protein, rat
  • Mitogen-Activated Protein Kinases
  • Nr1h3 protein, rat
  • Benzenesulfonamides
  • Fluorocarbons