LDT409 (pan-PPAR partial agonist) mitigates metabolic dysfunction-associated steatotic liver disease in high-fructose-fed mice

Mol Cell Endocrinol. 2024 Dec 1:594:112380. doi: 10.1016/j.mce.2024.112380. Epub 2024 Sep 26.

Abstract

Aim: This study sought to evaluate the effects of LDT409, a pan-PPAR partial agonist obtained from the main industrial waste from cashew nut processing, on hepatic remodeling, highlighting energy metabolism and endoplasmic reticulum (ER) stress in high-fructose-fed mice.

Methods: Male C57BL/6 mice received a control diet (C) or a high-fructose diet (HFRU) for ten weeks. Then, a five-week treatment started: C, C-LDT409, HFRU, and HFRU-LDT409. The LDT409 (40 mg/kg of body weight) was mixed with the diets.

Results: The HFRU diet caused insulin resistance and endoplasmic reticulum (ER) stress. High Pparg and decreased Ppara expression increased steatosis and pro-fibrogenic gene expression in livers of HFRU-fed mice. Suppressed lipogenic factors, orchestrated by PPAR-gamma, and mitigated ER stress concomitant with the increase in beta-oxidation driven by PPAR-alpha mediated the LDT409 beneficial effects.

Conclusions: LDT409 may represent a potential low-cost approach to treat metabolic dysfunction-associated steatotic liver disease, which does not currently have a specific treatment.

Keywords: ER stress; Fructose; LDT409; MASLD; PPAR-Alpha; PPAR-Gamma.

MeSH terms

  • Animals
  • Endoplasmic Reticulum Stress* / drug effects
  • Fatty Liver / drug therapy
  • Fatty Liver / metabolism
  • Fatty Liver / pathology
  • Fructose* / adverse effects
  • Insulin Resistance
  • Liver / drug effects
  • Liver / metabolism
  • Liver / pathology
  • Male
  • Metabolic Diseases / drug therapy
  • Metabolic Diseases / etiology
  • Metabolic Diseases / metabolism
  • Metabolic Diseases / pathology
  • Mice
  • Mice, Inbred C57BL*
  • Non-alcoholic Fatty Liver Disease / drug therapy
  • Non-alcoholic Fatty Liver Disease / metabolism
  • Non-alcoholic Fatty Liver Disease / pathology
  • PPAR alpha / agonists
  • PPAR alpha / genetics
  • PPAR alpha / metabolism
  • PPAR gamma / agonists
  • PPAR gamma / metabolism
  • Peroxisome Proliferator-Activated Receptors / agonists
  • Peroxisome Proliferator-Activated Receptors / metabolism

Substances

  • Fructose
  • Peroxisome Proliferator-Activated Receptors
  • PPAR alpha
  • PPAR gamma