Sesamin ameliorates lipotoxicity and lipid accumulation through the activation of the estrogen receptor alpha signaling pathway

Biochem Pharmacol. 2023 Oct:216:115768. doi: 10.1016/j.bcp.2023.115768. Epub 2023 Aug 29.

Abstract

Nonalcoholic fatty liver disease (NAFLD) has been linked to fat accumulation in the liver and lipid metabolism imbalance. Sesamin, a lignan commonly found in sesame seed oil, possesses antioxidant, anti-inflammatory, and anticancer properties. However, the precise mechanisms by which sesamin prevents hepatic steatosis are not well understood. This study aimed to explore the molecular mechanisms by which sesamin may improve lipid metabolism dysregulation. A in vitro hepatic steatosis model was established by exposing HepG2 cells to palmitate sodium. The results showed that sesamin effectively mitigated lipotoxicity and reduced reactive oxygen species production. Additionally, sesamin suppressed lipid accumulation by regulating key factors involved in lipogenesis and lipolysis, such as fatty acid synthase (FASN), sterol regulatory element-binding protein 1c (SREBP-1c), forkhead box protein O-1, and adipose triglyceride lipase. Molecular docking results indicated that sesamin could bind to estrogen receptor α (ERα) and reduce FASN and SREBP-1c expression via the Ca2+/calmodulin-dependent protein kinase kinase β (CaMKKβ)/AMP-activated protein kinase (AMPK) signaling pathway. Sesamin attenuated palmitate-induced lipotoxicity and regulated hepatic lipid metabolism in HepG2 cells by activating the ERα/CaMKKβ/AMPK signaling pathway. These findings suggest that sesamin can improve lipid metabolism disorders and is a promising candidate for treating hepatic steatosis.

Keywords: AMPK; ATGL; ERα; Lipid accumulation; SREBP-1c; Sesamin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase
  • Estrogen Receptor alpha / metabolism
  • Hep G2 Cells
  • Humans
  • Lignans* / pharmacology
  • Lipid Metabolism
  • Liver / metabolism
  • Molecular Docking Simulation
  • Non-alcoholic Fatty Liver Disease* / metabolism
  • Palmitates / metabolism
  • Signal Transduction
  • Sterol Regulatory Element Binding Protein 1 / genetics
  • Sterol Regulatory Element Binding Protein 1 / metabolism

Substances

  • sesamin
  • Estrogen Receptor alpha
  • Sterol Regulatory Element Binding Protein 1
  • AMP-Activated Protein Kinases
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase
  • Lignans
  • Palmitates