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Grapefruit Flavonoid Naringenin Regulates the Expression of LXRα in THP-1 Macrophages by Modulating AMP-Activated

Javier Saenz1, Consuelo Santa-María2, María Edith Reyes-Quiroz1

  • 1Departamento de Bioquímica Médica y Biología Molecular , Universidad de Sevilla , 41004 Sevilla , Spain.

Molecular Pharmaceutics
|November 16, 2017
PubMed

Insights

Grapefruit flavonoid naringenin boosts liver X receptor alpha (LXRα) and cholesterol efflux genes in macrophages via AMP-activated protein kinase (AMPK). This suggests a potential mechanism for naringenin in preventing atherosclerosis.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Pharmacology

Background:

  • Macrophages play a crucial role in cholesterol homeostasis and atherosclerosis.
  • Liver X receptor alpha (LXRα) is a key regulator of cholesterol metabolism.
  • Naringenin, a grapefruit flavonoid, possesses potential anti-atherosclerotic properties.

Purpose of the Study:

  • To investigate naringenin's effect on LXRα and its target genes in THP-1 macrophages.
  • To elucidate the role of AMP-activated protein kinase (AMPK) in naringenin-mediated LXRα modulation.
  • To assess naringenin's impact on cholesterol transport and cell migration.

Main Methods:

  • THP-1 macrophages were treated with naringenin.
  • LXRα and target gene expression (ABCA1, ABCG1, SREBP1c) were analyzed at mRNA and protein levels.
  • AMPK inhibition was achieved using compound C and siRNA.
  • Reverse cholesterol transport and cell migration assays were performed.

Main Results:

  • Naringenin upregulated LXRα mRNA and protein expression in THP-1 macrophages.
  • Naringenin increased the expression of LXRα target genes ABCA1, ABCG1, and SREBP1c.
  • AMPK inhibition reversed naringenin-induced LXRα expression.
  • Naringenin promoted reverse cholesterol transport and inhibited cell migration.

Conclusions:

  • Naringenin upregulates LXRα and its target genes in human macrophages in an AMPK-dependent manner.
  • Enhanced expression of cholesterol efflux genes suggests a role for naringenin in preventing foam cell progression.
  • Naringenin's modulation of cholesterol efflux pathways may offer a novel therapeutic strategy against atherosclerosis.
Keywords:
AMPKLXRαTHP-1atherosclerosisinflammationnaringenin

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