5,7,3',4'-tetramethoxyflavone ameliorates cholesterol dysregulation by mediating SIRT1/FOXO3a/ABCA1 signaling in osteoarthritis chondrocytes

Future Med Chem. 2021 Dec;13(24):2153-2166. doi: 10.4155/fmc-2021-0247. Epub 2021 Oct 5.

Abstract

Dyslipidemia has been associated with the development of osteoarthritis. Our previous study found that 5,7,3',4'-tetramethoxyflavone (TMF) exhibited protective activities against the pathological changes of osteoarthritis. Aim: To investigate the roles of TMF in regulating ABCA1-mediated cholesterol metabolism. Methods: Knockdown and overexpression were employed to study gene functions. Protein-protein interaction was investigated by co-immunoprecipitation, and the subcellular locations of proteins were studied by immunofluorescence. Results: IL-1β decreased ABCA1 expression and induced apoptosis. Therapeutically, TMF ameliorated the effects of IL-1β. FOXO3a knockdown expression abrogated the effects of TMF, and FOXO3a overexpression increased ABCA1 expression by interacting with LXRα. TMF promoted FOXO3a nuclear translocation by activating SIRT1 expression. Conclusions: TMF ameliorates cholesterol dysregulation by increasing the expression of FOXO3a/LXRα/ABCA1 signaling through SIRT1 in C28/I2 cells.

Keywords: ABCA1; FOXO3a; SIRT1; TMF; osteoarthritis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter 1 / genetics
  • ATP Binding Cassette Transporter 1 / metabolism*
  • Cells, Cultured
  • Cholesterol / metabolism
  • Chondrocytes / drug effects*
  • Chondrocytes / metabolism
  • Chondrocytes / pathology
  • Forkhead Box Protein O3 / genetics
  • Forkhead Box Protein O3 / metabolism*
  • Humans
  • Luteolin / chemistry
  • Luteolin / pharmacology*
  • Osteoarthritis / drug therapy*
  • Osteoarthritis / metabolism
  • Osteoarthritis / pathology
  • Signal Transduction / drug effects
  • Sirtuin 1 / genetics
  • Sirtuin 1 / metabolism*

Substances

  • ABCA1 protein, human
  • ATP Binding Cassette Transporter 1
  • FOXO3 protein, human
  • Forkhead Box Protein O3
  • methoxyluteolin
  • Cholesterol
  • SIRT1 protein, human
  • Sirtuin 1
  • Luteolin