Chrysin, apigenin and acacetin inhibit tumor necrosis factor-related apoptosis-inducing ligand receptor-1 (TRAIL-R1) on activated RAW264.7 macrophages

Int J Mol Sci. 2014 Jun 27;15(7):11510-22. doi: 10.3390/ijms150711510.

Abstract

Expression level of Tumor Necrosis Factor-related apoptosis-inducing ligand (TRAIL) receptors is one of the most important factors of TRAIL-mediated apoptosis in cancer cells. We here report for the first time data concerning TRAIL-R1 and TRAIL-R2 receptor expression on RAW264.7 macrophages. Three substances belonging to flavones: chrysin, apigenin and acacetin which differ from their substituents at the 4' position in the phenyl ring were used in assays because of the variety of biological activities (e.g., anticancer activity) of the polyphenol compounds. The expression of TRAIL-R1 and TRAIL-R2 death receptors on non-stimulated and LPS (lipopolysaccharide)-stimulated macrophages was determined using flow cytometry. We demonstrate that RAW264.7 macrophages exhibit TRAIL-R1 surface expression and that the tested compounds: chrysin, apigenin and acacetin can inhibit TRAIL-R1 death receptor expression level on macrophages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apigenin / pharmacology*
  • Cell Line
  • Flavones / pharmacology*
  • Flavonoids / pharmacology*
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Mice
  • Receptors, TNF-Related Apoptosis-Inducing Ligand / genetics
  • Receptors, TNF-Related Apoptosis-Inducing Ligand / metabolism*

Substances

  • Flavones
  • Flavonoids
  • Receptors, TNF-Related Apoptosis-Inducing Ligand
  • chrysin
  • Apigenin
  • acacetin