Plasma rich in quercetin metabolites induces G2/M arrest by upregulating PPAR-γ expression in human A549 lung cancer cells

Planta Med. 2011 Jul;77(10):992-8. doi: 10.1055/s-0030-1250735. Epub 2011 Jan 25.


In this study, we incubated human A549 lung cancer cells with quercetin-metabolite-enriched plasma (QMP) obtained from Mongolian gerbils 2 h after quercetin feeding (100 mg/kg body wt/week). We investigated the effects of QMP on the growth of A549 cells and the possible mechanisms for these effects. We found that QMP but not control plasma (CP) reduced the cell growth in A549 cells. QMP led to cell cycle arrest at the G (2)/M phase by downregulating the expression of cdk1 and cyclin B. QMP but not CP or quercetin itself significantly increased PPAR- γ expression (p < 0.05), which was accompanied by an increase of phosphatase and tensin homologue deleted on the chromosome ten level and a decrease of phosphorylation of Akt. Furthermore, quercetin-3-glucuronide and quercetin-3'-sulfate also significantly increased PPAR- γ expression in A549 cells. GW9662, a PPAR- γ antagonist, significantly suppressed the effects of 10 % QMP on cell proliferation and on the expression of cyclin B and cdk1. Taken together, these data suggest that the activation of PPAR- γ plays an important role, at least in part, in the antiproliferative effects of quercetin metabolites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Anilides / pharmacology
  • Animals
  • CDC2 Protein Kinase / drug effects
  • CDC2 Protein Kinase / metabolism
  • Cell Division / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cyclin B / drug effects
  • Cyclin B / metabolism
  • G2 Phase / drug effects*
  • Gerbillinae
  • Humans
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / pathology
  • Male
  • Oncogene Protein v-akt / drug effects
  • Oncogene Protein v-akt / metabolism
  • PPAR gamma / antagonists & inhibitors
  • PPAR gamma / metabolism*
  • PTEN Phosphohydrolase / drug effects
  • PTEN Phosphohydrolase / metabolism
  • Phosphorylation / drug effects
  • Plasma / metabolism
  • Quercetin / administration & dosage
  • Quercetin / analogs & derivatives
  • Quercetin / metabolism*
  • Quercetin / pharmacology*
  • Up-Regulation / drug effects


  • 2-chloro-5-nitrobenzanilide
  • Anilides
  • Cyclin B
  • PPAR gamma
  • quercetin 3'-sulfate
  • Quercetin
  • Oncogene Protein v-akt
  • CDC2 Protein Kinase
  • PTEN Phosphohydrolase
  • PTEN protein, human