Phloretin induces apoptosis in H-Ras MCF10A human breast tumor cells through the activation of p53 via JNK and p38 mitogen-activated protein kinase signaling

Ann N Y Acad Sci. 2009 Aug:1171:479-83. doi: 10.1111/j.1749-6632.2009.04692.x.

Abstract

Mutations in Ras play a critical role in the development of human cancers, including breast cancer. We investigated the possible antiproliferative effects of the naturally occurring dihydrochalcone phloretin [2',4',6'-trihydroxy-3-(4-hydroxyphenyl)-propiophenone] on H-Ras-transformed MCF10A human breast epithelial (H-Ras MCF10A) cells. Phloretin suppressed H-Ras MCF10A cell proliferation in a dose-dependent manner and induced nuclear condensation in the cells, indicating that phloretin-induced cell death occurs mainly via the induction of apoptosis. Prominent upregulation of p53 and Bax and cleavage of poly (ADP)-ribose polymerase were also detected in the phloretin-treated cells. Finally, phloretin markedly increased caspase-3 activity as well as JNK and p38 mitogen-activated protein kinase signaling. Our findings suggest that the phloretin-induced apoptosis of breast tumor cells contributes to the chemopreventive potential of phloretin against breast cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Blotting, Western
  • Caspase 3 / metabolism
  • Cell Line, Transformed
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Genes, ras / genetics
  • Humans
  • JNK Mitogen-Activated Protein Kinases / metabolism*
  • MAP Kinase Signaling System / drug effects*
  • Mammary Glands, Human / drug effects
  • Mammary Glands, Human / metabolism
  • Molecular Structure
  • Phloretin / chemistry
  • Phloretin / pharmacology*
  • Poly(ADP-ribose) Polymerases / metabolism
  • Tumor Suppressor Protein p53 / metabolism*
  • bcl-2-Associated X Protein / metabolism
  • bcl-X Protein / metabolism
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • BCL2L1 protein, human
  • Tumor Suppressor Protein p53
  • bcl-2-Associated X Protein
  • bcl-X Protein
  • Poly(ADP-ribose) Polymerases
  • JNK Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases
  • Caspase 3
  • Phloretin