{Gamma}-tocotrienol inhibits pancreatic tumors and sensitizes them to gemcitabine treatment by modulating the inflammatory microenvironment

Cancer Res. 2010 Nov 1;70(21):8695-705. doi: 10.1158/0008-5472.CAN-10-2318. Epub 2010 Sep 23.

Abstract

Pancreatic cancers generally respond poorly to chemotherapy, prompting a need to identify agents that could sensitize tumors to treatment. In this study, we investigated the response of human pancreatic cells to γ-tocotrienol (γ-T3), a novel, unsaturated form of vitamin E found in palm oil and rice bran oil, to determine whether it could potentiate the effects of gemcitabine, a standard of care in clinical treatment of pancreatic cancer. γ-T3 inhibited the in vitro proliferation of pancreatic cancer cell lines with variable p53 status and potentiated gemcitabine-induced apoptosis. These effects correlated with an inhibition of NF-κB activation by γ-T3 and a suppression of key cellular regulators including cyclin D1, c-Myc, cyclooxygenase-2 (COX-2), Bcl-2, cellular inhibitor of apoptosis protein, survivin, vascular endothelial growth factor (VEGF), ICAM-1, and CXCR4. In an orthotopic nude mouse model of human pancreatic cancer, p.o. administration of γ-T3 inhibited tumor growth and enhanced the antitumor properties of gemcitabine. Immunohistochemical analysis indicated a correlation between tumor growth inhibition and reduced expression of Ki-67, COX-2, matrix metalloproteinase-9 (MMP-9), NF-κB p65, and VEGF in the tissue. Combination treatment also downregulated NF-κB activity along with the NF-κB-regulated gene products, such as cyclin D1, c-Myc, VEGF, MMP-9, and CXCR4. Consistent with an enhancement of tumor apoptosis, caspase activation was observed in tumor tissues. Overall, our findings suggest that γ-T3 can inhibit the growth of human pancreatic tumors and sensitize them to gemcitabine by suppressing NF-κB-mediated inflammatory pathways linked to tumorigenesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / pharmacology*
  • Apoptosis / drug effects
  • Blotting, Western
  • Cell Proliferation / drug effects
  • Chromans / pharmacology*
  • Cyclooxygenase 2 / metabolism
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / pharmacology
  • Drug Resistance, Neoplasm / drug effects*
  • Gemcitabine
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / immunology
  • Inflammation / pathology
  • Inflammation Mediators / metabolism
  • Male
  • Matrix Metalloproteinase 9 / metabolism
  • Mice
  • Mice, Nude
  • NF-kappa B / genetics
  • NF-kappa B / metabolism
  • Pancreatic Neoplasms / drug therapy*
  • Pancreatic Neoplasms / immunology*
  • Pancreatic Neoplasms / pathology
  • RNA, Messenger / genetics
  • Reverse Transcriptase Polymerase Chain Reaction
  • Ribonucleotide Reductases / antagonists & inhibitors
  • Tumor Cells, Cultured
  • Vitamin E / analogs & derivatives*
  • Vitamin E / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • Antimetabolites, Antineoplastic
  • Chromans
  • Inflammation Mediators
  • NF-kappa B
  • RNA, Messenger
  • Deoxycytidine
  • Vitamin E
  • plastochromanol 8
  • Cyclooxygenase 2
  • Ribonucleotide Reductases
  • Matrix Metalloproteinase 9
  • Gemcitabine