Abstract
PPAR-gamma has been known to induce suppression, differentiation and reversal of malignant changes in colon cancer in vitro. However, there are several reports that PPAR-gamma ligands enhance colon polyp development in APCmin mice in vivo. These contradictory results have not yet been thoroughly explained. To explain the contradictory results, we analyzed the effects of different concentrations of the PPAR-gamma agonist, 15-deoxy-D12, 14-prostaglandin (15-d Delta PGJ2) and pioglitazone, on APC gene-mutated colon cancer cell lines (HT-29). We measured cell growth and suppression by cell count and MTT assay and analyzed the expression of beta-catenin and c-Myc protein by Western blot. In addition, we inoculated HT-29 cells into APCmin mice to compare tumor size. High concentrations (10-100 microM/L 15-d Delta PGJ2 and pioglitazone) of PPAR-gamma ligand suppressed growth, while low concentrations (0.01-1 microM/L 15-d Delta PGJ2 and pioglitazone) of PPAR-gamma ligand promoted growth. In particular, the effects of 0.1 microM/L 15-d Delta PGJ2 and pioglitazone on cell growth were statistically significant (P = 0.003, P = 0.001, respectively). Tumor growth was associated with an increase in beta-catenin and c-Myc expression. The growth of xenograft tumors was greater in PPAR-gamma ligand-treated mice than in control mice (control vs day 14: P = 0.024, control vs day 28: P = 0.007). The expression of beta-catenin and c-Myc protein were also elevated in PPAR-gamma-treated mouse tissues. PPAR-gamma ligand can promote the growth of APC-mutated HT-29 colon cancer cells in vitro and in vivo. In addition, the tumor promoting effect seems to be associated with an increase in beta-catenin and c-Myc expression. We think that well-controlled clinical trials should be conducted to confirm our results and to verify clinical applications.
MeSH Terms
Animals
Cell Proliferation/drug effects
Colonic Neoplasms/metabolism,pathology
Disease Models, Animal
Dose-Response Relationship, Drug
Gene Expression Regulation/drug effects
Genes, APC
HT29 Cells
Humans
Ligands
Mice
Mice, Nude
Mutation
PPAR gamma/metabolism
Pioglitazone
Prostaglandin D2/administration & dosage,analogs & derivatives,pharmacology
Proto-Oncogene Proteins c-myc/drug effects
Thiazolidinediones/administration & dosage,pharmacology
Xenograft Model Antitumor Assays
beta Catenin/drug effects,metabolism
Chemicals
15-deoxy-delta(12,14)-prostaglandin J2
Ligands
PPAR gamma
Proto-Oncogene Proteins c-myc
Thiazolidinediones
beta Catenin
Prostaglandin D2
Pioglitazone
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Choi I K
Division of Medical Oncology, Department of Internal Medicine, Medical College, Korea University Guro Hospital, 80 Guro-dong, Seoul, South Korea.
Kim Y H
Kim J S
Seo J H
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