Characterization of PPAR dual ligand MCC-555 in AOM-induced colorectal tumorigenesis

Exp Toxicol Pathol. 2013 Sep;65(6):919-24. doi: 10.1016/j.etp.2013.01.005. Epub 2013 Jan 29.

Abstract

Colorectal cancer (CRC) is one of the most commonly diagnosed cancers. Peroxisome proliferator-activated receptor γ (PPARγ) agonists represent a potentially important family of chemopreventive/therapeutic compounds for cancer treatment by affecting cell proliferation, differentiation, and apoptosis. Dual ligands for PPARα and PPARγ, such as netoglitazone (MCC-555), have been developed to improve treatment of metabolic syndromes, including hyperglycemia and hyperlipidemia. Interestingly, these dual ligands also possess anti-proliferative activities against a variety of cancer cell lines with a greater potency than conventional PPARγ specific ligands. In this study, chemopreventive properties of MCC-555 in colorectal tumorigenesis were evaluated using azoxymethane (AOM)-induced colonic aberrant crypt foci (ACF) in A/J mice. We found that MCC-555 suppressed AOM-induced ACF in A/J mice, compared to the control group. Administration of MCC-555 resulted in decreased mitoses and increased apoptotic cells in the colon. Furthermore, expression of tumor suppressor protein MUC2 was increased in MCC-555 treated mice. Our data clearly suggest that MCC-555 has an effect on the early events of colon carcinogenesis, thus providing evidence that MCC-555 could be a potential preventive compound for CRC.

Keywords: ACF; ANOVA; AOM; Aberrant crypt foci; Azoxymethane; CMC; CRC; Colon cancer; H&E; MCC-555; PPAR; PPAR ligand; TUNEL; TdT; TdT-mediated deoxyuridine triphosphate nick-end labeling; aberrant crypt foci; analysis of variance; azoxymethane; carboxyl methyl cellulose; colorectal cancer; hematoxylin and eosin; peroxisome proliferator-activated receptor; terminal deoxynucleotidyl transferase.

Publication types

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

MeSH terms

  • Aberrant Crypt Foci / chemically induced
  • Aberrant Crypt Foci / metabolism
  • Aberrant Crypt Foci / pathology
  • Aberrant Crypt Foci / prevention & control*
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Azoxymethane / toxicity*
  • Colorectal Neoplasms / chemically induced
  • Colorectal Neoplasms / metabolism
  • Colorectal Neoplasms / pathology
  • Colorectal Neoplasms / prevention & control*
  • Dose-Response Relationship, Drug
  • Female
  • Mice
  • Mice, Inbred Strains
  • Mitosis / drug effects
  • Mucin-2 / biosynthesis
  • PPAR gamma / agonists*
  • Thiazolidinediones / administration & dosage
  • Thiazolidinediones / pharmacology
  • Thiazolidinediones / therapeutic use*

Substances

  • Antineoplastic Agents
  • Muc2 protein, mouse
  • Mucin-2
  • PPAR gamma
  • Thiazolidinediones
  • Azoxymethane
  • netoglitazone