Chemoprevention of colon carcinogenesis by oleanolic acid and its analog in male F344 rats and modulation of COX-2 and apoptosis in human colon HT-29 cancer cells

Pharm Res. 2008 Sep;25(9):2151-7. doi: 10.1007/s11095-008-9582-7. Epub 2008 Apr 12.

Abstract

Purpose: To assess the chemopreventive effect of oleanolic acid (ONA) and its synthetic analog 18alpha-olean-12-ene-3beta-23,28-triol (OT) on azoxymethane (AOM)-induced colonic aberrant crypt foci (ACF) in F344 rats and understand anti-inflammatory properties and apoptosis effects in HT29 colon cancer cells and Raw 264.7 macrophage cell lines.

Methods: Five week-old male F344 rats were fed a control diet or experimental diets containing two doses of ONA (750 and 1,500 ppm) and OT (250 and 500 ppm). After 1 week, all animals were s.c. injected with AOM (15 mg/kg body weight, once weekly for 2 weeks). At 14 weeks of age, all rats were killed and colons were evaluated for ACF. Cyclooxygenase (COX)-2, inducible nitric oxide synthase (iNOS) expressions and apoptosis were assessed in cell lines exposed to OT using western blots and 4',6-diamidino-2-phenylindole staining.

Results: Administration of ONA and OT inhibited mean colonic ACF and multi-crypt AC/foci in a dose dependent manner (p < 0.001-0.0001). OT blocked the COX-2 expression induced by phorbol 12-myristate 13-acetate in a dose-dependent manner and induced apoptosis in HT-29 cancer cells, and suppressed iNOS activation in RAW264.7 macrophages.

Conclusions: ONA and OT possess chemopreventive activity against colon carcinogenesis in rat and OT inhibits the COX-2 and iNOS and induces apoptosis in cell lines.

MeSH terms

  • Animals
  • Anticarcinogenic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Azoxymethane
  • Cell Proliferation / drug effects
  • Colonic Neoplasms / chemically induced
  • Colonic Neoplasms / enzymology
  • Colonic Neoplasms / pathology
  • Colonic Neoplasms / prevention & control*
  • Cyclooxygenase 2 / metabolism*
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • HT29 Cells
  • Humans
  • Macrophages / drug effects
  • Macrophages / enzymology
  • Macrophages / pathology
  • Male
  • Mice
  • Nitric Oxide Synthase Type II / antagonists & inhibitors
  • Nitric Oxide Synthase Type II / metabolism
  • Oleanolic Acid / analogs & derivatives
  • Oleanolic Acid / pharmacology*
  • Precancerous Conditions / chemically induced
  • Precancerous Conditions / enzymology
  • Precancerous Conditions / pathology
  • Precancerous Conditions / prevention & control*
  • Rats
  • Rats, Inbred F344

Substances

  • Anticarcinogenic Agents
  • Cyclooxygenase 2 Inhibitors
  • Oleanolic Acid
  • NOS2 protein, human
  • Nitric Oxide Synthase Type II
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Azoxymethane