Cilostazol and enzymatically modified isoquercitrin attenuate experimental colitis and colon cancer in mice by inhibiting cell proliferation and inflammation

Food Chem Toxicol. 2017 Feb:100:103-114. doi: 10.1016/j.fct.2016.12.018. Epub 2016 Dec 15.

Abstract

We previously reported the anti-inflammatory effects of cilostazol, a selective inhibitor of phosphodiesterase 3, and two antioxidants, enzymatically modified isoquercitrin and α-lipoic acid in a dextran sodium sulphate-induced colitis mouse model. We further examined the chemopreventive effects of these substances in a murine azoxymethane/dextran sodium sulphate -induced colorectal carcinoma model and compared the effects with those of the well-known anticancer natural plant pigment, anthocyanin. In addition, the effects on cell proliferation activity were evaluated in colon cancer cell lines and mucosal epithelial cells in a model of acute dextran sodium sulphate-induced colitis. Cilostazol and enzymatically modified isoquercitrin improved the outcome of azoxymethane/dextran sodium sulphate-induced colorectal cancer along with anthocyanin though inhibiting inflammation and cell proliferation, but the effect of α-lipoic acid was minimal. Inhibition of cell proliferation by cilostazol was confirmed in vitro. In the acute dextran sodium sulphate-induced colitis model, cilostazol and enzymatically modified isoquercitrin prevented the decrease in epithelial proliferative cells. These results indicate that cilostazol and enzymatically modified isoquercitrin first exhibited an anti-dextran sodium sulphate effect at the initial stage of colitis and then showed antitumour effects throughout subsequent inflammation-related cancer developmental stages.

Keywords: Cilostazol; Colorectal cancer; Enzymatically modified isoquercitrin; Murine azoxymethane/dextran sodium sulphate-induced colorectal carcinoma model; Reactive oxygen species.

MeSH terms

  • Animals
  • Azoxymethane / toxicity
  • Carcinogens / toxicity
  • Cell Proliferation / drug effects*
  • Cilostazol
  • Colitis / chemically induced
  • Colitis / drug therapy*
  • Colitis / pathology
  • Colonic Neoplasms / chemically induced
  • Colonic Neoplasms / drug therapy*
  • Colonic Neoplasms / pathology
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Immunohistochemistry
  • Inflammation / metabolism
  • Inflammation / prevention & control*
  • Mice
  • Mice, Inbred BALB C
  • Organ Size / drug effects
  • Quercetin / analogs & derivatives*
  • Quercetin / pharmacology
  • Tetrazoles / pharmacology*
  • Vasodilator Agents / pharmacology

Substances

  • Carcinogens
  • Tetrazoles
  • Vasodilator Agents
  • isoquercitrin
  • Quercetin
  • Azoxymethane
  • Cilostazol