Threshold dose of liver tumor promoting effect of β-naphthoflavone in rats

J Toxicol Sci. 2012;37(3):517-26. doi: 10.2131/jts.37.517.

Abstract

To determine the threshold dose of β-Naphthoflavone (BNF) that induces hepatocellular tumor promoting effects, reactive oxygen species (ROS) generation and thiobarbituric acid-reactive substance (TBARS) formation, and drug-metabolizing enzymes that protect against ROS generation, two-stage liver carcinogenesis model was used. Partial hepatectomized rats (n = 11 to 12) were fed diets containing 0, 0.03, 0.06, 0.125 or 0.25% BNF for 6 weeks after an intraperitoneal injection of N-diethylnitrosamine (DEN) to initiate hepatocarcinogenesis. Histopathologically, glutathione S-transferase placental form (GST-P)-positive foci significantly increased in rats given 0.25% BNF. No marked changes in ROS production and TBARS contents were observed between the BNF treated and DEN alone groups. Real-time RT-PCR showed that the expression of Cyp1a1, Cyp1a2, Cyp1b1 and Nqo1 significantly increased in the groups given 0.03% BNF or more, but Ugt1a6, Akr7a3 and Gstm1 significantly increased in the groups given 0.125% BNF or more. Gpx2 and Yc2 significantly increased in the groups given 0.06% BNF or more and 0.25% BNF, respectively. Inflammation-related genes such as Ccl2, Mmp12, Serpine1 and Cox-2 significantly increased in the 0.25% BNF group. In immunohistochemistry, the number of cyclooxygenase-2 (COX-2)-positive cells increased in rats given 0.25% BNF. These results suggest that 0.25% BNF is the threshold dose for liver tumor promotion, and the fact that inflammation-related genes and COX-2 protein increased in the 0.25% BNF group strongly suggests that inflammation is involved in the liver tumor promoting effect of BNF in rats.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aryl Hydrocarbon Hydroxylases / genetics
  • Aryl Hydrocarbon Hydroxylases / metabolism
  • Chemokine CCL2 / genetics
  • Chemokine CCL2 / metabolism
  • Cyclooxygenase 2 / genetics
  • Cyclooxygenase 2 / metabolism
  • Cytochrome P-450 CYP1A1 / genetics
  • Cytochrome P-450 CYP1A1 / metabolism
  • Cytochrome P-450 CYP1A2
  • Cytochrome P-450 CYP1B1
  • Cytochromes / genetics
  • Cytochromes / metabolism
  • Diethylnitrosamine / toxicity
  • Dose-Response Relationship, Drug
  • Glucuronosyltransferase / genetics
  • Glucuronosyltransferase / metabolism
  • Glutathione Peroxidase / genetics
  • Glutathione Peroxidase / metabolism
  • Glutathione Transferase / genetics
  • Glutathione Transferase / metabolism
  • Hepatectomy / methods
  • Immunohistochemistry
  • Lipid Peroxidation / drug effects
  • Liver / drug effects*
  • Liver / pathology
  • Liver Neoplasms, Experimental / chemically induced
  • Liver Neoplasms, Experimental / pathology*
  • Male
  • NAD(P)H Dehydrogenase (Quinone) / genetics
  • NAD(P)H Dehydrogenase (Quinone) / metabolism
  • Oxidative Stress / drug effects
  • Plasminogen Activator Inhibitor 1 / genetics
  • Plasminogen Activator Inhibitor 1 / metabolism
  • Rats
  • Rats, Inbred F344
  • Reactive Oxygen Species / metabolism
  • Real-Time Polymerase Chain Reaction
  • Thiobarbituric Acid Reactive Substances / metabolism
  • Up-Regulation
  • beta-Naphthoflavone / toxicity*

Substances

  • Ccl2 protein, rat
  • Chemokine CCL2
  • Cytochromes
  • Plasminogen Activator Inhibitor 1
  • Reactive Oxygen Species
  • Serpine1 protein, rat
  • Thiobarbituric Acid Reactive Substances
  • Diethylnitrosamine
  • beta-Naphthoflavone
  • Glutathione Peroxidase
  • glutathione peroxidase 2, rat
  • Aryl Hydrocarbon Hydroxylases
  • Cyp1a2 protein, rat
  • Cyp1b1 protein, rat
  • Cytochrome P-450 CYP1A1
  • Cytochrome P-450 CYP1A2
  • Cytochrome P-450 CYP1B1
  • Cyclooxygenase 2
  • Ptgs2 protein, rat
  • NAD(P)H Dehydrogenase (Quinone)
  • NQO1 protein, rat
  • Glucuronosyltransferase
  • UDP-glucuronosyltransferase, UGT1A7
  • Glutathione Transferase
  • glutathione S-transferase M1