Selective COX-2 inhibition is associated with decreased mucosal damage induced by acid and pepsin in rabbit esophagitis

Inflammation. 2003 Feb;27(1):21-9. doi: 10.1023/a:1022635127814.

Abstract

Objective: To evaluate the effects of COX-1 and/or COX-2 inhibition in a model of chronic esophagitis in rabbits.

Methods: Both high- and low-grade esophagitis were induced in rabbits by the perfusion of acidified pepsin. Rabbits were treated with either a selective COX-2 inhibitor (DFU[3-(3-Fluorophenyl)-4-(4-Methanesulfonyl)-5,5-Dimethyl-5H-Furan-2-One];30 mg/Kg/day), a nonspecific COX inhibitor (indomethacin; 2 mg/Kg/day), or a COX-1 preferential inhibitor (piroxicam; 2 mg/Kg/12 h).

Results: Prostaglandins are derived from COX-1 activity in the normal esophagus. Both low- and high-grade esophagitis are associated with a progressive increase of COX activity, which is partially dependent on the COX-2 isoform. DFU reduced muscosal damage in both models of esophagitis. However, indomethacin did not affect significantly mucosal damage, and piroxicam increased damage in low-grade esophagitis.

Conclusions: COX-1 activity is constitutive in the rabbit esophageal mucosa, but both COX-2 and COX-1 activity are increased under the impact of acidified pepsin. Treatment with the COX-2 inhibitor DFU is associated with improvement of mucosal damage, which may have therapeutic implications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acids / administration & dosage
  • Acids / pharmacology
  • Animals
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / administration & dosage
  • Cyclooxygenase Inhibitors / pharmacology*
  • Esophagitis / chemically induced
  • Esophagitis / drug therapy*
  • Esophagitis / enzymology
  • Furans / administration & dosage
  • Furans / pharmacology
  • Indomethacin / administration & dosage
  • Indomethacin / pharmacology
  • Isoenzymes / metabolism*
  • Mouth Mucosa / drug effects*
  • Mouth Mucosa / enzymology
  • Mouth Mucosa / pathology
  • Pepsin A / administration & dosage
  • Pepsin A / pharmacology
  • Piroxicam / administration & dosage
  • Piroxicam / pharmacology
  • Prostaglandin-Endoperoxide Synthases / metabolism*
  • Prostaglandins / analysis
  • Rabbits

Substances

  • 5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methylsulfonyl)phenyl-2(5H)-furanone
  • Acids
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Furans
  • Isoenzymes
  • Prostaglandins
  • Piroxicam
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases
  • Pepsin A
  • Indomethacin