The effect of chloroquine administration on two experimental models of acute pancreatitis

Gastroenterology. 1993 Jun;104(6):1768-79. doi: 10.1016/0016-5085(93)90658-y.

Abstract

Background: Recent experimental findings have suggested that activation of trypsinogen by cathepsin B within acidic pancreatic acinar cell cytoplasmic vacuoles may be a critical early event in both secretagogue and diet-induced pancreatitis. The weak base chloroquine accumulates within acidic intracellular compartments, raises their pH, and can inhibit proteolysis as well as cathepsin B.

Methods: We have investigated the effect of in vivo chloroquine administration on both secretagogue and diet-induced experimental pancreatitis to determine if raising the pH of cytoplasmic vacuoles in these models of pancreatitis would have a protective effect.

Results: Infusion of chloroquine (5 mg.kg-1.h-1) resulted in the uptake and concentration of chloroquine in the pancreas, an increase in the pH of acinar cell acidic compartments, and interference with the pH-dependent sorting of lysosomal hydrolases from digestive enzyme zymogens. However, chloroquine administration did not have a protective effect against the hyperamylasemia, the pancreatic edema, the morphological changes or the mortality that is associated with these models of pancreatitis.

Conclusions: These observations lead us to conclude that raising the pH of acinar cell acidic compartments by in vivo administration of chloroquine does not prevent either secretagogue or diet-induced pancreatitis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acute Disease
  • Animals
  • Cathepsin B / pharmacology
  • Chloroquine / pharmacokinetics
  • Chloroquine / therapeutic use*
  • Enzyme Activation
  • Hydrogen-Ion Concentration
  • Male
  • Pancreatitis / etiology
  • Pancreatitis / pathology
  • Pancreatitis / prevention & control*
  • Rats
  • Rats, Wistar
  • Trypsinogen / metabolism
  • Vacuoles / drug effects
  • Vacuoles / metabolism

Substances

  • Chloroquine
  • Trypsinogen
  • Cathepsin B