Interleukin-1 beta- and tumour-necrosis-factor-induced inhibition of rat gastric fundus motility in vitro

Pharmacol Res. 1994 Jul;30(1):25-33. doi: 10.1016/1043-6618(94)80084-7.

Abstract

In this study, we compared the effects of interleukin-1 beta (IL-1 beta) and tumour necrosis factor (TNF) on in vitro rat gastric fundus motility. IL-1 beta and TNF produced rapid, concentration-dependent relaxation of the rat gastric fundus strips with maximal effect at 300 pg ml-1 and 10 ng ml-1, and estimated EC50S at 10 and 450 pg ml-1, respectively. The relaxant effects of IL-1 beta and TNF were not influenced by the inhibition of cyclo-oxygenase or NO-synthase activities. IL-1 beta- and TNF-induced gastric relaxations were inhibited by BW 755c, which inhibits both cyclo-oxygenase and lipoxygenase (LO), BW A4c, which selectively inhibits the 5-LO pathway, and SC 41930, a selective leukotriene B4 (LTB4) receptor antagonist, providing pharmacological evidence that LTB4 is involved in the relaxant effects of both cytokines. The IL-1 beta- and TNF-induced activation of 5-LO pathway did not appear to be triggered by phospholipase A2. An alternative pathway could involve the activation of a phospholipase C, specific for phosphatidylcholine, from which, in sequence: the formation of diacylglycerol (DAG), DAG-induced activation of protein kinase C and the formation of free arachidonic acid from DAG would ensue. This mechanism is suggested by the finding that LTB4 is able to mimic cytokine-induced strip relaxation only in the presence of phorbol 12-myristate 13-acetate, which selectively activates protein kinase C.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine / pharmacology
  • Animals
  • Dose-Response Relationship, Drug
  • Female
  • Gastric Fundus / physiology*
  • Gastrointestinal Motility / drug effects*
  • In Vitro Techniques
  • Interleukin-1 / pharmacology*
  • Leukotrienes / physiology
  • Male
  • Rats
  • Rats, Wistar
  • Tumor Necrosis Factor-alpha / pharmacology*
  • Type C Phospholipases / physiology

Substances

  • Interleukin-1
  • Leukotrienes
  • Tumor Necrosis Factor-alpha
  • 4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine
  • Type C Phospholipases