Pseudopterosin A inhibits phagocytosis and alters intracellular calcium turnover in a pertussis toxin sensitive site in Tetrahymena thermophila

Comp Biochem Physiol C Toxicol Pharmacol. 2006 Aug;143(4):436-43. doi: 10.1016/j.cbpc.2006.04.005. Epub 2006 Apr 28.

Abstract

The free living ciliate Tetrahymena thermophila was chosen as a cellular model in order to investigate the mode of action of the anti-inflammatory marine natural product Pseudopterosin A (PsA). In this paper we present evidence that PsA inhibits phagosome formation (KD=10.5 microM) and triggers a discrete intracellular calcium release (depletion) from a site in T. thermophila cells (KD=6.4 microM). Pre-treatment with the Gi/o protein inhibitor, pertussis toxin (PTX), inhibits PsA activity of both responses providing pharmacological evidence that the site of action for PsA is at a PTX sensitive G protein or a G protein coupled receptor (GPCR). Addition of extracellular calcium induced a concentration dependent increase in the incidence of phagosome formation (KD=30.3 microM) and was blocked by PsA pre-treatment. This particular effect of PsA on extracellular calcium was not blocked by PTX pre-treatment.

Publication types

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

MeSH terms

  • Animals
  • Calcium / metabolism*
  • Calcium Chloride / pharmacology
  • Diterpenes / antagonists & inhibitors
  • Diterpenes / pharmacology*
  • Estrenes / pharmacology
  • GTP-Binding Proteins / physiology
  • Glycosides / antagonists & inhibitors
  • Glycosides / pharmacology*
  • Pertussis Toxin / pharmacology*
  • Phagocytosis / drug effects*
  • Phagosomes / drug effects
  • Phagosomes / physiology
  • Pyrrolidinones / pharmacology
  • Tetrahymena thermophila / drug effects

Substances

  • Diterpenes
  • Estrenes
  • Glycosides
  • Pyrrolidinones
  • pseudopterosins
  • 1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
  • Pertussis Toxin
  • GTP-Binding Proteins
  • Calcium Chloride
  • Calcium