Effect of thuringiensin on adenylate cyclase in rat cerebral cortex

Toxicol Appl Pharmacol. 2004 Jan 1;194(1):34-40. doi: 10.1016/j.taap.2003.08.015.

Abstract

The purpose of this work is to evaluate the effect of thuringiensin on the adenylate cyclase activity in rat cerebral cortex. The cyclic adenosine 3'5'-monophosphate (cAMP) levels were shown to be dose-dependently elevated 17-450% or 54-377% by thuringiensin at concentrations of 10 microM-100 mM or 0.5-4 mM, due to the activation of basal adenylate cyclase activity of rat cerebral cortical membrane preparation. Thuringiensin also activated basal activity of a commercial adenylate cyclase from Escherichia coli. However, the forskolin-stimulated adenylate cyclase activity in rat cerebral cortex was inhibited by thuringiensin at concentrations of 1-100 microM, thus cAMP production decreased. Furthermore, thuringiensin or adenylate cyclase inhibitor (MDL-12330A) reduced the forskolin (10 microM)-stimulated adenylate cyclase activity at concentrations of 10 microM, 49% or 43% inhibition, respectively. In conclusion, this study demonstrated that thuringiensin could activate basal adenylate cyclase activity and increase cAMP concentrations in rat cerebral cortex or in a commercial adenylate cyclase. Comparing the dose-dependent effects of thuringiensin on the basal and forskolin-stimulated adenylate cyclase activity, thuringiensin can be regarded as a weak activator of adenylate cyclase or an inhibitor of forskolin-stimulated adenylate cyclase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemistry
  • Adenosine / pharmacology*
  • Adenylyl Cyclases / metabolism*
  • Animals
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / enzymology*
  • Cyclic AMP / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Activation / drug effects
  • Enzyme Activation / physiology
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Sugar Acids / chemistry
  • Sugar Acids / pharmacology*

Substances

  • Sugar Acids
  • Cyclic AMP
  • Adenylyl Cyclases
  • thuringiensin
  • Adenosine