Synthetic heteroprostanoids of A- and E-types as novel non-comprehensive inhibitors of adenylyl cyclase in rat hepatocytes

Biochem Biophys Res Commun. 2006 Mar 10;341(2):357-62. doi: 10.1016/j.bbrc.2005.12.196. Epub 2006 Jan 19.

Abstract

Treatment of rat hepatocyte plasma membranes with five novel synthetic heteroprostanoids of A- and E-types significantly decreased basal activity of adenylyl cyclase. Inhibition of forskolin-stimulated activity of the enzyme was seen as well. The maximal effective concentration for all substances tested was found at approximately 5x10(-6)-1x10(-5) M. The values of half maximal concentration (IC50) for all prostanoids were at the region of 0.7-1.1 microM. Prostanoids belonging to cyclopentenone group A (U-39, U-26) were less active than analogs of 11-deoxy-PGE1 (TA-227, TA-280, and TA-239). The strongest inhibitory effect of adenylyl cyclase activity (more than 3 times) was determined in the presence of prostanoid TA-227 possessing hydrophobic 15-phenyl ring and isoxazol group in omega-chain. The investigation of AC activity in the presence of different concentrations of prostanoids and varying concentrations of Mg x ATP has demonstrated that a non-comprehensive mechanism with particular effect takes place in case of AC inhibition by the heteroprostanoids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclase Inhibitors*
  • Adenylyl Cyclases / metabolism
  • Alprostadil / analogs & derivatives
  • Alprostadil / metabolism
  • Animals
  • Cell Membrane / metabolism
  • Colforsin / metabolism
  • Cyclic AMP / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology*
  • Hepatocytes / drug effects
  • Hepatocytes / enzymology*
  • Hepatocytes / metabolism
  • Inhibitory Concentration 50
  • Male
  • Models, Chemical
  • Prostaglandins / chemistry*
  • Prostaglandins / metabolism
  • Rats
  • Rats, Wistar

Substances

  • Adenylyl Cyclase Inhibitors
  • Enzyme Inhibitors
  • Prostaglandins
  • Colforsin
  • Cyclic AMP
  • Adenylyl Cyclases
  • Alprostadil
  • 11-deoxyprostaglandin E1