Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II

J Enzyme Inhib Med Chem. 2012 Feb;27(1):37-42. doi: 10.3109/14756366.2011.574130. Epub 2011 May 3.

Abstract

The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was compared to recombinant hCA I and hCA II expressed in Ecoli. IC(50) values of the drugs that caused inhibition were determined by means of activity percentage diagrams. The IC(50) concentrations of dexketoprofen trometamol and dexamethasone sodium phosphate on hCA I were 683 μM and 4250 μM and for hCA II 950 μM and 6200 μM respectively. Conversely, the enzyme activity was increased by diflofenac sodium. In addition, thiocolchicoside has not any affect on hCA I and hCA II. The effect of these drugs on erythrocyte hCA I and hCA II were consistent with the inhibition of recombinant enzymes.

MeSH terms

  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Carbonic Anhydrase I / antagonists & inhibitors*
  • Carbonic Anhydrase I / isolation & purification
  • Carbonic Anhydrase I / metabolism
  • Carbonic Anhydrase II / antagonists & inhibitors*
  • Carbonic Anhydrase II / isolation & purification
  • Carbonic Anhydrase II / metabolism
  • Dose-Response Relationship, Drug
  • Erythrocytes / cytology
  • Erythrocytes / drug effects*
  • Humans
  • Molecular Structure
  • Recombinant Proteins / antagonists & inhibitors
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Recombinant Proteins
  • Carbonic Anhydrase I
  • Carbonic Anhydrase II