Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity

Molecules. 2021 Jan 2;26(1):200. doi: 10.3390/molecules26010200.

Abstract

Human neutrophil elastase (HNE) is used as diagnostic biomarker for inflammation/infection. In this work, 10 ionic liquids (ILs) and 11 ionic liquids active pharmaceutical ingredients (ILs-APIs) were tested to evaluate the inhibition effect on the activity of porcine pancreatic elastase enzyme, frequently employed as a model for HNE. The insertion of ionic liquids in some drugs is useful, as the insertion of ILs with inhibitory capacity will also slow down all processes in which this enzyme is involved. Therefore, a spectrophotometric method was performed to the determination of EC50 values of the compounds tested. EC50 values of 124 ± 4 mM to 289 ± 11 mM were obtained, with the most toxic IL for elastase being tetrabutylammonium acetate and the least toxic 1-butyl-3-methylimidazolium acetate. Moreover, sodium salicylate (raw material) presented the lower and benzethonium bistriflimide the higher EC50 when compared with all the IL-APIs tested. This work provides significant information about the effect of the studied IL and IL-APIs in elastase enzyme activity.

Keywords: elastase; enzyme activity; inhibition; ionic liquids; ionic liquids active pharmaceutical ingredients.

MeSH terms

  • Aniline Compounds / metabolism
  • Animals
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Ionic Liquids / chemistry*
  • Ionic Liquids / pharmacology*
  • Ionic Liquids / toxicity
  • Pancreatic Elastase / antagonists & inhibitors*
  • Pancreatic Elastase / metabolism
  • Quaternary Ammonium Compounds / chemistry
  • Quaternary Ammonium Compounds / pharmacology
  • Serine Proteinase Inhibitors / chemistry*
  • Serine Proteinase Inhibitors / pharmacology*
  • Sodium Salicylate / pharmacology
  • Structure-Activity Relationship
  • Swine

Substances

  • 1-butyl-3-methylimidazolium
  • Aniline Compounds
  • Imidazoles
  • Ionic Liquids
  • Quaternary Ammonium Compounds
  • Serine Proteinase Inhibitors
  • 4-nitroaniline
  • tetrabutylammonium
  • Pancreatic Elastase
  • Sodium Salicylate