Microsome biocolloids for rapid drug metabolism and inhibition assessment by LC-MS

Drug Metab Lett. 2008 Aug;2(3):158-62. doi: 10.2174/187231208785425854.

Abstract

Rat liver microsomes attached to nanoparticles were used for LC-MS studies of CYP3A and 2E1 enzymes in metabolism of N-nitroso compounds. Using these biocolloids, turnover rates were measured within 2 min. Inhibitor IC(50) values for ketoconazole (KET) and 4-methylpyrazole (4-MEP) were estimated.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Chromatography, Liquid / methods
  • Colloids / chemistry
  • Cytochrome P-450 CYP2E1 / metabolism*
  • Cytochrome P-450 CYP2E1 Inhibitors
  • Cytochrome P-450 CYP3A / metabolism*
  • Cytochrome P-450 CYP3A Inhibitors
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / pharmacology*
  • Fomepizole
  • Inhibitory Concentration 50
  • Ketoconazole / administration & dosage
  • Ketoconazole / pharmacology
  • Microsomes, Liver / enzymology
  • Microsomes, Liver / metabolism
  • Nanoparticles
  • Nitroso Compounds / metabolism*
  • Pyrazoles / administration & dosage
  • Pyrazoles / pharmacology
  • Rats
  • Tandem Mass Spectrometry / methods

Substances

  • Colloids
  • Cytochrome P-450 CYP2E1 Inhibitors
  • Cytochrome P-450 CYP3A Inhibitors
  • Enzyme Inhibitors
  • Nitroso Compounds
  • Pyrazoles
  • Fomepizole
  • Cytochrome P-450 CYP2E1
  • Cytochrome P-450 CYP3A
  • Ketoconazole