Quercetin as the active principle of Hypericum hircinum exerts a selective inhibitory activity against MAO-A: extraction, biological analysis, and computational study

J Nat Prod. 2006 Jun;69(6):945-9. doi: 10.1021/np060015w.

Abstract

The methanol extract from Hypericum hircinum leaves exhibited in vitro inhibition of monoamine oxidases (MAO). Bioassay-guided fractionation led to the isolation of quercetin and five compounds identified for the first time from H. hircinum. Quercetin was the only compound with a selective inhibitory activity against MAO-A, with an IC50 value of 0.010 microM. To explain MAO selective inhibition at the molecular level, a computational study was carried out by conformational search and docking techniques using recently determined crystallographic models of both enzymatic isoforms. An in vivo study in mice was carried out using the forced swimming test in order to elucidate the behavioral effects of quercetin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Disease Models, Animal
  • Hypericum / chemistry*
  • Inhibitory Concentration 50
  • Mice
  • Molecular Conformation
  • Molecular Structure
  • Monoamine Oxidase Inhibitors* / chemistry
  • Monoamine Oxidase Inhibitors* / isolation & purification
  • Monoamine Oxidase Inhibitors* / pharmacology
  • Motor Activity / drug effects
  • Plant Leaves / chemistry
  • Plants, Medicinal / chemistry*
  • Quercetin* / analogs & derivatives
  • Quercetin* / chemistry
  • Quercetin* / isolation & purification
  • Quercetin* / pharmacology
  • Swimming

Substances

  • Monoamine Oxidase Inhibitors
  • Quercetin