Kavalactone pharmacophores for major cellular drug targets

Mini Rev Med Chem. 2011 Jan;11(1):79-83. doi: 10.2174/138955711793564088.

Abstract

A number of studies have identified differential kavalactone activity against a variety of molecular targets, including P-glycoprotein (Pgp), platelet monoamine oxidase (MAO-B), transcription factor binding domains, pregnane X (PXR) and GABA receptors, and cytochrome P450 and cyclo-oxygenase (COX) enzymes. The molecular structure of the kavalactones possesses a pharmacophore for several of these targets. In most cases, conformational stability is more significant than the substituents present. The analysis of these pharmacophores provides important insights for future medicinal chemistry-based approaches to kavalactone-type drugs.

Publication types

  • Review

MeSH terms

  • Animals
  • Cells / enzymology
  • Cells / metabolism*
  • Drug Discovery
  • Humans
  • Lactones / chemistry
  • Lactones / metabolism*
  • Lactones / pharmacology
  • Pyrones / chemistry
  • Pyrones / metabolism*
  • Pyrones / pharmacology

Substances

  • Lactones
  • Pyrones