Kavalactone pharmacophores for major cellular drug targets

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.