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.
Keywords: Kavalactone, pharmacophore, molecular targets, conformational isomerism, Piper methysticum, P-Glycoprotein (Pgp), kavain/dihydrokavain, methysticin/dihydromethysticin, desmethoxyyangonin, Cyclo-Oxygenase Enzymes, COX, NSAIDs, luciferase-based assay, Kavain, 7,8-Dihydrokavain, Methysticin, 7,8-Dihydromethysticin, Yangonin, Cytochrome P450, Pregnane X Receptor, GABA, LITAF
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