Faculty of Pharmacy, Bank Building (A15), University of Sydney, Sydney, NSW 2006, Australia.
Mini Rev Med Chem. 2011 Jan;11(1):79-83. doi: 10.2174/138955711793564088.
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.
许多研究已经确定了不同的卡瓦内酯对各种分子靶点的活性，包括 P-糖蛋白 (Pgp)、血小板单胺氧化酶 (MAO-B)、转录因子结合结构域、孕烷 X (PXR) 和 GABA 受体以及细胞色素 P450 和环氧化酶 (COX) 酶。卡瓦内酯的分子结构具有针对其中一些靶点的药效团。在大多数情况下，构象稳定性比存在的取代基更为重要。对这些药效团的分析为基于药物化学的卡瓦内酯类药物的未来方法提供了重要的见解。
