当归中靶向调控核受体TR3抗肿瘤苯酞类成分的分离与鉴定
The isolation and identification of antitumor-active phthalides targeting nuclear receptor TR3 from Angelica sinensis
摘要
近年来，分子靶向药物已成为抗癌新药研究的新趋势，而核受体作为作用靶点之一尤其备受关注。TR3/Bcl-2细胞凋亡途径是一条孤儿核受体TR3参与，独特有效的癌细胞凋亡调控通路。本研究对传统中药材当归进行针对性的组分分离，诣在筛选出具有靶向核受体TR3发挥抗癌作用潜力的化合物。 本研究借助多种色谱学分离手段，对当归的化学成分进行了细致分离，并通过理化性质和现代的波普解析手段分别鉴定了其化学结构，最终得到28个化合物。包括简单苯酞类化合物10个：Z-蒿本内酯（1）、E-蒿本内酯（2）、丁基苯酞（3）、洋川芎内酯G（8）、Z-8-羟基正丁烯苯酞（15）、Z-6，7-epoxyligustilide（... Recent years, molecular targeted drugs have become a new trend of research and development of new anti-cancer drugs. As one of the targets, nuclear receptors are especially closely watched. TR3/Bcl-2 apoptosis pathway is an unique and effective regulation pathways of cancer cells apoptosis with the orphan nuclear receptor TR3 participation. The aim of our study was to isolate the compounds target...