Sichaem Jirapast, Rojpitikul Thanawan, Sawasdee Pattara, Lugsannangarm Kiattisak, Santi Tip-pyang
Nat Prod Commun. 2015 Aug;10(8):1359-62.
Nine furoquinoline alkaloids (1-9) were isolated from the leaves of Evodia lepta based on bioassay-guided fractionation and chromatographic techniques. All isolates were evaluated for their cholinesterase (ChEs) inhibitory activities, in which kokusaginine (7) and melineurine (5) exhibited the highest activity toward AChE and BChE, respectively. Lineweaver-Burk plots indicated that 5 and 7 were mixed mode inhibitors of both ChE enzymes. Molecular docking studies on the binding sites of AChE and BChE were performed in order to afford a molecular insight into the mode of action of these active compounds. From this study these compounds have emerged as promising molecules for Alzheimer's disease therapy.
基于生物活性导向分离和色谱技术,从鸦胆子叶中分离出9种呋喃喹啉生物碱(1-9)。对所有分离物进行了胆碱酯酶(ChEs)抑制活性评估,其中吴茱萸次碱(7)和吴茱萸新碱(5)分别对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)表现出最高活性。Lineweaver-Burk图表明5和7是两种胆碱酯酶的混合型抑制剂。为了从分子层面深入了解这些活性化合物的作用模式,对AChE和BChE的结合位点进行了分子对接研究。从这项研究来看,这些化合物有望成为治疗阿尔茨海默病的分子。