title: Furoquinoline Alkaloids from the Leaves of Evodia lepta as Potential Cholinesterase Inhibitors and their Molecular Docking.
abstract: 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.
authors.forename: Jirapast
authors.initials: J
authors.lastname: Sichaem
authors.forename: Thanawan
authors.initials: T
authors.lastname: Rojpitikul
authors.forename: Pattara
authors.initials: P
authors.lastname: Sawasdee
authors.forename: Kiattisak
authors.initials: K
authors.lastname: Lugsannangarm
authors.forename: Tip-pyang
authors.initials: TP
authors.lastname: Santi
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D032086:Evodia / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry* / Q000302:isolation & purification; D018515:Plant Leaves / Q000737:chemistry
chemical_list: D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; D000110:Acetylcholinesterase