title: Cholinesterase inhibitors from the roots of Harpagophytum procumbens.
abstract: Inhibition of cholinesterase has been proposed to be a therapeutic target for the treatment of Alzheimer's diseases. In our preliminary screening study on the acetylcholinesterase (AChE) inhibitory activity, an ethyl acetate soluble fraction of the roots of Harpagophytum procumbens (Pedaliaceae) was found to inhibit AChE activity at the concentration of 100 μg/mL. Ten compounds (1-10) were isolated from the active fraction and evaluated for their inhibitory effect on AChE and butyrylcholinesterase (BChE). Among the isolates, verbascosides (5, 6, and 8) containing a caffeoyl and a 3,4-dihydroxyphenethyl groups in their structures, showed effective AChE inhibitory activity and also possessed BChE inhibitory activity. The findings suggest that verbascoside derivatives may be partially related to the anti-Alzheimer effect of this medicinal plant.
authors.affiliation: College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk, 712-702, Korea.
authors.forename: Yoon Ho
authors.initials: YH
authors.lastname: Bae
authors.forename: To Dao
authors.initials: TD
authors.lastname: Cuong
authors.forename: Tran Manh
authors.initials: TM
authors.lastname: Hung
authors.forename: Jeong Ah
authors.initials: JA
authors.lastname: Kim
authors.forename: Mi Hee
authors.initials: MH
authors.lastname: Woo
authors.forename: Jeong Su
authors.initials: JS
authors.lastname: Byeon
authors.forename: Jae Sue
authors.initials: JS
authors.lastname: Choi
authors.forename: Byung Sun
authors.initials: BS
authors.lastname: Min
mesh_terms: D000085:Acetates / Q000737:chemistry; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002396:Catechols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D005591:Chemical Fractionation; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D004187:Disaccharides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D055808:Drug Discovery; D020834:Ethnopharmacology; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D031684:Harpagophytum / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D055670:Medicine, Korean Traditional; D015394:Molecular Structure; D018697:Nootropic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D009994:Osmolar Concentration; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry; D059808:Polyphenols
chemical_list: D000085:Acetates; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002396:Catechols; D002800:Cholinesterase Inhibitors; D004187:Disaccharides; D005960:Glucosides; D018697:Nootropic Agents; D010636:Phenols; D010936:Plant Extracts; D012997:Solvents; C000597554:decaffeoylverbascoside; C058956:acteoside; D059808:Polyphenols; C064683:isoacteoside; C007650:ethyl acetate