title: Inhibitory effect of verbascoside isolated from Buddleja brasiliensis Jacq. ex Spreng on prolyl oligopeptidase activity.
abstract: The phenylpropanoid glycoside verbascoside [2-(3,4-dihydroxyphenylethyl)-1-O-α-L-rhamnopyranosyl-(1→3)-β-D-(4-O-caffeyl)-glucopyranoside] (1) has been isolated as the main constituent of the crude extract of Buddleja brasiliensis Jacq. ex Spreng from Southern Brazil. The crude extract, main fractions and the compound 1 were evaluated for inhibition of the enzymes acetylcholinesterase (AChE), dipeptidyl peptidase-IV (DPP-IV) and prolyl oligopeptidase (POP). Compound 1 showed weak activity against DPP-IV with an IC(50) >> 150 µM and was inactive against AChE, with a pMIQ determined by bioautography of 9.6. In contrast, 1 displayed significant inhibition of POP in a dose-dependent manner with an IC(50) value of 1.3 ± 0.2 µM, similar to the positive control, baicalin, with a POP IC(50) of 12 ± 3 µM.
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais NPPN, Departamento de Química, Universidade Federal de Santa Maria, Santa Maria RS, Brazil.
authors.forename: Augusto G
authors.initials: AG
authors.lastname: Filho
authors.forename: Ademir F
authors.initials: AF
authors.lastname: Morel
authors.forename: Luciana
authors.initials: L
authors.lastname: Adolpho
authors.forename: Vinícius
authors.initials: V
authors.lastname: Ilha
authors.forename: Ernest
authors.initials: E
authors.lastname: Giralt
authors.forename: Teresa
authors.initials: T
authors.lastname: Tarragó
authors.forename: Ionara I
authors.initials: II
authors.lastname: Dalcol
mesh_terms: D032861:Buddleja / Q000737:chemistry*; D005591:Chemical Fractionation; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000737:chemistry / Q000302:isolation & purification; D005960:Glucosides / Q000737:chemistry* / Q000302:isolation & purification; D020128:Inhibitory Concentration 50; D010636:Phenols / Q000737:chemistry* / Q000302:isolation & purification; D010936:Plant Extracts / Q000737:chemistry; D000085822:Prolyl Oligopeptidases; D012697:Serine Endopeptidases / Q000737:chemistry*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D059808:Polyphenols
chemical_list: D002800:Cholinesterase Inhibitors; D054873:Dipeptidyl-Peptidase IV Inhibitors; D005960:Glucosides; D010636:Phenols; D010936:Plant Extracts; D000085822:Prolyl Oligopeptidases; D012697:Serine Endopeptidases; D015842:Serine Proteinase Inhibitors; C058956:acteoside; D059808:Polyphenols