Inhibitory effect of verbascoside isolated from Buddleja brasiliensis Jacq. ex Spreng on prolyl oligopeptidase activity

Phytother Res. 2012 Oct;26(10):1472-5. doi: 10.1002/ptr.4597. Epub 2012 Jan 25.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Buddleja / chemistry*
  • Chemical Fractionation
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / isolation & purification
  • Dipeptidyl-Peptidase IV Inhibitors / chemistry
  • Dipeptidyl-Peptidase IV Inhibitors / isolation & purification
  • Glucosides / chemistry*
  • Glucosides / isolation & purification
  • Inhibitory Concentration 50
  • Phenols / chemistry*
  • Phenols / isolation & purification
  • Plant Extracts / chemistry
  • Prolyl Oligopeptidases
  • Serine Endopeptidases / chemistry*
  • Serine Proteinase Inhibitors / chemistry*
  • Serine Proteinase Inhibitors / isolation & purification

Substances

  • Cholinesterase Inhibitors
  • Dipeptidyl-Peptidase IV Inhibitors
  • Glucosides
  • Phenols
  • Plant Extracts
  • Serine Proteinase Inhibitors
  • acteoside
  • Serine Endopeptidases
  • Prolyl Oligopeptidases