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Does the relationship of procyanidin and proanthocyanidin in grape powder to cholinesterase inhibition differ in human plasma?
In a recent study, grape extract containing procyanidins of varying size was evaluated for its ability to inhibit butyrylcholinesterase (BuChE) and plasma butyrylcholinesterase (pBuChE) using the Ellman assay. The aim of this study was to determine the contribution of different procyanidin oligomers to the overall inhibition of BuChE and pBuChE and whether this is related to differences in molecular weight or degree of polymerisation. Freshly prepared grape powder was extracted in 50% MeOH/0.1% HCl and then fractionated using size exclusion chromatography. Analytical HPLC and mass spectrometry were used to identify the oligomers present. The inhibitory capacity of the fractions against pBuChE and BuChE was measured using a spectrophotometric method. The fractions containing procyanidins were then analysed by mass spectrometry to determine their molecular weights. Both the percentage of procyanidin oligomers and the degree of polymerisation significantly affected the inhibition of both BuChE and pBuChE, whereas the differences in molecular weight had no significant effect. Sixty-one of the 72 procyanidin oligomer fractions inhibited pBuChE and BuChE with IC50 values ranging between 0.5 and 30 μM. The IC50 values of low-Mw procyanidins (DP1-DP2) with a degree of polymerisation (DP) of up to 4 were similar to
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