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Bioavailability of gallic acid and catechins from neuroprotective grape seed extract is improved by repeated dosing in rats
Author(s) -
Lobo Jessica Kathleen,
Ferruzzi Mario G,
Janle Elsa M,
Whittaker Naomi,
Cooper Bruce R,
Weaver Connie M,
Simon James E,
Wu QingLi,
Welch Cara,
Ho Lap,
Pasinetti Giulio M
Publication year - 2009
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.23.1_supplement.104.4
Subject(s) - grape seed extract , bioavailability , catechin , gallic acid , neuroprotection , chemistry , pharmacology , proanthocyanidin , pharmacokinetics , food science , biochemistry , polyphenol , medicine , antioxidant , alternative medicine , pathology
Grape Seed Extract (GSE), a rich source of biologically active phenolic acids and proanthocyanidins (PAC's), has demonstrated neuroprotective activities consistent with prevention of Alzheimer disease (AD). To understand how specific GSE components are absorbed, the impact of acute and repeated GSE exposure on bioavailability and brain deposition of major phenolics was investigated. Rats were pre‐treated with GSE acutely and in dose‐escalation from 50 to 150 mg/kg BW over 10 d prior to assessment of pharmacokinetic response. LC‐MS identified gallic acid (GA), catechin (C), epicatechin (EC) in plasma of rats gavaged with GSE. Additionally, 4‐methylgallic acid (4‐OMeGA), 3′‐methytlcatechin (3′‐OMeC) and 3′‐methylepicatechin (3′‐OMeEC) were identified as circulating metabolites of GSE phenolics. Repeated daily exposure to GSE was found to significantly increase bioavailability relative to animals receiving a single acute GSE dose. EC and C were not detectable in brain tissues of rats receiving a single GSE dose but reached levels of 290.7±45.9 and 576.7±227.7 pg/g respectively in brain of rats administered GSE for 10 d. These results suggest that GA, C and EC are readily absorbed and metabolized from acute doses of GSE and that plasma response and brain deposition of these neuroprotective phenolic compounds may be enhanced by repeated dosing. Supported by NIH‐NCCAM grant P01AT004511‐01.