Abstract:
:We report the development of a chemical modification method of general applicability to polyphenols, which increases solubility to influence absorption. Glucosyl groups were added to the resveratrol kernel via a succinate linker, yielding 3,4',5-tri-(alpha-D-glucose-3-O-succinyl) resveratrol. The construct was only slowly hydrolyzed in acid and at pH 6.8, but it was destroyed by blood esterases in less than 1h. In rats its administration resulted in a blood concentration versus time curve shifted to longer times in comparison to resveratrol, a useful modulation of pharmacokinetics. The area-under-curve parameter and the metabolite mix were similar to those of resveratrol. The method may be advantageously employed to solubilize other polyphenols and to make them more palatable.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Biasutto L,Marotta E,Bradaschia A,Fallica M,Mattarei A,Garbisa S,Zoratti M,Paradisi Cdoi
10.1016/j.bmcl.2009.09.114subject
Has Abstractpub_date
2009-12-01 00:00:00pages
6721-4issue
23eissn
0960-894Xissn
1464-3405pii
S0960-894X(09)01382-1journal_volume
19pub_type
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