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In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates

Authors
Kim, Mi Kyoung; Park, Kwang-su; Yeo, Woon-Seok; Choo, Hyunah; Chong, Youhoon
Issue Date
2009-02-01
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.17, no.3, pp.1164 - 1171
Abstract
In order to discover a quercetin prodrug with improved bioavailability, we synthesized nine quercetin amion acid conjugates and estimated their pharmacokinetic properties including water solubility, stability against chemical or enzymatic hydrolysis, and cell permeability. Among the synthesized quercetin prodrugs, quercetin-glutamic acid conjugate Qu-E (4g/5g) showed remarkable increases in water solubility, stability, and cell permeability compared with quercetin, which warrants further development as a quercetin prodrug. (c) 2008 Elsevier Ltd. All rights reserved.
Keywords
TANDEM MASS-SPECTROMETRY; INTESTINAL OLIGOPEPTIDE TRANSPORTER; LIQUID-CHROMATOGRAPHY; MODEL PRODRUGS; TRANSEPITHELIAL TRANSPORT; FLAVONOL METABOLITES; DIETARY FLAVONOIDS; BETA-GLUCURONIDASE; HUMAN PLASMA; IDENTIFICATION; TANDEM MASS-SPECTROMETRY; INTESTINAL OLIGOPEPTIDE TRANSPORTER; LIQUID-CHROMATOGRAPHY; MODEL PRODRUGS; TRANSEPITHELIAL TRANSPORT; FLAVONOL METABOLITES; DIETARY FLAVONOIDS; BETA-GLUCURONIDASE; HUMAN PLASMA; IDENTIFICATION; Quercetin; Prodrug; Solubility; Stability; Permeability
ISSN
0968-0896
URI
https://pubs.kist.re.kr/handle/201004/132751
DOI
10.1016/j.bmc.2008.12.043
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KIST Article > 2009
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