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

被引：118

作者：

Kim, Mi Kyoung ^{[1
]}

Park, Kwang-su ^{[1
]}

Yeo, Woon-Seok ^{[1
]}

Choo, Hyunah ^{[2
]}

Chong, Youhoon ^{[1
]}

机构：

[1] Konkuk Univ, Dept Biosci & Biotechnol, Seoul 143701, South Korea

[2] Korea Inst Sci & Technol, Div Life Sci, Seoul 130650, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 03期

关键词：

Quercetin; Prodrug; Solubility; Stability; Permeability; INTESTINAL OLIGOPEPTIDE TRANSPORTER; LIQUID-CHROMATOGRAPHY; MODEL PRODRUGS; TRANSEPITHELIAL TRANSPORT; FLAVONOL METABOLITES; DIETARY FLAVONOIDS; HUMAN PLASMA; IDENTIFICATION; CELLS; PHARMACOKINETICS;

D O I：

10.1016/j.bmc.2008.12.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1164 / 1171

页数：8

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