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

Mi Kyoung Kim; Kwang su Park; Woon seok Yeo; Hyunah Choo; Youhoon Chong

doi:10.1016/j.bmc.2008.12.043

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

Mi Kyoung Kim
, Kwang su Park
, Woon seok Yeo
, Hyunah Choo
, Youhoon Chong

Research output: Contribution to journal › Article › peer-review

138 Scopus citations

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.

Original language	English
Pages (from-to)	1164-1171
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	3
DOIs	https://doi.org/10.1016/j.bmc.2008.12.043
State	Published - 1 Feb 2009
Externally published	Yes

Keywords

Permeability
Prodrug
Quercetin
Solubility
Stability

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10.1016/j.bmc.2008.12.043

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

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.",

keywords = "Permeability, Prodrug, Quercetin, Solubility, Stability",

author = "Kim, \{Mi Kyoung\} and Park, \{Kwang su\} and Yeo, \{Woon seok\} and Hyunah Choo and Youhoon Chong",

note = "Funding Information: This work was supported by grant KRF-2007-313-C00476 from the Korea Research Foundation, Republic of Korea (MOEHRD, Basic Research Promotion Fund) and by grants from Biogreen 21 (Korea Ministry of Agriculture and Forestry), and the second Brain Korea 21 (Korea Ministry of Education). KSP is supported by the second Brain Korea 21.",

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doi = "10.1016/j.bmc.2008.12.043",

language = "English",

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pages = "1164--1171",

journal = "Bioorganic and Medicinal Chemistry",

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TY - JOUR

T1 - In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates

AU - Kim, Mi Kyoung

AU - Park, Kwang su

AU - Yeo, Woon seok

AU - Choo, Hyunah

AU - Chong, Youhoon

N1 - Funding Information: This work was supported by grant KRF-2007-313-C00476 from the Korea Research Foundation, Republic of Korea (MOEHRD, Basic Research Promotion Fund) and by grants from Biogreen 21 (Korea Ministry of Agriculture and Forestry), and the second Brain Korea 21 (Korea Ministry of Education). KSP is supported by the second Brain Korea 21.

PY - 2009/2/1

Y1 - 2009/2/1

N2 - 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.

AB - 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.

KW - Permeability

KW - Prodrug

KW - Quercetin

KW - Solubility

KW - Stability

UR - https://www.scopus.com/pages/publications/58949103807

U2 - 10.1016/j.bmc.2008.12.043

DO - 10.1016/j.bmc.2008.12.043

M3 - Article

C2 - 19128975

AN - SCOPUS:58949103807

SN - 0968-0896

VL - 17

SP - 1164

EP - 1171

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 3

ER -

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

Abstract

Keywords

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