schliessen

Filtern

 

Bibliotheken

Ultrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations

Flavonoids present in food, botanicals, and body fluids occur as complex mixtures, and data on their combinatorial estrogenic effects are sparse. Human cell lines that permanently express estrogen receptor (ER) alpha and ERbeta proteins were developed for the measurement of the global estrogenicity... Full description

Journal Title: Assay and drug development technologies 2007-06, Vol.5 (3), p.355-362
Main Author: Wong, Shih Peng
Other Authors: Li, Jun , Shen, Ping , Gong, Yinhan , Yap, Sook Peng , Yong, Eu Leong
Format: Electronic Article Electronic Article
Language: English
Subjects:
Quelle: Alma/SFX Local Collection
Publisher: United States
ID: ISSN: 1540-658X
Link: https://www.ncbi.nlm.nih.gov/pubmed/17638535
Zum Text:
SendSend as email Add to Book BagAdd to Book Bag
Staff View
recordid: cdi_proquest_miscellaneous_19740532
title: Ultrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations
format: Article
creator:
  • Wong, Shih Peng
  • Li, Jun
  • Shen, Ping
  • Gong, Yinhan
  • Yap, Sook Peng
  • Yong, Eu Leong
subjects:
  • Drug Synergism
  • Drug Therapy, Combination
  • Estrogen Receptor alpha - drug effects
  • Estrogen Receptor beta - drug effects
  • Estrogens - pharmacology
  • Flavonoids - pharmacology
  • Humans
  • Sensitivity and Specificity
  • Structure-Activity Relationship
ispartof: Assay and drug development technologies, 2007-06, Vol.5 (3), p.355-362
description: Flavonoids present in food, botanicals, and body fluids occur as complex mixtures, and data on their combinatorial estrogenic effects are sparse. Human cell lines that permanently express estrogen receptor (ER) alpha and ERbeta proteins were developed for the measurement of the global estrogenicity of flavonoids in such complex mixtures. The presence of estrogenic ligands, known and unknown, in these mixtures can be detected by activation of an ER-driven luciferase reporter gene. We also examined the effect of hydroxylation on the estrogenic activities of four common flavonoids-apigenin, kaempferol, luteolin, and quercetin, alone and in combination. An inverse relationship was observed between the number of hydroxyl groups in flavonoids and ERalpha bioactivity. When submaximal doses of apigenin, luteolin, kaempferol, genistein, and estradiol were combined in binary and higher order mixtures, the experimental estrogenic effects matched those obtained by summing effects extrapolated from dose-response curves of individual compounds. The estrogenic activities of mixtures containing quercetin were observed to deviate from additivity, suggesting that it was a partial agonist/antagonist. Our assay reveals superagonistic, additive, and antagonistic ERalpha or ERbeta actions of flavonoids and adds to our understanding of the estrogenic effects of phytoestrogens in complex mixtures.
language: eng
source: Alma/SFX Local Collection
identifier: ISSN: 1540-658X
fulltext: fulltext
issn:
  • 1540-658X
  • 1557-8127
url: Link


@attributes
NO1
SEARCH_ENGINEprimo_central_multiple_fe
SEARCH_ENGINE_TYPEPrimo Central Search Engine
RANK2.0808501
LOCALfalse
PrimoNMBib
record
control
sourceidproquest_cross
recordidTN_cdi_proquest_miscellaneous_19740532
sourceformatXML
sourcesystemPC
sourcerecordid19740532
originalsourceidFETCH-LOGICAL-c267t-cdb2589c13183457c9c0f7173e410a0a5184499f4f8f9235e2a79ff33dd351a53
addsrcrecordideNpFUctu2zAQJIoWzau3ngueeopcUhRN6RgEaRMgQC4JkJuwIpc2C4lMSNqI_zCfFco2kAsfO7OzjyHkJ2cLztruD5i8qBlTCyaXX8gpl1JVLa_V1_ndsGop2-cTcpbSf8ZqJlTznZxwtRStFPKUvD-NOUJCn1x2W6Qax7EaSsDQwQVICXbUhkjzGumEkDYRJ_SZBktXYxhgpJhyDCv0TlPQRcPl3YzaEbbBB2fo5N5ySUs04hZhdH5FwZh9ucsSK-lOHz7gDUW_Bq9L-Vks-ESdL514iLs9vHarNUYaoimnDtMM7XkX5JuFMeGP431Onv7ePF7fVvcP_-6ur-4rXS9VrrQZatl2mgveikYq3WlmFVcCG86AgeRt03SdbWxru1pIrEF11gphjJAcpDgnvw-6LzG8bkr3_eTSvDXwGDap551qmBR1IV4eiDqGlCLa_iW6qczRc9bPzvXFuX52ri_OFfqvo-5mmNB8ko9WiQ-orpon
sourcetypeAggregation Database
isCDItrue
recordtypearticle
pqid19740532
display
typearticle
titleUltrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations
sourceAlma/SFX Local Collection
creatorWong, Shih Peng ; Li, Jun ; Shen, Ping ; Gong, Yinhan ; Yap, Sook Peng ; Yong, Eu Leong
creatorcontribWong, Shih Peng ; Li, Jun ; Shen, Ping ; Gong, Yinhan ; Yap, Sook Peng ; Yong, Eu Leong
descriptionFlavonoids present in food, botanicals, and body fluids occur as complex mixtures, and data on their combinatorial estrogenic effects are sparse. Human cell lines that permanently express estrogen receptor (ER) alpha and ERbeta proteins were developed for the measurement of the global estrogenicity of flavonoids in such complex mixtures. The presence of estrogenic ligands, known and unknown, in these mixtures can be detected by activation of an ER-driven luciferase reporter gene. We also examined the effect of hydroxylation on the estrogenic activities of four common flavonoids-apigenin, kaempferol, luteolin, and quercetin, alone and in combination. An inverse relationship was observed between the number of hydroxyl groups in flavonoids and ERalpha bioactivity. When submaximal doses of apigenin, luteolin, kaempferol, genistein, and estradiol were combined in binary and higher order mixtures, the experimental estrogenic effects matched those obtained by summing effects extrapolated from dose-response curves of individual compounds. The estrogenic activities of mixtures containing quercetin were observed to deviate from additivity, suggesting that it was a partial agonist/antagonist. Our assay reveals superagonistic, additive, and antagonistic ERalpha or ERbeta actions of flavonoids and adds to our understanding of the estrogenic effects of phytoestrogens in complex mixtures.
identifier
0ISSN: 1540-658X
1EISSN: 1557-8127
2DOI: 10.1089/adt.2007.056
3PMID: 17638535
languageeng
publisherUnited States
subjectDrug Synergism ; Drug Therapy, Combination ; Estrogen Receptor alpha - drug effects ; Estrogen Receptor beta - drug effects ; Estrogens - pharmacology ; Flavonoids - pharmacology ; Humans ; Sensitivity and Specificity ; Structure-Activity Relationship
ispartofAssay and drug development technologies, 2007-06, Vol.5 (3), p.355-362
lds50peer_reviewed
citesFETCH-LOGICAL-c267t-cdb2589c13183457c9c0f7173e410a0a5184499f4f8f9235e2a79ff33dd351a53
links
openurl$$Topenurl_article
openurlfulltext$$Topenurlfull_article
thumbnail$$Usyndetics_thumb_exl
backlink$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17638535$$D View this record in MEDLINE/PubMed
search
creatorcontrib
0Wong, Shih Peng
1Li, Jun
2Shen, Ping
3Gong, Yinhan
4Yap, Sook Peng
5Yong, Eu Leong
title
0Ultrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations
1Assay and drug development technologies
addtitleAssay Drug Dev Technol
descriptionFlavonoids present in food, botanicals, and body fluids occur as complex mixtures, and data on their combinatorial estrogenic effects are sparse. Human cell lines that permanently express estrogen receptor (ER) alpha and ERbeta proteins were developed for the measurement of the global estrogenicity of flavonoids in such complex mixtures. The presence of estrogenic ligands, known and unknown, in these mixtures can be detected by activation of an ER-driven luciferase reporter gene. We also examined the effect of hydroxylation on the estrogenic activities of four common flavonoids-apigenin, kaempferol, luteolin, and quercetin, alone and in combination. An inverse relationship was observed between the number of hydroxyl groups in flavonoids and ERalpha bioactivity. When submaximal doses of apigenin, luteolin, kaempferol, genistein, and estradiol were combined in binary and higher order mixtures, the experimental estrogenic effects matched those obtained by summing effects extrapolated from dose-response curves of individual compounds. The estrogenic activities of mixtures containing quercetin were observed to deviate from additivity, suggesting that it was a partial agonist/antagonist. Our assay reveals superagonistic, additive, and antagonistic ERalpha or ERbeta actions of flavonoids and adds to our understanding of the estrogenic effects of phytoestrogens in complex mixtures.
subject
0Drug Synergism
1Drug Therapy, Combination
2Estrogen Receptor alpha - drug effects
3Estrogen Receptor beta - drug effects
4Estrogens - pharmacology
5Flavonoids - pharmacology
6Humans
7Sensitivity and Specificity
8Structure-Activity Relationship
issn
01540-658X
11557-8127
fulltexttrue
rsrctypearticle
creationdate2007
recordtypearticle
recordideNpFUctu2zAQJIoWzau3ngueeopcUhRN6RgEaRMgQC4JkJuwIpc2C4lMSNqI_zCfFco2kAsfO7OzjyHkJ2cLztruD5i8qBlTCyaXX8gpl1JVLa_V1_ndsGop2-cTcpbSf8ZqJlTznZxwtRStFPKUvD-NOUJCn1x2W6Qax7EaSsDQwQVICXbUhkjzGumEkDYRJ_SZBktXYxhgpJhyDCv0TlPQRcPl3YzaEbbBB2fo5N5ySUs04hZhdH5FwZh9ucsSK-lOHz7gDUW_Bq9L-Vks-ESdL514iLs9vHarNUYaoimnDtMM7XkX5JuFMeGP431Onv7ePF7fVvcP_-6ur-4rXS9VrrQZatl2mgveikYq3WlmFVcCG86AgeRt03SdbWxru1pIrEF11gphjJAcpDgnvw-6LzG8bkr3_eTSvDXwGDap551qmBR1IV4eiDqGlCLa_iW6qczRc9bPzvXFuX52ri_OFfqvo-5mmNB8ko9WiQ-orpon
startdate200706
enddate200706
creator
0Wong, Shih Peng
1Li, Jun
2Shen, Ping
3Gong, Yinhan
4Yap, Sook Peng
5Yong, Eu Leong
scope
0CGR
1CUY
2CVF
3ECM
4EIF
5NPM
6AAYXX
7CITATION
87QO
98FD
10FR3
11P64
sort
creationdate200706
titleUltrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations
authorWong, Shih Peng ; Li, Jun ; Shen, Ping ; Gong, Yinhan ; Yap, Sook Peng ; Yong, Eu Leong
facets
frbrtype5
frbrgroupidcdi_FETCH-LOGICAL-c267t-cdb2589c13183457c9c0f7173e410a0a5184499f4f8f9235e2a79ff33dd351a53
rsrctypearticles
prefilterarticles
languageeng
creationdate2007
topic
0Drug Synergism
1Drug Therapy, Combination
2Estrogen Receptor alpha - drug effects
3Estrogen Receptor beta - drug effects
4Estrogens - pharmacology
5Flavonoids - pharmacology
6Humans
7Sensitivity and Specificity
8Structure-Activity Relationship
toplevel
0peer_reviewed
1online_resources
creatorcontrib
0Wong, Shih Peng
1Li, Jun
2Shen, Ping
3Gong, Yinhan
4Yap, Sook Peng
5Yong, Eu Leong
collection
0Medline
1MEDLINE
2MEDLINE (Ovid)
3MEDLINE
4MEDLINE
5PubMed
6CrossRef
7Biotechnology Research Abstracts
8Technology Research Database
9Engineering Research Database
10Biotechnology and BioEngineering Abstracts
jtitleAssay and drug development technologies
delivery
delcategoryRemote Search Resource
fulltextfulltext
addata
au
0Wong, Shih Peng
1Li, Jun
2Shen, Ping
3Gong, Yinhan
4Yap, Sook Peng
5Yong, Eu Leong
formatjournal
genrearticle
ristypeJOUR
atitleUltrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations
jtitleAssay and drug development technologies
addtitleAssay Drug Dev Technol
date2007-06
risdate2007
volume5
issue3
spage355
epage362
pages355-362
issn1540-658X
eissn1557-8127
abstractFlavonoids present in food, botanicals, and body fluids occur as complex mixtures, and data on their combinatorial estrogenic effects are sparse. Human cell lines that permanently express estrogen receptor (ER) alpha and ERbeta proteins were developed for the measurement of the global estrogenicity of flavonoids in such complex mixtures. The presence of estrogenic ligands, known and unknown, in these mixtures can be detected by activation of an ER-driven luciferase reporter gene. We also examined the effect of hydroxylation on the estrogenic activities of four common flavonoids-apigenin, kaempferol, luteolin, and quercetin, alone and in combination. An inverse relationship was observed between the number of hydroxyl groups in flavonoids and ERalpha bioactivity. When submaximal doses of apigenin, luteolin, kaempferol, genistein, and estradiol were combined in binary and higher order mixtures, the experimental estrogenic effects matched those obtained by summing effects extrapolated from dose-response curves of individual compounds. The estrogenic activities of mixtures containing quercetin were observed to deviate from additivity, suggesting that it was a partial agonist/antagonist. Our assay reveals superagonistic, additive, and antagonistic ERalpha or ERbeta actions of flavonoids and adds to our understanding of the estrogenic effects of phytoestrogens in complex mixtures.
copUnited States
pmid17638535
doi10.1089/adt.2007.056