Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands.
The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor that mediates many of the biological and toxicological actions of structurally diverse chemicals. In this study, we examined the ability of a series of ginsenosides extracted from ginseng, a traditional Chinese medicine,...
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2013-01-01
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doaj-c129c5c557bd40f5ab8073812b5b52522020-11-25T01:49:45ZengPublic Library of Science (PLoS)PLoS ONE1932-62032013-01-0186e6625810.1371/journal.pone.0066258Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands.Qin HuGuochun HeJing ZhaoAnatoly SoshilovMichael S DenisonAiqian ZhangHuijun YinDomenico FraccalvieriLaura BonatiQunhui XieBin ZhaoThe aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor that mediates many of the biological and toxicological actions of structurally diverse chemicals. In this study, we examined the ability of a series of ginsenosides extracted from ginseng, a traditional Chinese medicine, to bind to and activate/inhibit the AHR and AHR signal transduction. Utilizing a combination of ligand and DNA binding assays, molecular docking and reporter gene analysis, we demonstrated the ability of selected ginsenosides to directly bind to and activate the guinea pig cytosolic AHR, and to stimulate/inhibit AHR-dependent luciferase gene expression in a recombinant guinea pig cell line. Comparative studies revealed significant species differences in the ability of ginsenosides to stimulate AHR-dependent gene expression in guinea pig, rat, mouse and human cell lines. Not only did selected ginsenosides preferentially activate the AHR from one species and not others, mouse cell line was also significantly less responsive to these chemicals than rat and guinea pig cell lines, but the endogenous gene CYP1A1 could still be inducted in mouse cell line. Overall, the ability of these compounds to stimulate AHR signal transduction demonstrated that these ginsenosides are a new class of naturally occurring AHR agonists.http://europepmc.org/articles/PMC3679084?pdf=render |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Qin Hu Guochun He Jing Zhao Anatoly Soshilov Michael S Denison Aiqian Zhang Huijun Yin Domenico Fraccalvieri Laura Bonati Qunhui Xie Bin Zhao |
spellingShingle |
Qin Hu Guochun He Jing Zhao Anatoly Soshilov Michael S Denison Aiqian Zhang Huijun Yin Domenico Fraccalvieri Laura Bonati Qunhui Xie Bin Zhao Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. PLoS ONE |
author_facet |
Qin Hu Guochun He Jing Zhao Anatoly Soshilov Michael S Denison Aiqian Zhang Huijun Yin Domenico Fraccalvieri Laura Bonati Qunhui Xie Bin Zhao |
author_sort |
Qin Hu |
title |
Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
title_short |
Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
title_full |
Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
title_fullStr |
Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
title_full_unstemmed |
Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
title_sort |
ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands. |
publisher |
Public Library of Science (PLoS) |
series |
PLoS ONE |
issn |
1932-6203 |
publishDate |
2013-01-01 |
description |
The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor that mediates many of the biological and toxicological actions of structurally diverse chemicals. In this study, we examined the ability of a series of ginsenosides extracted from ginseng, a traditional Chinese medicine, to bind to and activate/inhibit the AHR and AHR signal transduction. Utilizing a combination of ligand and DNA binding assays, molecular docking and reporter gene analysis, we demonstrated the ability of selected ginsenosides to directly bind to and activate the guinea pig cytosolic AHR, and to stimulate/inhibit AHR-dependent luciferase gene expression in a recombinant guinea pig cell line. Comparative studies revealed significant species differences in the ability of ginsenosides to stimulate AHR-dependent gene expression in guinea pig, rat, mouse and human cell lines. Not only did selected ginsenosides preferentially activate the AHR from one species and not others, mouse cell line was also significantly less responsive to these chemicals than rat and guinea pig cell lines, but the endogenous gene CYP1A1 could still be inducted in mouse cell line. Overall, the ability of these compounds to stimulate AHR signal transduction demonstrated that these ginsenosides are a new class of naturally occurring AHR agonists. |
url |
http://europepmc.org/articles/PMC3679084?pdf=render |
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