Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands

Qin Hu, Guochun He, Jing Zhao, Anatoly Soshilov, Michael S. Denison, Aiqian Zhang, Huijun Yin, Domenico Fraccalvieri, Laura Bonati, Qunhui Xie, Bin Zhao

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Article numbere66258
JournalPLoS One
Volume8
Issue number6
DOIs
StatePublished - Jun 11 2013

Fingerprint

Ginsenosides
Aryl Hydrocarbon Receptors
hydrocarbons
Ligands
receptors
guinea pigs
Cells
Guinea Pigs
Cell Line
cell lines
Signal transduction
Gene expression
signal transduction
Rats
Signal Transduction
mice
Genes
Gene Expression
ginsenosides
ligands

ASJC Scopus subject areas

  • Agricultural and Biological Sciences(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Medicine(all)

Cite this

Hu, Q., He, G., Zhao, J., Soshilov, A., Denison, M. S., Zhang, A., ... Zhao, B. (2013). Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands. PLoS One, 8(6), [e66258]. https://doi.org/10.1371/journal.pone.0066258

Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands. / Hu, Qin; He, Guochun; Zhao, Jing; Soshilov, Anatoly; Denison, Michael S.; Zhang, Aiqian; Yin, Huijun; Fraccalvieri, Domenico; Bonati, Laura; Xie, Qunhui; Zhao, Bin.

In: PLoS One, Vol. 8, No. 6, e66258, 11.06.2013.

Research output: Contribution to journalArticle

Hu, Q, He, G, Zhao, J, Soshilov, A, Denison, MS, Zhang, A, Yin, H, Fraccalvieri, D, Bonati, L, Xie, Q & Zhao, B 2013, 'Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands', PLoS One, vol. 8, no. 6, e66258. https://doi.org/10.1371/journal.pone.0066258
Hu Q, He G, Zhao J, Soshilov A, Denison MS, Zhang A et al. Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands. PLoS One. 2013 Jun 11;8(6). e66258. https://doi.org/10.1371/journal.pone.0066258
Hu, Qin ; He, Guochun ; Zhao, Jing ; Soshilov, Anatoly ; Denison, Michael S. ; Zhang, Aiqian ; Yin, Huijun ; Fraccalvieri, Domenico ; Bonati, Laura ; Xie, Qunhui ; Zhao, Bin. / Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands. In: PLoS One. 2013 ; Vol. 8, No. 6.
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