eFood

Volume 1, Issue 6, December 2020, Pages 392 - 398

In vitro Anti-Inflammatory Potency of Sanguinarine and Chelerythrine via Interaction with Glucocorticoid Receptor

Authors
Jie Zhang, Yuan Liang, Li Ren*, Tiehua Zhang*
College of Food Science and Engineering, Jilin University, Changchun 130062, China
*Corresponding authors. Email: liren77@jlu.edu.cn; zhangthjlu@163.com
Corresponding Author
Li Ren
Received 13 December 2020, Accepted 13 January 2021, Available Online 21 January 2021.
DOI
https://doi.org/10.2991/efood.k.210118.001How to use a DOI?
Keywords
Anti-inflammatory potency, sanguinarine, chelerythrine, glucocorticoid receptor
Abstract

As quaternary benzo[c]phenanthridine alkaloids, sanguinarine and chelerythrine possess multiple biological activities including anti-inflammatory effects. They have been confirmed to regulate gene expression of inflammatory-related cytokines at transcription level. This work aims to investigate the glucocorticoid-like anti-inflammatory effects of sanguinarine and chelerythrine, which may be mediated by Glucocorticoid Receptor (GR). Firstly, the interactions of GR with sanguinarine and chelerythrine were investigated by fluorescence polarization assay and the result showed that these two alkaloids could bind to GR with potent affinities. Luciferase reporter assay showed that sanguinarine was a weak GR agonist but chelerythrine failed to induce GR transcriptional activation in HeLa cells. These two alkaloids at high concentration showed similar tumor necrosis factor-α inhibitory potency to dexamethasone in RAW 264.7 cells, indicating their anti-inflammatory effects in vitro. In addition, the results of molecular docking and dynamics simulations showed that sanguinarine and chelerythrine could bind effectively with GR and might serve as its functional ligands. In conclusion, chelerythrine was speculated to be a selective GR modulator that might exhibit GR-mediated beneficial actions with reduced side effects.

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Copyright
© 2021 The Authors. Publishing services by Atlantis Press International B.V.
Open Access
This is an open access article distributed under the CC BY-NC 4.0 license (http://creativecommons.org/licenses/by-nc/4.0/).

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Journal
eFood
Volume-Issue
1 - 6
Pages
392 - 398
Publication Date
2021/01
ISSN (Online)
2666-3066
DOI
https://doi.org/10.2991/efood.k.210118.001How to use a DOI?
Copyright
© 2021 The Authors. Publishing services by Atlantis Press International B.V.
Open Access
This is an open access article distributed under the CC BY-NC 4.0 license (http://creativecommons.org/licenses/by-nc/4.0/).

Cite this article

TY  - JOUR
AU  - Jie Zhang
AU  - Yuan Liang
AU  - Li Ren
AU  - Tiehua Zhang
PY  - 2021
DA  - 2021/01
TI  - In vitro Anti-Inflammatory Potency of Sanguinarine and Chelerythrine via Interaction with Glucocorticoid Receptor
JO  - eFood
SP  - 392
EP  - 398
VL  - 1
IS  - 6
SN  - 2666-3066
UR  - https://doi.org/10.2991/efood.k.210118.001
DO  - https://doi.org/10.2991/efood.k.210118.001
ID  - Zhang2021
ER  -