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Oxyresveratrol Is a Phytoestrogen Exerting Anti-inflammatory Effects Through NF-κB and Estrogen Receptor Signaling

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Abstract

Recent studies suggest an anti-inflammatory activity of oxyresveratrol, a stilbene extracted from Cortex mori root used in traditional Chinese medicine that also presents estrogen-like activity. We herein tested the hypothesis that oxyreservatrol exerts an anti-inflammatory effect through its estrogenic-like function. In MCF-7 cells, oxyresveratrol significantly induced proliferation, which was accompanied with estrogen receptor (ER)-mediated transcriptional activation, increased estrogen-targeted gene expression (e.g., pS2, PGR, and CTSD), and increased ERα/β proteins. The estrogen-like effect of oxyresveratrol was reversed by the ER inhibitor ICI 182780. Strong ER-binding activities of oxyresveratrol were revealed by negative docking scores. The LPS-induced inflammatory response (e.g., upregulated IκB-α phosphorylation, NF-κB nuclear translocation, and cytokine messenger RNA expression) was significantly suppressed in an ER-dependent manner by oxyresveratrol in RAW264.7 cells. These results suggest that oxyresveratrol may function as an ER agonist and modulate NF-κB signaling.

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ACKNOWLEDGEMENTS

This work was supported by State Key Program of National Natural Science Foundation of China (81630106), National Key Basic Research Program of China (973 Program) (No.2012CB518404), and Ministry of Education of Republic of China “Program for Innovative Research Team in University” (IRT-16R54).

We also thank Zemin Yao and Jiachen Sun for assistance with the experiments.

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Correspondence to Xiu-Mei Gao or Guan-Wei Fan.

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Wei, J., Chen, JR., Pais, E.M.A. et al. Oxyresveratrol Is a Phytoestrogen Exerting Anti-inflammatory Effects Through NF-κB and Estrogen Receptor Signaling. Inflammation 40, 1285–1296 (2017). https://doi.org/10.1007/s10753-017-0572-y

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  • DOI: https://doi.org/10.1007/s10753-017-0572-y

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