Abstract

Psoralen is one of the most effective ingredients extracted from the Chinese herb, Psoralea corylifolia L. Studies have found that psoralen has anti-inflammatory and estrogen-like effects; however, little research has been conducted to elucidate the mechanisms underlying these effects. Through the molecule docking assay, psoralen was found to have a better combination with ERα than ERβ. In human periodontal ligament cells, psoralen was found to upregulate the estrogen target genes (e.g., CTSD, PGR, TFF1) and down-regulate the expression of inflammatory cytokines (TNF-α, IL-1β, IL-6 and IL-8) stimulated by P. gingivalis LPS, as well as TLR4-IRAK4-NF-κb signaling pathway proteins. These effects were reversed by the ER antagonist ICI 182780. These results indicated that psoralen may exert anti-inflammatory effects as an agonist to ER, which could provide a theoretical basis for the use of psoralen for adjuvant therapy and prevention of periodontitis.

Highlights

  • Psoralen is one of the most effective ingredients extracted from the Chinese herb, Psoralea corylifolia L

  • Psoralen was docked into the pocket bound to the ER-α ligand. By analyzing their binding mode, we found that the binding of psoralen to estrogen receptor α (ERα) was similar to estradiol

  • The results showed that psoralen could reduce the protein levels of inflammatory cytokines (TNF-α, IL-1β, IL-8, and IL-6), which could be reversed by the ER antagonist

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Summary

Introduction

Psoralen is one of the most effective ingredients extracted from the Chinese herb, Psoralea corylifolia L. In human periodontal ligament cells, psoralen was found to upregulate the estrogen target genes (e.g., CTSD, PGR, TFF1) and down-regulate the expression of inflammatory cytokines (TNF-α, IL-1β, IL-6 and IL-8) stimulated by P. gingivalis LPS, as well as TLR4-IRAK4-NF-κb signaling pathway proteins. These effects were reversed by the ER antagonist ICI 182780. During the treatment of periodontal disease, severer resorption of alveolar bone is observed in those osteoporotic patients, which increases the risk of tooth l­oss[17]. During the development of periodontitis, estrogen plays a pivotal role in preventing the resorption of alveolar bone and modulating inflammatory mediators

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