补骨脂素通过雌激素受体信号通路对人牙周膜细胞的抗炎活性。
Anti-inflammatory activity of psoralen in human periodontal ligament cells via estrogen receptor signaling pathway.
机构信息
Department of Periodontology, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200011, China.
College of Stomatology, Shanghai Jiao Tong University; National Center for Stomatology; National Clinical Research Center for Oral Diseases; Shanghai Key Laboratory of Stomatology; Research Unit of Oral and Maxillofacial Regenerative Medicine, Chinese Academy of Medical Sciences, Shanghai, 200011, China.
出版信息
Sci Rep. 2021 Apr 22;11(1):8754. doi: 10.1038/s41598-021-85145-1.
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.
补骨脂素是从中药补骨脂中提取的最有效的成分之一。研究发现，补骨脂素具有抗炎和类雌激素作用；然而，对于这些作用的机制研究甚少。通过分子对接试验，发现补骨脂素与 ERα 的结合优于 ERβ。在人牙周韧带细胞中，补骨脂素可上调雌激素靶基因（如 CTSD、PGR、TFF1），并下调 P. gingivalis LPS 刺激的炎症细胞因子（TNF-α、IL-1β、IL-6 和 IL-8）的表达，同时下调 TLR4-IRAK4-NF-κb 信号通路蛋白。这些作用可被 ER 拮抗剂 ICI 182780 逆转。这些结果表明，补骨脂素可能作为 ER 的激动剂发挥抗炎作用，这可为补骨脂素用于辅助治疗和预防牙周炎提供理论依据。
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