Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, China.
Key Laboratory of Pharmacology of Traditional Chinese Medicine Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, #312 Anshanxi Road, Nankai District, Tianjin, 300193, China.
Inflammation. 2017 Aug;40(4):1285-1296. doi: 10.1007/s10753-017-0572-y.
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.
最近的研究表明，白藜芦醇具有抗炎活性，白藜芦醇是从传统中药桑白皮中提取的一种二苯乙烯，也具有类雌激素活性。我们在此假设白藜芦醇通过其类雌激素功能发挥抗炎作用。在 MCF-7 细胞中，白藜芦醇显著诱导增殖，这伴随着雌激素受体 (ER) 介导的转录激活、增加雌激素靶向基因表达（例如 pS2、PGR 和 CTSD）以及增加 ERα/β 蛋白。白藜芦醇的类雌激素作用被 ER 抑制剂 ICI 182780 逆转。通过负对接评分揭示了白藜芦醇与 ER 结合的强烈活性。白藜芦醇在 RAW264.7 细胞中以 ER 依赖性方式显著抑制 LPS 诱导的炎症反应（例如，上调 IκB-α 磷酸化、NF-κB 核易位和细胞因子信使 RNA 表达）。这些结果表明，白藜芦醇可能作为 ER 激动剂发挥作用并调节 NF-κB 信号。
