School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China; Tang Center of Herbal Medicine Research and Department of Anesthesia & Critical Care, University of Chicago, Chicago, IL 60637, United States.
Phytomedicine. 2019 Oct;63:153036. doi: 10.1016/j.phymed.2019.153036. Epub 2019 Aug 1.
Genkwanin is a flavone isolated from the traditional Chinese herb Daphne genkwa. Our previous work proved that four flavonoids (including genkwanin) isolated from D. genkwa (FFD) significantly improved the symptoms of arthritis in rat models. Recent studies have revealed that genkwanin exhibited anti-inflammatory and immunomodulatory activities, both of which were closely related to the pathology of rheumatoid arthritis (RA). Therefore, studying the anti-RA effects and mechanisms of genkwanin may give us insight into FFD's therapeutic effects on RA.
This study aimed to investigate the anti-rheumatoid arthritis activity of genkwanin on adjuvant-induced arthritis (AIA) model in rats and explore the underlying mechanisms.
The anti-rheumatoid arthritis activity of genkwanin was evaluated on AIA rat model by determining the paw swelling degrees and arthritis index scores, along with histopathological analysis of joint tissues. The serum cytokine levels were measured by ELISA method, and serum NO levels were measured by Griess method. The expression and phosphorylation levels of proteins in JAK/STAT and NF-κB signaling pathways were determined by western blot analysis and immunohistochemistry analysis.
Genkwanin significantly decreased the paw swelling and arthritis index in AIA rats and also decreased the inflammation and bone destruction in joint tissues. The serum TNF-α, IL-6, and NO concentrations were markedly reduced while the IL-10 concentration was markedly increased with the treatment of genkwanin. Genkwanin inhibited the activation of JAK/STAT and NF-κB signaling pathways in synovial tissues of AIA rats.
Genkwanin exerted anti-rheumatoid arthritis effects on AIA rats through inhibiting the activation of JAK/STAT and NF-κB signaling pathways. The results obtained in this work lead us to suggest that Genkwanin could play a crucial role on the previously demonstrated anti-rheumatoid arthritis activity of flavonoid extract of D. genkwa (namely FFD).
根皮素是从传统中药芫花中分离得到的一种黄酮类化合物。我们之前的工作证明，芫花（FFD）中分离得到的四种黄酮类化合物（包括根皮素）可显著改善关节炎大鼠模型的症状。最近的研究表明，根皮素具有抗炎和免疫调节作用，这两者都与类风湿关节炎（RA）的病理密切相关。因此，研究根皮素的抗 RA 作用及其机制可能使我们深入了解 FFD 对 RA 的治疗作用。
本研究旨在探讨根皮素对佐剂诱导关节炎（AIA）大鼠模型的抗类风湿关节炎活性，并探讨其潜在机制。
通过测定爪肿胀度和关节炎指数评分以及关节组织的组织病理学分析，评估根皮素对 AIA 大鼠模型的抗类风湿关节炎活性。采用 ELISA 法测定血清细胞因子水平，Griess 法测定血清 NO 水平。采用 Western blot 分析和免疫组化分析测定 JAK/STAT 和 NF-κB 信号通路中蛋白的表达和磷酸化水平。
根皮素可显著降低 AIA 大鼠的爪肿胀度和关节炎指数，减轻关节组织的炎症和骨破坏。根皮素治疗可显著降低血清 TNF-α、IL-6 和 NO 浓度，增加 IL-10 浓度。根皮素抑制 AIA 大鼠滑膜组织中 JAK/STAT 和 NF-κB 信号通路的激活。
根皮素通过抑制 JAK/STAT 和 NF-κB 信号通路的激活，对 AIA 大鼠发挥抗类风湿关节炎作用。本工作的结果表明，根皮素可能在先前证明的芫花（FFD）的抗类风湿关节炎活性中发挥重要作用。
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