Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China.
Molecules. 2021 Dec 23;27(1):78. doi: 10.3390/molecules27010078.
has been used as a Yao folk medicine to treat arthritis for years in China, although its active anti-arthritic moieties have not been clarified so far. In this study, two natural phenolic diterpenoids with anti-rheumatoid arthritis (RA) effects, rosmanol and carnosol, isolated from the medicinal plant were reported on for the first time. In type II collagen-induced arthritis DBA/1 mice, both rosmanol (40 mg/kg/d) and carnosol (40 mg/kg/d) alone alleviated the RA symptoms, such as swelling, redness, and synovitis; decreased the arthritis index score; and downregulated the serum pro-inflammatory cytokine levels of interleukin 6 (IL-6), monocyte chemotactic protein 1 (MCP-1), and tumor necrosis factor α (TNF-α). Additionally, they blocked the activation of the Toll-like receptor 4 (TLR4)/nuclear factor κB (NF-κB)/c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) pathways. Of particular interest was that when they were used in combination (20 mg/kg/d each), the anti-RA effect and inhibitory activity on the TLR4/NF-κB/MAPK pathway were significantly enhanced. The results demonstrated that rosmanol and carnosol synergistically alleviated RA by inhibiting inflammation through regulating the TLR4/NF-κB/MAPK pathway, meaning they have the potential to be developed into novel, safe natural combinations for the treatment of RA.
在中国，元宝枫已被用作治疗关节炎的瑶药多年，但迄今为止，其具有抗炎活性的成分仍未得到阐明。本研究首次报道了从药用植物元宝枫中分离得到的两种具有抗类风湿关节炎（RA）作用的天然酚类二萜化合物——罗斯曼醇和卡诺醇。在Ⅱ型胶原诱导的关节炎 DBA/1 小鼠中，单独使用罗斯曼醇（40mg/kg/d）和卡诺醇（40mg/kg/d）均可缓解 RA 症状，如肿胀、发红和滑膜炎；降低关节炎指数评分；下调血清促炎细胞因子白细胞介素 6（IL-6）、单核细胞趋化蛋白 1（MCP-1）和肿瘤坏死因子 α（TNF-α）水平。此外，它们还阻断了 Toll 样受体 4（TLR4）/核因子 κB（NF-κB）/c-Jun N-末端激酶（JNK）和丝裂原活化蛋白激酶（MAPK）通路的激活。特别值得注意的是，当它们联合使用（各 20mg/kg/d）时，抗 RA 作用和对 TLR4/NF-κB/MAPK 通路的抑制活性显著增强。研究结果表明，罗斯曼醇和卡诺醇通过调节 TLR4/NF-κB/MAPK 通路抑制炎症，协同缓解 RA，这意味着它们有可能被开发成治疗 RA 的新型、安全的天然组合药物。
