Inhibition of Nitric Oxide Production in BV2 Microglial Cells by Triterpenes from Tetrapanax papyriferus.
Inhibition of Nitric Oxide Production in BV2 Microglial Cells by Triterpenes from Tetrapanax papyriferus.
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DOI：
10.3390/molecules21040459
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发表时间：
2016-04-07
期刊：
影响因子：
--
通讯作者：
Sung SH
中科院分区：
文献类型：
--
作者：
Cho N;Moon EH;Kim HW;Hong J;Beutler JA;Sung SH
众所周知，激活的小胶质细胞产生一氧化氮（NO），一氧化氮在阿尔茨海默病等神经退行性疾病的病理生理中起着重要作用。在从药用植物中寻找治疗神经炎症性疾病的新药物的过程中，发现纸莎草四七醇提物对脂多糖（LPS）刺激的BV2小胶质细胞具有显著的NO抑制活性。从papyriferus的叶和茎中分离到了9个齐墩烷型三萜，包括两个新化合物epipapyriogenin C-3-O-β-d-glucopyranoside(6)和11-O-butylpapyrioside LIIc(9)。这些化合物的结构通过一维和二维核磁共振和质谱数据进行了鉴定。其中Δ11,13个齐墩烷型三萜中，化合物3对BV-2细胞有明显的NO抑制活性，降低lps诱导的COX-2和促炎细胞因子TNF-α、IL-6的表达。化合物7和9对Δ12齐墩烷型三萜皂苷也有NO抑制作用。这些结果表明，从papyriferus中分离的齐墩烷型三萜可能是用于治疗神经退行性疾病的NO抑制剂的潜在天然资源。
It is well known that activated microglia produce nitric oxide (NO), which has an important role in the pathophysiology of several neurodegenerative diseases such as Alzheimer’s disease. In the course of searching for novel therapeutic agents from medicinal plants against neuroinflammatory diseases, the methanolic extract of Tetrapanax papyriferus was found to have significant NO inhibitory activity in lipopolysaccharide (LPS)-stimulated BV2 microglia cells. Nine oleanane-type triterpenes, including two new compounds, epipapyriogenin C-3-O-β-d-glucopyranoside (6) and 11-O-butylpapyrioside LIIc (9), were isolated from the leaves and stems of Tetrapanax papyriferus. The structures of these compounds were elucidated with 1D- and 2D-NMR and MS data. Among these Δ11,13 oleanane-type triterpenes, compound 3 showed significant NO inhibitory activity in BV-2 cells, reducing the LPS-induced expression of COX-2 and pro-inflammatory cytokines such as TNF-α and IL-6. Compounds 7 and 9 also showed NO inhibitory activities among the Δ12 oleanane-type triterpene saponins. These results show that oleanane-type triterpenes isolated from T. papyriferus could be a potential natural resource of NO inhibitors used in the treatment of neurodegenerative disorders.
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