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Anti-inflammatory lignans and phenylethanoid glycosides from the root of Isodon ternifolius (D.Don) Kudô
Phytochemistry ( IF 3.2 ) Pub Date : 2018-09-01 , DOI: 10.1016/j.phytochem.2018.05.017
Yanjun Zhang , Ke Wang , Huangcan Chen , Ruijie He , Runlin Cai , Jian Li , Dexiong Zhou , Wei Liu , Xishan Huang , Ruiyun Yang , Shengping Deng , Jun Li , Xinlan Guan

Five undescribed lignans, three undescribed phenylethanoid glycosides and eight known compounds were isolated from the root of Isodon ternifolius (D.Don) Kudô (Lamiaceae). The structures of all of the isolated constituents were characterized by physical data analyses including NMR, MS and ECD. The anti-inflammatory activities of the isolates were evaluated based on their ability to inhibit NO, PGE2 and TNF-α production in LPS-induced RAW 264.7 macrophage cells. Six phenyl-naphthalene lignans, ternifoliuslignan A, ternifoliuslignan B, ternifoliuslignan C, ternifoliuslignan D, ternifoliuslignan E and 3-carboxy-6,7-dihydroxy-1-(3',4'-dihydroxyphenyl) -naphthalene, can substantially inhibit the release of NO with IC50 values in the range of 9.98-29.14 μM, which are better than the positive reference. These phenyl-naphthalene lignans could markedly decrease the secretions of PGE2 and TNF-α in LPS-induced RAW264.7 cells. Ternifoliuslignan C and ternifoliuslignan D decreased iNOS, COX-2 and NF-κB/p65 protein expression. A preliminary structure-activity relationship among the phenyl-naphthalene lignans for the anti-inflammatory activity was discussed.

中文翻译:

来自 Isodon ternifolius (D.Don) Kudô 根的抗炎木脂素和苯乙醇苷

从 Isodon ternifolius (D.Don) Kudô (Lamiaceae) 的根中分离出五种未描述的木脂素、三种未描述的苯乙醇苷和八种已知化合物。所有分离成分的结构都通过物理数据分析进行表征,包括 NMR、MS 和 ECD。根据分离物抑制 LPS 诱导的 RAW 264.7 巨噬细胞中 NO、PGE2 和 TNF-α 产生的能力评估分离物的抗炎活性。六苯基萘木脂素、三叶木脂素A、三叶木脂素B、三叶木脂素C、三叶木脂素D、三叶木酚素E和3-羧基-6,7-二羟基-1-(3',4'-二羟基苯基)-萘,可显着抑制释放NO 的 IC50 值在 9.98-29.14 μM 范围内,优于阳性参考。这些苯基萘木脂素可以显着减少 LPS 诱导的 RAW264.7 细胞中 PGE2 和 TNF-α 的分泌。Ternifoliuslignan C 和 ternifoliuslignan D 降低 iNOS、COX-2 和 NF-κB/p65 蛋白表达。初步讨论了苯基萘木脂素之间抗炎活性的构效关系。
更新日期:2018-09-01
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