State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Guilin, 541004, China; School of Petroleum and Chemical Engineering, Qinzhou University, Qinzhou, 535000, China.
State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Guilin, 541004, China.
Phytochemistry. 2018 Sep;153:36-47. doi: 10.1016/j.phytochem.2018.05.017. Epub 2018 May 31.
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 IC 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.
从 Isodon ternifolius（D.Don）Kudô（唇形科）的根部分离得到五个未描述的木脂素、三个未描述的苯乙醇苷和八个已知化合物。所有分离得到的成分的结构均通过包括 NMR、MS 和 ECD 在内的物理数据分析进行了表征。根据它们抑制 LPS 诱导的 RAW 264.7 巨噬细胞中 NO、PGE2 和 TNF-α 产生的能力，评估了这些分离物的抗炎活性。六种苯萘木脂素、ternifoliuslignan A、ternifoliuslignan B、ternifoliuslignan C、ternifoliuslignan D、ternifoliuslignan E 和 3-羧基-6,7-二羟基-1-（3',4'-二羟基苯基）-萘，可显著抑制 NO 的释放，IC 值范围为 9.98-29.14 μM，优于阳性对照。这些苯萘木脂素可以显著降低 LPS 诱导的 RAW264.7 细胞中 PGE2 和 TNF-α 的分泌。ternifoliuslignan C 和 ternifoliuslignan D 降低了 iNOS、COX-2 和 NF-κB/p65 蛋白的表达。讨论了苯萘木脂素类化合物抗炎活性的初步构效关系。
