Novel phenanthrene/bibenzyl trimers from the tubers of Bletilla striata attenuate neuroinflammation via inhibition of NF-κB signaling pathway  

作　　者：SHAO Siyuan SUN Mohan MA Xianjie JIANG Jianwei TIAN Jinying ZHANG Jianjun YE Fei LI Shuai 

机构地区：[1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China

出　　处：《Chinese Journal of Natural Medicines》2024年第5期441-454,共14页中国天然药物（英文版）

基　　金：This research was supported by the National Natural Science Foundation of China(No.81903488);the CAMS Innovation Fund for Medical Sciences(No.CIFMS-2021-I2M-1-026)。

摘　　要：Five novel(9,10-dihydro)phenanthrene and bibenzyl trimers,as well as two previously identified biphenanthrenes and bibenzyls,were isolated from the tubers of Bletilla striata.Their structures were elucidated through comprehensive analyses of NMR and HRESIMS spectroscopic data.The absolute configurations of these compounds were determined by calculating rotational energy barriers and comparison of experimental and calculated ECD curves.Compounds 5b and 6 exhibited inhibitory effects on LPS-induced NO production in BV-2 cells,with IC_(50) values of 12.59±0.40 and 15.59±0.83μmol·L^(-1),respectively.A mechanistic study suggested that these compounds may attenuate neuroinflammation by reducing the activation of the AKT/IκB/NF-κB signaling pathway.Additionally,compounds 3a,6,and 7 demonstrated significant PTP1B inhibitory activities,with IC_(50) values of 1.52±0.34,1.39±0.11,and 1.78±0.01μmol·L^(-1),respectively.Further investigation revealed that compound 3a might inhibit LPS-induced PTP1B overexpression and NF-κB activation,thereby mitigating the neuroinflammatory response in BV-2 cells.

关 键 词：Bletilla striata Phenanthrene/bibenzyl trimer NO inhibition AKT/IκB/NF-κB signaling pathway PTP1B inhibitory effect 

分 类 号：R285[医药卫生—中药学]