NF-κB Inhibition and PPAR Activation by Phenolic Compounds from Hypericum perforatum L. Adventitious Root

Bulletin of the Korean chemical society

Young Ho Kim¹  Chun Whan Choi¹  Yan Ding¹  Eun Jung Lee¹  Kee Yoeup Paek¹  Nguyen Thi Thanh Ngan¹  Wei Li¹  Ya Nan Sun¹  Tran Hong Quang¹  Xi Tao Yan¹  Seo Young Yang¹ 

关键词: Hypericum perforatum;    Hypericaceae;    NF-κB-luciferase assay;    PPRE-luciferase assay;    PPAR transactivational activity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A new compound, perforaphenonoside A (1), along with 11 known compounds (2-12) were isolated from a methanol extract of adventitious roots of Hypericum perforatum. Their chemical structures were elucidated using chemical and physical methods as well as comparison of NMR and mass spectral data with previously reported data. Their inhibition of NF-κB and activation of PPAR was measured in HepG2 cells using a luciferase reporter system. Among the compounds 3, 6, 7 and 12 inhibited NF-κB activation stimulated by TNFα in a dose-dependent manner, with IC50 values ranging from 0.85 to 8.10 μM. Moreover, compounds 1- 3, 7, 11 and 12 activated the transcriptional activity of PPARs in a dose-dependent manner, with EC50 values ranging from 7.3 to 58.7 μM. The transactivational effects of compounds 1-3, 7, 11 and 12 were evaluated on three individual PPAR subtypes. Among them, compound 2 activated PPARα transcriptional activity, with 153.97% stimulation at 10 μM, while compounds 1, 2 and 11 exhibited transcriptional activity of PPARγ, with stimulation from 124.76% to 126.91% at 10 μM.

【 授权许可】

Unknown