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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 5
BKCSDE 34(5)
May 20, 2013 

NF-κB Inhibition and PPAR Activation by Phenolic Compounds from Hypericum perforatum L. Adventitious Root
Wei Li, Yan Ding, Tran Hong Quang, Nguyen Thi Thanh Ngan, Ya Nan Sun, Xi Tao Yan, Seo Young Yang, Chun Whan Choi, Eun Jung Lee, Kee Yoeup Paek, Young Ho Kim*
Hypericum perforatum, Hypericaceae, NF-κB-luciferase assay, PPRE-luciferase assay, PPAR transactivational activity
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.
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