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

Abstract

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 IC 50 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 EC 50 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.

Constituents ofTalisia nervosawith Potential Utility against Metabolic Syndrome

“…Subsequently, these compounds were also evaluated for NF-κB and iNOS inhibition, in order to investigate their anti-inflammatory potential. As a result, compound 1 did not show inhibition of phorbol 12-myristate 13-acetate (PMA) induced NF-κB activation, which is in agreement with the previous report related to the effect of catechin on NF-κB [19]. In addition, no inhibition of iNOS activity in LPS induced macrophages was seen, even though a weak effect of catechin on iNOS was reported earlier [20].…”

Cratoxylum formosum (Jack) Dyer ssp. pruniflorum (Kurz) Gogel. (Hóng yá mù) extract induces apoptosis in human hepatocellular carcinoma HepG2 cells through caspase-dependent pathways

“…Xanthones, anthraquinones, and cochinchinone were identified in dichloromethane extracts of CF roots and bark [ 13 , 37 ], and quercetin, xanthones, and mangiferin were found in CF leaves and stem [ 38 ]. The bioactive compounds possessing anticancer activity in CF were cochinchinone A [ 39 , 40 ], macluraxanthon [ 41 ], norcowanin [ 42 , 43 ], and brasilixanthone [ 44 ]. Other activities were also reported for the dichloromethane extract, in which dulcisxanthone B had a DPPH-scavenging effect and inhibited lipid peroxidation [ 45 ].…”

COVID-19 Spotlights Connections between Disease and Multiple Lifestyle Factors

“… 250 In addition to the direct antiviral effects of flavonoid derivates described above, phenolics in dark green leafy vegetables such as kale and spinach activate a transcription factor that terminates inflammation. 251 Foods with high levels of omega-3 fatty acids also promote termination of inflammation. 252 Finally, foods containing high levels of certain carotenoids decrease inflammation markers.…”