Using activity-guided fractionation, six extracts with different polarity, isolated fractions, and purified compounds from Lycii Radicis Cortex were tested for NF-魏B inhibition and PPAR纬 activation in vitro. The structure of the purified compounds was elucidated by NMR and MS techniques.
The ethyl acetate extract and the methanol extract of Lycii Radicis Cortex suppressed tumor necrosis factor alpha (TNF-伪)-induced activation of NF-魏B, while the dichloromethane extract activated PPAR纬. Nine phenolic amide analogues, including trans-N-(p-coumaroyl)tyramine (1), trans-N-feruloyltyramine (2), trans-N-caffeoyltyramine (3), dihydro-N-caffeoyltyramine (4), three neolignanamides (5-7), and two lignanamide (8, 9), were isolated and their inhibitory potential on NF-魏B was determined (1-4 were also contained in water decoction). Two of the nine isolated phenolic amides inhibited TNF-伪-induced NF-魏B activation. Trans-N-caffeoyltyramine was verified as the key component responsible for the NF-魏B inhibition with an IC50 of 18.4 渭M in our cell-based test system. Activation of PPAR纬 was attributed to a palmitic-acid enriched fraction which displayed concentration-dependent effect ablated upon co-treatment with the PPAR纬 antagonist T0070907.
Phenolic amides were confirmed as main components from Lycii Radicis Cortex responsible for NF-魏B inhibition. Fatty acids were identified as the major plant constituent responsible for the PPAR纬 activation. Structure-activity relationship analysis suggests that the NF-魏B inhibitory activity of trans-N-caffeoyltyramine may be attributed to its Michael acceptor-type structure (伪,尾-unsaturated carbonyl group). The data of this study contribute to a better understanding of the molecular mechanism of action of Lycii Radicis Cortex extracts in the context of inflammation.