NF-κB activation and ppar transactivational effects of a new aliphatic acid amide from pericarps of zanthoxylum piperitum

Abstract

A new aliphatic acid amide, ZP-amide F (1), and eight known compounds, including bungeanumamide A (2), tumuramide C (3), ZP-amide A (4), ZP-amide B (5), ZP-amide D (6), hyperin (7), quercitrin (8), and (-)- sesamin (9), were isolated from pericarps of Zanthoxylum piperitum. The effects of these compounds on TNFα-induced NF-ΚB activation and transactivational activity of PPARs, including PPARα, PPARβ(Δ) and PPARγ subtypes, were evaluated. Compounds 7 and 9 exhibited potent inhibitory effects on TNFα-induced NF-ΚB activation with IC50 values of 5.50 and 8.10 μM, respectively. Aliphatic acid amide compounds 3, 4 and 6 displayed enhanced effects on PPAR transactivational activity with EC50 values of 47.12, 19.13 and 12.02 μM, respectively. Among them, compound 4 demonstrated an increase in PPARα transactivational activity, compound 3 showed a moderate increase on all PPAR subtypes, whereas compound 6 displayed weak PPAR transactivational activity.