The chemical composition of Piper sarmentosum roots and their anti-inflammatory activity were investigated. A new amide alkaloid,namely chaplupyrrolidone D (1),together with nine known compounds,namely magnolamide (2),N-trans-cinnamoyltyramine (3),trans-N-p-coumaroyltyramine (4),indole-3-carbaldehyde (5),indole-3-carboxylic acid (6),N-benzoyl-2-phenylethylamine (7),N-benzoyltyramine (8),N-benzoyltyramine methyl ether (9),hortiamide (10),was isolated and purified from the 95% ethanol extract of P. sarmentosum roots by comprehensive chromatography methods of silica gel column,Sephadex LH-20 gel column and semi-preparative HPLC.All compounds except compound 5 are obtained from P. sarmentosum for the first time. Biologically,compounds 1,2,4 and 10 exhibited inhibitory effects on LPS-induced NO production in RAW 264.7 cells with IC₅₀ values of 34.65 ± 1.78,25.41 ± 0.94,15.27 ± 0.82 and 39.57 ± 2.10 μmol/L,respectively.