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Anti-inflammatory activity of a crude extract of Piper magnibaccum(Piperaceae) and of compounds isolated from it was established using the TPA-induced mouse ear edema model and an in vitroquantitative lipoxygenase inhibition assay. Five compounds were isolated from P. magnibaccum[β-sitosterol, N-isobutyl-(2E,4E)-tetradecadienamide, linoleic acid, 13-(4′, 5′-dimethoxytridecanoyl)piperidine, and piperine]. The light petroleum extract of the plant exhibited significant anti-inflammatory activity in both models. N-isobutyl-(2E,4E)-tetradecadienamide showed significant activity, with an IE % value of 70.2 + 5.4 in the TPA-induced mouse ear edema model and 87.2 + 0.11 in the in vitroquantitative lipoxygenase inhibition assay.