Eight amides, pellitorine (1), guineensine (2), brachystamide B (3), sarmentine (4), brachyamide B (5), 1-piperettyl pyrrolidine (6), 3',4',5'-trimethoxycinnamoyl pyrrolidine (7) and sarmentosine (8), two lignans, (+)-asarinin (9) and sesamin (10), and four other compounds, 1-(3,4-methylenedioxyphenyl)-1E-tetradecene (11), methyl piperate (12) and a mixture of beta-sitosterol (13) and stigmasterol (14), were isolated from the fruits of Piper sarmentosum (Piperaceae). This is the first reported isolation of compounds 2, 3, 5, 6, 7, 9, 10 and 12 from this plant species. Their structures were established from spectral data. These compounds were evaluated in antituberculosis and antiplasmodial tests. The results showed that compounds 4 and 6 exhibited both activities while compounds 1, 2, 5, 8 and 11 showed only antituberculosis activity. This is the first report of the antituberculosis and antiplasmodial activities for these compounds.