<p>One new and three known compounds were isolated from the ethanol extract of <i>Psychotria prainii</i> aerial parts. By means of spectroscopic methods, their structures were elucidated to be deacetylasperulosidic acid 6-ethyl ether (<b>1</b>), asperulosidic acid (<b>2</b>), asperuloside (<b>3</b>) and obtucarbamates C (<b>4</b>). The isolated compounds were evaluated for their inhibitory effect on NO production in LPS-stimulated RAW264.7 cells. Among them, compounds <b>2</b> and <b>4</b> exhibited strong effect with the IC<sub>50</sub> values of 5.75 ± 0.85 and 6.92 ± 0.43 μM, respectively. This is the first report for the chemical composition and biological activity of <i>P. prainii</i>.</p
