Six compounds have been isolated from the leaves of Pyrenacantha staudtii, two of which are new compounds.  The new compounds have been characterized as kaempherol 3-O-β-rhamnopyranosyl (1®6)- β-D-glucopyranoside (1) and 4-β-glucopyranosyl-(2-furyl)-5-methy-l,2-glucopyranoside phenylmethanone (2).  The known compounds are 3-pyridinecarboxylic acid (3), β-sitosterol (4), sitosterol 3-O-β-glucopyranoside (5) and taraxerol (6).  Their structures were determined by spectroscopic and chemical evidences.  The two new compounds together with 3-pyridinecarboxylic acid showed significant in vitro xanthine oxidase inhibitory activity.  To the best of our knowledge, this is the first report of these compounds from this plant.