Three naphthopyrone glucosides, cassiaside (1), $rubrofusarin-6-O-{eta}-D-gentiobioside$ (2), and $toralactone-9-O-{eta}-D-gentiobioside$ (3), were isolated from the BuOH-soluble extract of the seeds of Cassia tora as active constituents, using an in vitro bioassay based on the inhibition of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structures of 1-3 were determined by spectroscopic data interpretation, particularly by extensive 1D and 2D NMR studies. All the isolates (1-3) were evaluated for the inhibitory activity on AGEs formation in vitro.