Luteolin glycosides identified in lemongrass by 1H NMR,namely luteolin 7-O-β-glucopyranoside, luteolin 6-C-β-glucopyranoside (isoorientin) and luteolin 2″-O-rhamnosyl-C-(6-deoxy-ribo-hexos-3-ulosyl) (cassiaoccidentalin B) demonstrated lower cy-totoxicity than luteolin aglycone, suggesting that these compounds could be an interesting alternative to NSAIDs, known to have gastrointestinal adverse effects.The data pre-sented here also evidenced that the in vitro anti-inflammatory activity of luteolin is dependent on its glycosylation, allow-ing the establishment of structure–activity relationships. For the anti-inflammatory parameters analyzed luteolin 7-O-β-glucopyranoside demonstrated strong anti-inflammatory ac-tivity than C-glycosides.