AbstractTwo new furanoflavonoids, retamasins A and B (1 and 2, resp.), along with five known flavonoids, 3–7, were isolated from the aerial parts of Retama raetam. Their structures were determined on the basis of extensive spectroscopic (IR, MS, and 1D‐ and 2D‐NMR) analyses and by comparison with the literature data. This is the first report of the isolation of new furanoflavonoids 1 and 2 from Retama genus, while compounds 3, 5, and 6 were found for the first time from R. raetam. Antioxidant and anti‐inflammatory activities of the isolated compounds were also evaluated. Compounds 2, 3, and 5–7 exhibited potent inhibitions of iNOS activity with IC50 values of 2.9, 5.0, 3.1, 1.2, and 4.8 μg/ml, respectively. All compounds inhibited NF‐κB except 1 and 5. Compound 6 was most active in inhibiting iNOS and NF‐κB activity, as well as in decreasing oxidative stress.