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The present work was designed to study the chemical composition, antioxidant, antihyperglycemic effect, and toxicity assessment of <i>Ridolfia segetum</i> (L.) Moris extract. The chemical composition was studied by use of high-performance liquid chromatography (HPLC). Antioxidant power was tested by use of DPPH and FRAP assays. The antihyperglycemic effect was tested by use of a glucose tolerance test, while toxicity assessment was done in vivo by use of Wistar rats for 14 days. Analysis of the extract by HPLC-UV revealed the presence of gallic acid, catechol, vanillic acid, catechin, tannic acid, rosmarinic acid, naringenin, and coumarin acid. The crude hydroethanolic extract possessed high levels of total phenols (15.6 ± 1.76 mg EAG/g), condensed tannins (383.49 mg ECat/g DM), and flavonoid (11.63 mg EQ/g). The findings showed that the studied extract possessed good antioxidant power with IC₅₀ values equal to 550, 650, 700 µg/mL respectively for the decoction, the ethyl acetate fraction (F_2M), and the ethyl acetate fraction (F_2E). For the antioxidant activity by FRAP, the aqueous fraction (F_3E) and the aqueous extract (F₄) showed CE₅₀ values of 0.33 mg/mL and 0.4 mg/mL, respectively. Glucose tolerance test analysis showed that <i>R. segetum</i> (L.) Moris decoction had a significant postprandial antihyperglycemic effect in normal Wistar rats. The results of the acute toxicity test showed that the decoction was not toxic even at 2 g/Kg. Pancreatic α-amylase activity was significantly inhibited in the presence of <i>R. segetum</i> (L.) Moris extract (IC₅₀ = 0.133 ± 0.09 mg/mL). The outcome of the present work showed that <i>R. segetum</i> (L.) Moris is very rich in phenolic compounds with potent antioxidant and antihyperglycemic effects.