The antioxidant, anticholinesterase, anti-tyrosinase, anti-α-glucosidase, cytotoxic, antifungal and antibacterial activities of Ethyl acetate (EtOAc) and n-butanol (n-BuOH) extracts and three compounds isolated from Anvillea radiata (Asteracea); two epimer germacranolides 9α-hydroxyparthenolide(1), 9β-hydroxyparthenolide(2) and a phenolic acid; 3,5-O-dicaffeoylquinic acid (3), were evaluated.The antioxidant activity was assessed using two methods (DPPH and ABTS). In the DPPH and ABTS methods, EtOAc extract exhibited the strongest radical scavenging activity with an IC50 value of 0.0026 mg/mL and 0.0011 mg/mL, respectively. This extract and the two germacranolides (1) and (2) exhibited considerable anticholinesterase and anti-tyrosinase activities, 9α-hydroxyparthenolide(1) exhibited the highest effect with values of IC50 = 0.025 mg/mL and % of inhibition = 79.55%, respectively. Compound 3 displayed the highest α-glucosidase inhibitory activity with IC50 = 0.09 mg/mL. The antibacterial effect of the isolated compounds and the studied extracts was rated limited. The two compounds 1 and 2 exhibited a high cytotoxic activity against MCF-7 cancer cell lines with growth inhibition of 98.12% and 78.50%, respectively at 50 μM but showed a moderate cytotoxic effect towards OVCAR-3 cell lines. These results suggest that A.radiata has several biological activities and could provide a potential natural source of bioactive compounds and be beneficial to the human health and as source of natural antioxidants in food industry.