Ethnobotanical evidences substantiate the use of several Centaurea species to treat and/or manage several human ailments. In the present study, the phytochemical profile of the ethyl acetate, methanol, and aqueous extracts (prepared by infusion and decoction) of Centaurea bornmuelleri Hausskn. aerial parts was established. The enzyme inhibitory and antioxidant properties were also determined by in vitro bioassays. Methanol extract (38.58 mg gallic acid equivalent/g extract) and ethyl acetate extract (38.83 mg rutin equivalent/g extract) possessed the highest concentration of phenolics and flavonoids, respectively. Aqueous extract prepared following traditional infusion method showed potent DPPH (38.54 mg TE/g extract) and ABTS (57.75 mg TE/g extract) scavenging abilities. The methanol extract (101.46 mg TE/g extract) of C. bornmuelleri exhibited potent reducing activity in the CUPRAC assay while the aqueous extract obtained by infusion was more active in the FRAP assay (69.81 mg TE/g extract). Ethyl acetate extract of C. bornmuelleri inhibited both acetylcholinesterase (1.14 mg galantamine equivalent [GALAE]/g extract), butyrylcholinesterase (0.63 mg GALAE/g extract), tyrosinase (69.84 mg kojic acid equivalent/g extract), amylase (19.90 mg acarbose equivalent [ACAE]/g extract), and glucosidase (33.12 mg ACAE/g extract). The phytochemical profile of C. bornmuelleri has been characterized and the main components quantified in order to provide scientific base to design innovative products including pharmaceuticals, cosmetics or nutraceuticals although further investigation concerning the isolation of the main bioactive compounds would be required.