Objectives This study investigates into the biological effects of solvent extracts (ethyl acetate, methanol, and water) of Scutellaria orientalis L. and Scutellaria salviifolia Benth. based on its enzyme inhibitory activity and antioxidant ability together with the screening of bioactive compounds. Methods Total and individual bioactive components were determined using spectrophotometric and HPLC-ESI-MS methods. Six antioxidant assays were conducted and enzyme inhibition was tested against key enzymes linked to the pathology of common chronic disorders. Key findings Results revealed that the aqueous extracts of both plants exerted better 2,2 '-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid scavenging, reducing power, metal chelating, and alpha-glucosidase inhibitory activities. The methanol extracts showed highest tyrosinase inhibition and antioxidant activity in phosphomolybdenum assay while the less polar ethyl acetate extracts showed better acetylcholinesterase, butyrylcholinesterase, and alpha-amylase inhibition. Phytochemical evaluation by HPLC-ESI-MS revealed the presence of high amounts of flavones. Conclusions Scutellaria orientalis and S. salviifolia are important sources of bioactive agents that warrants further studies.