Antidiabetic, anti-Alzheimer, general toxicity, and antioxidant activities of Salvia syriaca were evaluated. Phytochemical composition of the essential oil and methanolic extract of the plant were identified using gas chromatography-mass spectrometry and reverse-phase high-performance liquid chromatography-diode array detector techniques, respectively. Essential oil of S. syriaca exhibited strong cytotoxicity, antioxidant, α-amylase, and α-glucosidase inhibitory activities. Gas chromatography-mass spectrometry analysis showed that spathulenol (87.4%), isospathulenol (7.6%), and bornyl acetate (2.7%) are the major compounds in essential oil. High-performance liquid chromatography analysis indicated that rutin, quercetin, apigenin, rosmarinic acid, and ferulic acid are the most abundant phenolic components. S. syriaca could be considered as a valuable source of bioactive natural compounds for functional foods, medical, and pharmaceutical applications.