© University of Ankara. All rights reserved.Objective: In this study, we aimed to evaluate the HPLC, phytochemical, anticholinesterase and antioxidant profiles of the aerial parts of Asperula taurina subsp. caucasica. Material and Method: The fingerprint of the phenolic compounds of the methanolic extract of the plant was obtained using RP-HPLC method. The method was also validated in terms of detection limits, quantification limits, linearity, accuracy, precision and selectivity. The phenolic contents of A. taurina subsp. caucasica were detected as proto-catechuic acid, p-OH benzoic acid and benzoic acid. In the phytochemical studies, quercetin 3-O-β-galactoside was isolated from the ethyl acetate subfraction of A. taurina subsp. caucasica using by several chromatographic methods. The structure of the pure compound was elucidated by means of spectral analysis (1H NMR, 13C NMR, and ESI-MS). Anticholinesterase and antioxidant activity studies were performed on quercetin 3-O-β-galactoside and the methanolic extract of the plant. Result and Discussion: While quercetin 3-O-β-galactoside shown moderate inhibitory activity against butyrylcholinesterase at 200 μg/ml, quercetin3-O-β-galactoside and the metanolic exract of the plant did not show acetylcholinesterase inhibitory activity. Quercetin 3-O-β-galactoside shown DPPH free radical scavenging activity at 50 and 100 µg/ml, moderate lipid peroxidation inhibitory activity at 25, 50 and 100 µg/ml; the methanolic extract of the plant moderate lipid peroxidation inhibitory activity at 25, 50 and 100 µg/ml. In conclusion, A. taurina subsp. caucasica and quercetin 3-O-β-galactoside could be important and valuable sources for protecting our body health, especially Alzheimer's disease.