Since the leaves of some Pistacia species are used in traditional folk medicine for diabetes, this study investigated the in vitro antidiabetic effect (alpha-glucosidase and alpha-amylase) of Pistacia vera leaves. Additionally, the current study investigated the anti-hyper-cholesterolemic (cholesterol esterase), antiobesity (pancreatic lipase), and antioxidant activities (i.e., total antioxidant capacity, DPPH (2,2-Diphenyl-1-picrylhydrazyl) radical scavenging activity, metal chelating activity, and ferric-reducing antioxidant power) of P. vera leaves. The aqueous-alcoholic leaf extract inhibited alpha-amylase, alpha-glucosidase, and pancreatic lipase with the half-maximal inhibitory concentration values of 7.74 +/- 0.72,11.08 +/- 3.96, and 168.43 +/- 26.10 mu g/mL, respectively. It was determined that the crude extract had high DPPH radical scavenging activity, ferric-reducing power, and moderate metal chelating activity. The ethyl acetate (EtOAc) subextract obtained by the liquid-liquid fractionation of the crude extract showed potent alpha-amylase and alpha-glucosidase inhibitory activities. The EtOAc subextract (5.794 +/- 0.027 g/100 g subextract) was standardized by reversed-phase high-performance liquid chromatography based on beta-pentagalloyl glucose, which showed inhibitory effects on both amylase and glucosidase enzymes. Fifteen compounds, seven of which are organic acid derivatives and eight of which are flavonoids, were identified by liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS) analysis in the crude extract of P. vera leaves. Seven of the fifteen phenolic compounds detected in the crude extract by LC-QTOF-MS have both glucosidase and amylase inhibitory effects. As a result, P. vera leaves can be a potential source for compounds with high antioxidant effects that show inhibitory effects on enzymes involved in carbohydrate digestion in the prevention and treatment of diabetes or can be evaluated as a standardized extract.