The leaves and fruits of Rhus coriaria are traditionally used in Turkey for the treatment of diabetes. The aim of the present study is to determine α-amylase, α-glucosidase, and pancreatic lipase inhibitory activities of R. coriaria leaf and fruit ethanol extracts (80%), and to isolate active compounds against these enzymes. As a result of the activity-guided isolation, the active compounds were determined as the amentoflavone, agathisflavone, and 1,2,3,4,6-penta-O-galloyl-βglucopyranose. Agathisflavone, amentoflavone, and penta-O-galloyl-β-glucopyranose inhibited α-glucosidase with 11.4 ± 0.9, 11.3 ± 0.7, and 4.1 ± 0.1 μM IC 50 values, respectively. Furthermore, penta-O-galloyl-β-glucopyranose inhibited αamylase with 6.32 ± 0.18 μM IC 50. These three compounds also significantly inhibited (P < 0.05) pancreatic lipase. The results of high-performance liquid chromatography analysis showed that penta-O-galloyl-β-D-glycopyranose was one of the main compounds in both fruit and leaf extracts. Therefore, it may be considered that R. coriaria fruit and leaf extracts can be standardized on this substance and used in the development of both medicinal products and functional food for diabetes.