The genus Rubus has a number of economically important members which can be considered as natural agents in several traditional folk remedies. Taking this into consideration, the present study was designed to investigate antioxidant activities and enzyme inhibitory effects of the extracts and fractions (RC1, H2O; RC2, 50% MeOH; RC3, MeOH; RC4, Et2O; RC5, EtOAc; RC6, n-BuOH) obtained from the aerial parts of Rubus caesius. Different assays to detect antioxidant capacity, especially free radical scavenging (ABTS and DPPH assays), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating were performed. Enzyme inhibitory effects were also tested towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), tyrosinase, and glycolytic enzymes. Additionally, total phenolic and flavonoid content using colorimetric assays was examined. Strongest antioxidant potential among all samples RC1-RC6 was observed for the RC5 which ranging from 1.58 ± 0.01 to 4.98 ± 0.05 mmol TE/g extract. Also, RC5 contained highest concentration of total polyphenolics (315.02 ± 9.11 mg GAE/g) and flavonoids (38.13 ± 0.37 mg RE/g). Highest metal chelating capabilities was observed for RC2, being equal to 16.62 ± 1.71 mg EDTAE/g. All tested samples were active against AChE, however only three fractions RC1, RC2 and RC3 were active against BChE. Activity was observed in range of 1.99 ± 0.04 - 2.46 ± 0.01 mg GALAE/g and 1.00 ± 0.09 - 1.10 ± 0.01 mg GALAE/g for AChE and BChE, respectively. Tested extracts and fractions inhibited α-amylase, with RC5 showing highest activity equal to 0.70 ± 0.07 mmol ACAE/g, while the same fraction (RC5) was most effective inhibitor (2.03 ± 0.01 mmol ACAE/g) of α-glucosidase. The RC6 fraction had the strongest anti-tyrosinase inhibitor ability 63.12 ± 0.26 mg KAE/g. The present study demonstrated that R. caesius may be considered as a source of biologically active phytoconstituents to develop novel functional products or natural drugs in pharmaceutical field.