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In this study, the chemical composition, antioxidant, and hypoglycemic activity of Rosa arvensisHuds. leaves and fruits collected from Zlatibor, Željin, Veliki Krš mountains and Petnica village (Serbia) were analysed. Phenolic and vitamin profiles, as well as in vitroantioxidant potential and enzyme inhibitory activity on α-amylase and α-glucosidase, were studied. Phytochemical analysis showed higher phenolic content in leaf extracts than in those obtained from fruits. Gallic, chlorogenic and syringic acids were the most abundant phenolic acids, while catechin was the major flavonoid compound. Furthermore, the highest level of α-tocopherol (1.94 mg/100 g fw) in achenes and ascorbic acid (9.60 mg/100 g fw) in hypanthium were quantified in the fruits sampled on the Veliki Krš Mt. High antioxidant capacity was observed for the leaf extracts. It was highly correlated with their chemical composition and primarily referred to the catechin content (r > 0.95, p < 0.01), while the quinic acid had the opposite effect (r > −0.97, p < 0.01). Leaf extracts also showed good α-glucosidase and moderate α-amylase inhibitory potential in contrast to hypanthium and achenes extracts with lower antidiabetic activity. The high phenolic content and noted antioxidative potential were strongly correlated with the α-glucosidase inhibitory activity (r > 0.80, p < 0.01), while the α-amylase inhibition was only moderately correlated with those compounds (r > 0.49, p < 0.01). Among the tested R. arvensissamples, those from Zlatibor Mt. contained the highest amount of target compounds and expressed the highest biological activity. The obtained results suggest that R. arvensisextracts present a new source of bioactive compounds that could be implemented as novel food ingredients.