Medicinal plants are extensively studied because of their wealth in various substances with a potential use in medicine and food. Pistacia lentiscus, a plant growing in the Mediterranean basin, is widely used in traditional medicine for the treatment of various inflammatory-related conditions. Thus, the present study was designed to investigate the antioxidant, anti-inflammatory, antidiabetic, anti-hyperuricemic and neuroprotective potential, and identification of active compounds, using appropriate methodology. Phytochemical studies using preparative HPLC, HPLC-MS and NMR allowed the identification and structural elucidation of several known and new anthocyanins, flavonols and flavanols, thus shedding more light on the phytochemical constituents of this plant. Pistacia lentiscus extracts and fractions exhibited an outstanding scavenging capacity against a number of deleterious radicals while significantly enhancing superoxide dismutase and catalase activities, thus counterbalancing the oxidant status. Administration of Pistacia lentiscus extracts significantly decreased carrageenan-induced mice paw oedema, reduced effectively IL-1β levels in cell culture and significantly inhibited the uric acid-producing enzyme, xanthine oxidase, thereby enhancing the gouty situation of mice. On the other side, Pistacia lentiscus extracts showed good neuro-protection and restored cognitive functions in mice, partially through inhibition of acetylcholine esterase and amyloid plaque formation. Several experiments, in vitro and in vivo, indicated that Pistacia lentiscus extracts are free of genotoxic activity. Therefore, with regard to its wealth and diversity in phenolic compounds and their activity on several disease-like situations, Pistacia lentiscus could be used in palliative treatments against inflammatory conditions and diabetes complications, as well as against deterioration of cognitive functions.