Fruits of Vitis species (grapes) are one of the most consumed, even as fresh or processed products (such as juices and wines). Among organoleptic characteristics of these products (e.g., taste, aroma and freshness), the antioxidant capacity is well known. The review focuses on the classification of biologically active compounds having antioxidant activity, their analyses and pharmaceutical properties. Vitis species such as V. vinifera, V. riparia, V. aestivalis, V. rotundifolia, V. rupestris, V. coignetiae, or V. amurensis have been reviewed. Moreover, possible valorization of these antioxidant compounds, that also includes wastes from the wine industry, was emphasized and critically discussed.