Up-cycling of agro-alimentary industry waste is getting more attention from the scientists due to the fact that most of vegetable residues may be considered as a resource of high added value products, such as flavours, antioxidants, cosmetic excipients or active principles, drugs or drug adjuvants. This paper focuses on the opportunities opened by grapes (Vitis vinifera), one of the largest and most common fruit crop in Europe. Identification and/or isolation of bioactive natural products from this waste, as well as their chemical and/or enzymatic modification, are the main directions to obtain valuable natural compounds from up-cycled food industry waste.