This book reviews the role of bioactive compounds in grape seed and their beneficial effects. Among the 11 chapters, the authors also discuss the composition, biological activity, and potential applications of grape seeds in the food industry and the health effects of grape seed extracts. As in other matrices, the presence of bioactive molecules in grape seed is related to several factors like grape varieties, climatic and soil conditions, vinification processes, winemaking procedures, extraction techniques and finally evaluation protocols. Chapter 1 addresses the extraction methodologies to obtain biomolecules of interest from grape seed, from the conventional to the most innovative. Chapter 2 discusses the most important and used methods to evaluate the antioxidant capacity of grape seed. Chapter 3 is focused on how flavonoids could modulate the body homeostasis acting directly on the gastrointestinal tract, explaining their effects on obesity-related pathologies. Chapter 4, using liquid chromatographic and mass detection techniques, centers on flavanols, one of the most important types of polyphenols occurring in grape seed. Chapter 5 complements Chapter 2 in evaluating total antioxidant capacity considering that antioxidant activity is usually due to different antioxidants present in grape seed. Chapter 6 studies the effects of polyphenolic extracts in arterial hypertension and oxidative stress via glutathione-peroxidase. Chapter 7 revises the antioxidant properties of grape seed in the conservation of different meat products and dose effect to increasing the shelf life of these products. Chapter 8 shows the potential application of developing new products with healthier characteristics to garner greater consumer acceptance using grape seed in their formulations. Chapter 9 provides a review of the composition and nutritional value of the majority compounds (fatty acid, amino acid and mineral profile), showing the potential application of the use of grape seed as a food supplement to improve the human diet. Chapter 10 indicates the potent antimicrobial activity of grape seed extract against many different microorganisms due to the presence of flavan-3-ols, inhibiting their growth, and potential applications in the food or pharmaceutical industries or even in the medical field. Chapter 11 is focused on the potential use of bioactive compounds in grape seed extract as a remedy against lipid oxidation of meat products.