Autoxidation in food and biological systems is responsible for a multitude of adverse effects and implications in human health as well as in food stability and preservation. Antioxidants play a major role in preventing or delaying autoxidation and have attracted much attention as food stabilizers, dietary supplements and natural health products. Both synthetic and natural antioxidants are widely used in food products and an ever increasing number of research papers have appeared in the recent literature on the discovery and application of natural antioxidants and their therapeutic use in inhibiting a myriad of diseases. However, some common synthetic antioxidants have also become controversial due to their potential adverse effects on health. This overview provides the latest developments about novel antioxidants, particularly phenolic derivatives, peptides/protein hydrolysates, phospholipids and polysaccharides, and their role in food quality preservation and human health promotion.