Epidemiological studies associate whole grain consumption with a reduced risk of many diseases. This paper focuses on the antioxidant component of cereal dietary fibre starting from its chemical structure, bioavailability and biological meaning. By the critical assessment of the intervention studies performed using cereal bran and whole grains, the hypothesis that the slow and continuous release in the gut of the dietary fibre bound antioxidants determines the health benefits, is illustrated. In the last part of the work, new perspectives and technological possibilities to enhance the health potential of this cereal component are also highlighted.