The “diseases of affluence” are defined as particular medical conditions determined by an increasing wealth in a society and to the consequent increase in life expectancy and change in lifestyle. Unhealthy dietary habits and additional risk factors (smoking, alcohol consumption, poor physical exercise) have been recognized as important triggering agents for the diseases of affluence. Increasing evidence linked a correct dietary intake to a clear reduction of the risk of developing most of these pathologies. Therefore a big effort is now concentrated on studying food from a functional (pharmaceutical) point of view together with the nutritional point of view leading to the raise of the “nutraceutical” science. Our laboratory has for many years focused its research on the functional properties of wheat sprout. The sprout is the functionally richest growth stage of wheat (and possibly of many other vegetables) and we previously demonstrated that an extract from wheat sprouts possess a large amount of antioxidant molecules and a consequently wide range of biological activities. In this mini review, we summarize the data obtained from our attempt to separate and characterize the molecular components of this extract. The characterization revealed two main classes of functional molecules: an hydrophilic peptidic fraction and moderately hydrophobic polyphenolic fractions. Both the classes exert a remarkable activity that explains the functional properties already demonstrated for the whole wheat sprout extract.