The increasing global population places a clear priority on increasing food production. However, the continued undernourishment of a significant proportion of the global population is accompanied by increases in developed and rapidly developing countries of over-consumption, particularly of highly refined processed foods which are rich in starch, sugars, and fats, including products made from white wheat flour. This diet combined with an increasingly sedentary lifestyle is associated with a cluster of symptoms which have been termed the metabolic syndrome and are associated with increased risk of type 2 diabetes, atherosclerosis, cardiovascular disease, and forms of cancer. There is clear evidence that the consumption of either wholegrain cereals or components present in these (notably dietary fiber) has beneficial effects in reducing the risk of the metabolic syndrome and associated diseases. This article therefore reviews the major groups of bioactive components present in the wheat grain and discusses strategies for manipulating their amounts and compositions to increase the health benefits of both wholegrain and white flour products.