The dairy industry generates substantial amounts of whey, which
should be adequately managed not only to attend to environmental
concerns, but also to generate added valued products. The conversion
ofwhey into useful products can be achieved by enzymatic catalysis. Intensive
research has been devoted to investigate the ability of different
enzymes and conditions to generate bioactive peptides from whey.
Several proteolytic enzymes have been used to produce whey-derived
products showing improved biological activities, such as antimicrobial,
antioxidant, antihypertensive, and antidiabetic, among others. The
association of this variety of biological activities with diverse peptide
sequences derived fromwhey proteins indicates thatwhey is an important
source of bioactive peptides. However, additional research is necessary
regarding cytotoxicity studies to ensure safety and the absence of
adverse effects in vivo. The importance and necessity of confirming the
already established effects by human trials, evaluating different aspects
such as dose, toxicity, and possible side effects should be also considered.
Detailed investigation is required to provide a better knowledge
about the maintenance of bioactivity during gastrointestinal transit,
mechanisms of peptide absorption, and their fate and site(s) of action
in vivo. The mechanismof action of many whey-derived bioactive peptides
needs to be completely elucidated. As these peptides (or hydrolysates)
would be intended to be ingested in food formulations, the
interaction with other components in the food matrix should be investigated.
In addition, their incorporation as free or encapsulated ingredients
is also an interesting topic for future research. The cost of peptide
isolation or synthesis leads to the necessity of large-scale production
methodologies to warrant sufficient material for in vivo studies and
food formulations. Therefore, further technological studies are required
to establish experimental conditions to reach higher yields of these bioactive
molecules.