Milk proteins are currently the main source of a range of biologically active substances which are inactive within the sequence of native protein but can be released by enzymatic hydrolysis. Milk borne bioactive peptides have been found to exhibit various physiological activities such as antihypertensive, opioid, immunomodulatory antimicrobial, antioxidative, antithrombotic, and cytomodulatory. Such bioactive peptides may find use in the treatment of diarrhea, hypertension, thrombosis, dental carries, oxidative stress, mineral malabsorption, and immunodeficiency. These bioactive peptides may be used in formulation of functional foods, nutraceuticals, and natural drugs because of their health benefit effects.