Cow milk proteins are considered as the rich source of bioactive peptides which has a great influence in the various biological processes. The present study was aimed to evaluate anti-inflammatory (stabilizing of Erythrocyte Membrane Integrity) and antihypertensive (Angiotensin Converting Enzyme inhibition) bioactive peptides derived from cow milk protein casein after treatment with trypsin. Casein was prepared and treated with trypsin & extent of hydrolysis was analyzed. Bioactive peptides thus generated were evaluated for their said activities. Maximum anti-inflammatory effect was shown after 4 hours of enzymatic treatment; while maximum antihypertensive effect was shown after 3 hours of treatment. The results obtained hence proved that bioactive peptides released during tryptic digestion at different incubation times show significant effect on metabolic activities providing the need for further investigation for their targeted use as human nutritional supplements for specific medical conditions.