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Bioactive peptides are functional agents encrypted in food proteins with several potential health benefits. Food-derived proteins when hydrolysed release large variety of bioactive peptides which are similar in structure to peptide sequences acting in the organism as endogenous signals, or hormones and alter their physiological functions. Moreover, these bioactive peptides owing to their high tissue affinity, specificity and efficiency can interact with receptors, enzymes and certain biomolecules in organism thereby confer health promoting effects. In addition, several studies have revealed that these peptides exhibit beneficial effects for the treatment and management of chronic and several degenerative diseases including hypertension, diabetes, obesity and cancer. Therefore, this review mainly used ISI, SCOPUS and PubMed indexed journals containing various experimental reports on in vitro and in vivo studies from humans and animals to elucidate the potential health promoting effects of food-derived bioactive peptides with emphasis on antihypertensive peptides, antidiabetic peptides, cholesterol-lowering peptides, anticancer peptides, and antimicrobial peptides.