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Bioactive peptides have been defined as specific protein fragments that have a positive impact on body functions and conditions and may ultimately influence health [79]. According to Fitzgerald and Murray [46], bioactive peptides have been defined as peptides with hormone- or drug like activity that eventually modulate physiological function through binding interactions to specific receptors on target cells leading to induction of physiological responses. According to their functional properties, bioactive peptides may be classified as antimicrobial, antithrombotic, antihypertensive, opioid, immunomodulatory, mineral binding and antioxidative. These peptides play an important role human health. In this review, we describe above stated properties of bioactive peptides especially derived from milk.