Background: The value of proteins in human health as the main source of amino acids has been proven. In addition to nutritional value, proteins also have biological functions that are expressed by bioactive peptides. Production methods of bioactive peptides affect their function. This article aims to investigate sources and production methods of bioactive peptides effective on human health. Methods: For gathering information in this review, English articles between 1988 and 2018 containing one of the keywords "bioactive peptides, enzymatic hydrolysis, anti-cancer and anti-hypertensive agents" were searched in PubMed, Scopus, Science Direct and the Islamic World Science Citation Database (ISC). Among 643 papers found, 28 articles related to the subject were selected. Results: The articles show that utilizing the enzymatic hydrolysis method for therapeutic applications causes them to be more stable in comparison with fermentation and solvent extraction methods and is safer than the other two methods. Also, the positive health effects of these compounds include reducing the risk of chronic diseases, increasing immune function, reducing cholesterol, antimicrobial activity, as well as antioxidant, anti-clotting, antihypertensive, and anticancer properties. Conclusion: In recent years, the role of bioactive peptides as therapeutic compounds has been highlighted. Bioactive peptides can play an effective role in human health. Therefore, investment and planning in this area can affect the future health of the country.
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