Marine organisms represent a great source of natural bioactive molecules, from which bioactive peptides are of great importance in biomedicine application in many diseases such as diabetes and its related complications. In this study, greater weever (Trachinus Draco) myofibrillar proteins were sequentially hydrolyzed and the different RP-HPLC purified fractions were tested for potential inhibitory activities of ACE and DPP4, in addition to metal chelation and antioxidant activities. Four fractions were found to have high levels of activity (with two peptides being multifunctional) and were subsequently sequenced using the de novo sequencing method. The results indicate that the peptides are novel and highly effective for each related activity compared to reference molecules. The current findings suggest these multifunctional peptides as promising therapeutics against oxidative stress, hypertension, and diabetes.