The development of high-value bioactive compounds from marine resources has enormous promise. Bioactive compounds of marine origin have become more prevalent in the last 10 years. Much work has been done to study how marine natural products are made from bioactive compounds and determine how these compounds get their complex structures and biological functions. In recent years, only a few marine species were studied to have regenerative potential due to the presence of bioactive compounds. However, scientists’ hard work and technological advances have helped make much progress in this field. Many of these compounds have played important roles as pharmaceutical leads for wound healing drugs and anticancer/antimicrobial drugs, which in turn have led to the development of treatments for cancer. Peptide-based chemotherapy can be divided into peptide-alone therapy, peptide vaccines, and peptide-conjugated nanomaterials. Some compounds with interesting biological effects build up fairly rapidly in marine invertebrates. When peptides are mixed with nonmaterial, their ability to treat cancer increases significantly by improving drug delivery stability and oversensitivity. This chapter describes advances in biologically active peptide research and how bioactives and peptides in marine organisms with regeneration activity make secondary metabolites. In the end, we talk about the future of this research and the new ways that marine organism peptides have been used in treating cancer and wound healing in recent years, including in diagnosis, treatment, and prognosis. This book chapter could strengthen our understanding of fundamental principles, advancements, and patent applications in different life sciences industries. © 2024 Elsevier B.V., All rights reserved.