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Background: The well-recognized but not fully explored antioxidant activity of marine-biota-derived, biologically active substances has led to interest in their study as substitutes of antibiotics, antiaging agents, anticancer and antiviral drugs, and others. The aim of this review is to present the current state of the art of marine-biota-derived antioxidants to give some ideas for potential industrial applications. Methods: This review is an update for the last 5 years on the marine sources of natural antioxidants, different classes antioxidant compounds, and current derivation biotechnologies. Results: New marine sources of antioxidants, including byproducts and wastes, are presented, along with new antioxidant substances and derivation approaches. Conclusions: The interest in high-value antioxidants from marine biota continues. Natural substances combining antioxidant and antimicrobial action are of particular interest because of the increasing microbial resistance to antibiotic treatments. New antioxidant substances are discovered, along with those extracted from marine biota collected in other locations. Byproducts and wastes provide a valuable source of antioxidant substances. The application of optimized non-conventional derivation approaches is expected to allow the intensification of the production and improvement in the quality of the derived substances. The ability to obtain safe, high-value products is of key importance for potential industrialization.

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(1) Background: (KLAKLAK)2 is a representative of the antimicrobial peptide group which also shows good anticancer properties. (2) Methods: Herein, we report synthesis using SPPS and characterization by HPLC/MS of a series of shortened analogues of (KLAKLAK)2. They contain single sequence KLAKLAK as C-terminal amides. In addition, substitution of some natural amino acids with unnatural β-Ala and nor-Leu is realized. In addition, these structures are conjugated with second pharmacophore with well proven anticancer properties 1,8-naphthalimide or caffeic acid. Cytotoxicity, antiproliferative effect and antimicrobial activity of newly synthesized structures were studied. (3) Results: The obtained experimental results reveal significant selective index for substances with common chemical structure KLβAKLβAK-NH2. The antibacterial properties of newly synthesized analogues at two different concentrations 10 μM and 20 μM, were tested against Gram-negative microorganisms Escherichia coli K12 407. Only two of the studied compounds KLAKLAK-NH2 and the one conjugated with second pharmacophore 1,8-naphthalimide and unnatural amino acid nor-Leu showed moderate activity against tested strains at concentration of 20 μM. (4) Conclusions: The obtained results reveal that the introducing of 1,8-naphthalimideGly- and Caf- increase the cytotoxicity and antiproliferative activity of the peptides but not their selectivity. Only two compounds KLAKLAK-NH2 and 1,8-naphthalimideGKnLAKnLAK-NH2 show moderate activity against Escherichia coli K12 at low concentration of 20 μM.