Synthesis, Characterization and Pharmacological Evaluation of Ultra Short Dipeptides as Antimicrobial and Anticancer Agents

Background: The biological compounds known as peptides are found in nature. They are peptide (amide) links that connect short chains of amino acid monomers. Nowadays, peptide-based therapeutic treatments are employed because of their intriguing and prospective uses in drug design. These applications include minimal cytotoxicity, high specificity, tumor-penetrating ability, small size, and ease of modification. In this article, we examine a number of investigations into diverse Antimicrobial Peptides (AMPs) that have cytotoxic properties against cancer cells. The pharmacological analysis and synthesis of extremely short dipeptides form the foundation of the current research. Materials and Methods: Using microwave-assisted solid phase peptide synthesis, six extremely short dipeptides (2a-f) were created, and their in vitro antibacterial and anticancer activity was assessed. Using the agar dilution technique, the antibacterial activity of produced dipeptides was evaluated against three fungi, two gram-positive and two gram-negative bacterial strains. Spectroscopy techniques such as Proton NMR, Carbon NMR, HPLC, and LC-MS were used to characterise the synthesised dipeptides. The MTT assay was used to test the anticancer activity of produced dipeptides against the HeLa and MCF-7 cell lines. Results: The antibacterial activity of peptides 2a and 2d was shown to be superior to that of other synthetic peptides. With a MIC value of around 5–50 µg/mL, peptide 2d was shown to have strong antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus pyogenes, Staphylococcus aureus. With MFC in the range of 200–250 µg/mL, peptides 2b, 2c, and 2e demonstrated strong antifungal activity against Candida albicans. Conclusion: According to the results of the present study, extremely short dipeptides that have been created are efficient in fighting cancer and bacteria while also being safe, affordable, and less harmful.