Development of formulations based on bioactive peptides from Brazilian biodiversity with antimicrobial, antiproliferative and cytotoxic potential.
Bioactive Peptides; Surgamides; TsAP-2
Non-ribosomal cyclic octapeptides, surugamides A-E, were previously obtained from species of the genera Streptomyces and Saccharomyces and showed the ability to inhibit bovine cathepsin B, indicating that they may be promising for use in the treatment of cancer cell lines. TsAP-2, associated with the venom of Tityus serrulatus and the venom gland of T. stigmurus, is a linear peptide amidated at the C-terminal end with antimicrobial and anticancer properties, tested in vitro and ex vivo. In order to synthesize and obtain more efficient TsAP-2 analogues and Surugamides A-E in satisfactory quantities for pharmacological assays, synthesis methodologies were developed using the Fmoc strategy for Solid Phase Peptide Synthesis (SPFS). The biomolecules were purified by High Performance Liquid Chromatography (HPLC), identified by ESI-IT-MS (Electrospray Ionization - Ion trap - Mass Spectometry) and characterized by Nuclear Magnetic Resonance (NMR). The cytotoxic properties, anticancer action mechanisms and synergistic effects with doxorubicin of surugamides were investigated. The current results of this study and of collaborations encourage the expansion of future studies on the biological activities and the development of formulations based on bioactive peptides.