Research Unit of Analysis and Process Applied to The Environment-APAE (UR17ES32) Higher Institute of Applied Sciences and Technology of Mahdia, University of Monastir, Monastir, Tunisia.
Florida International University, Port St. Lucie, FL, 34987, USA.
Environ Sci Pollut Res Int. 2021 Aug;28(30):40908-40916. doi: 10.1007/s11356-021-13683-2. Epub 2021 Mar 27.
Dermaseptins are peptides found in the skin secretions of Phyllomedusinae frogs. These peptides exert a lytic action on various microorganisms and have no considerable hemolytic effect except dermaseptin S4 (DS4) which exhibits a powerful cytotoxic effect. Therefore, we synthesized several analogs of DS4 in an attempt to find molecules with a weak hemolytic effect and significant bioactivities. In this study, we performed the synthesis of truncated peptides by introducing C-terminal and N-terminal amino acid deletions of the native sequence. All peptide analogs, in comparison with parental peptide, were tested firstly on human red blood cells to work out their cytotoxicity, secondly on the multidrug-resistant bacteria by trying to find MICs, and finally on colon cancer tumor cell line SW620 using the MTT test so as to investigate the anti-proliferative effect. Our results showed that, on the one hand, the N terminus of the native peptide was necessary for the antibacterial activity and the anti-proliferative effect of the peptide. On the other hand, the hemolytic activity was more notable in the sequences broken down on the C-terminal side.
棘肽是在 Phyllomedusinae 青蛙的皮肤分泌物中发现的肽。这些肽对各种微生物具有裂解作用，除了棘肽 S4（DS4）之外，没有相当大的溶血作用，DS4 表现出强大的细胞毒性作用。因此，我们合成了几种 DS4 的类似物，试图找到溶血作用较弱但具有显著生物活性的分子。在这项研究中，我们通过引入天然序列的 C 末端和 N 末端氨基酸缺失来进行截短肽的合成。与亲本肽相比，所有肽类似物首先在人红细胞上进行测试，以确定其细胞毒性，其次在多药耐药菌上进行测试，以确定 MICs，最后在结肠癌细胞系 SW620 上进行 MTT 测试，以研究抗增殖作用。我们的结果表明，一方面，天然肽的 N 端对于肽的抗菌活性和抗增殖作用是必要的。另一方面，在 C 末端断裂的序列中，溶血活性更为明显。
