LIPPSO, Department of Chemistry, University of Girona, Campus Montilivi, E-17071 Girona, Spain.
Peptides. 2012 Jan;33(1):9-17. doi: 10.1016/j.peptides.2011.12.003. Epub 2011 Dec 16.
We designed and prepared peptidotriazoles based on the antimicrobial peptide BP100 (LysLysLeuPheLysLysIleLeuLysTyrLeu-NH(2)) by introducing a triazole ring in the peptide backbone or onto the side chain of a selected residue. These compounds were screened for their in vitro growth inhibition of bacterial and fungal phytopathogens, and for their cytotoxic effects on eukaryotic cells and tobacco leaves. Their proteolytic susceptibility was also analyzed. The antibacterial activity and the hemolysis were influenced by the amino acid that was modified with the triazole as well as by the absence of presence of a substituent in this heterocyclic ring. We identified sequences active against the bacteria Xanthomonas axonopodis pv. vesicatoria, Erwinia amylovora, Pseudomonas syringae pv. syringae (MIC of 1.6-12.5 μM), and against the fungi Fusarium oxysporum (MIC<6.2-12.5 μM) with low hemolytic activity (0-23% at 50 μM), high stability to protease digestion and no phytotoxicity. These peptidotriazoles constitute good candidates to design new antimicrobial agents.
我们设计并制备了基于抗菌肽 BP100（LysLysLeuPheLysLysIleLeuLysTyrLeu-NH2）的肽三唑，方法是在肽主链或选定残基的侧链上引入三唑环。这些化合物在体外筛选了对细菌和真菌植物病原体的生长抑制作用，以及对真核细胞和烟草叶片的细胞毒性作用。还分析了它们的蛋白水解易感性。三唑修饰的氨基酸以及该杂环中是否存在取代基会影响抗菌活性和溶血。我们鉴定了针对 Xanthomonas axonopodis pv. vesicatoria、Erwinia amylovora、Pseudomonas syringae pv. syringae（MIC 为 1.6-12.5 μM）细菌和 Fusarium oxysporum（MIC<6.2-12.5 μM）真菌具有活性的序列，溶血活性低（50 μM 时为 0-23%），对蛋白酶消化稳定，无植物毒性。这些肽三唑是设计新型抗菌剂的良好候选物。
