LIPPSO, Department of Chemistry, University of Girona, Campus Montilivi, Girona, Spain.
Laboratory of Plant Pathology, Institute of Food and Agricultural Technology-CIDSAV-XaRTA, University of Girona, Campus Montilivi, Girona, Spain.
Peptides. 2019 Feb;112:85-95. doi: 10.1016/j.peptides.2018.11.009. Epub 2018 Nov 30.
Recent strong restrictions on the use of pesticides has prompted the search for safer alternatives, being antimicrobial peptides promising candidates. Herein, with the aim of identifying new agents, 15 peptides reported as plant defense elicitors, promiscuous, multifunctional or antimicrobial were selected and tested against six plant pathogenic bacteria of economic importance. Within this set, KSL-W (KKVVFWVKFK-NH) displayed high antibacterial activity against all the tested pathogens, low hemolysis and low phytotoxicity in tobacco leaves. This peptide was taken as a lead and 49 analogues were designed and synthesized, including N-terminal deletion sequences, peptides incorporating a d-amino acid and lipopeptides. The screening of these sequences revealed that a nine amino acid length was the minimum for activity. The presence of a d-amino acid significantly decreased the hemolysis and endowed KSL-W with the capacity to induce the expression of defense-related genes in tomato plants. The incorporation of an acyl chain led to sequences with high activity against Xanthomonas strains, low hemolysis and phytotoxicity. Therefore, this study demonstrates that KSL-W constitutes an excellent candidate as new agent to control plant diseases and can be considered as a lead to develop derivatives with multifunctional properties, including antimicrobial and plant defense elicitation.
最近对农药使用的严格限制促使人们寻找更安全的替代品,而抗菌肽则是很有前途的候选物。在此,为了寻找新的抗菌药物,我们选择了 15 种被报道具有植物防御诱导活性、多功能或抗菌活性的肽进行测试,以评估其对 6 种具有经济重要性的植物病原菌的抗菌活性。在这些肽中,KSL-W(KKVVFWVKFK-NH)对所有测试的病原菌均表现出高抗菌活性,对烟草叶片的溶血活性和植物毒性较低。该肽被作为先导化合物,设计并合成了 49 种类似物,包括 N 端缺失序列、包含 D-氨基酸的肽和脂肽。这些序列的筛选结果表明,九肽长度是发挥活性的最小长度。D-氨基酸的存在显著降低了溶血活性,并使 KSL-W 具有诱导番茄植物防御相关基因表达的能力。酰基链的引入导致对黄单胞菌菌株具有高活性、低溶血活性和低植物毒性的序列。因此,本研究表明 KSL-W 是一种很有前途的控制植物病害的新候选物,可作为开发具有多功能特性的衍生物的先导化合物,包括抗菌和植物防御诱导活性。