Synthesis and biological activity of lipophilic analogs of the cationic antimicrobial active peptide anoplin
作者:Kostas Chionis、Dimitrios Krikorian、Anna-Irini Koukkou、Maria Sakarellos-Daitsiotis、Eugenia Panou-Pomonis
DOI:10.1002/psc.2939
日期:2016.11
order to investigate how these modifications affect their antimicrobial activity. These cationic analogs exhibited higher antimicrobial activity than the native peptide; they are also nontoxic at their minimum inhibitory concentration (MIC) values and resistant to enzymatic degradation. The substituted peptide GLLKF5IKK8LL‐NH2 exhibited high activity against Gram‐negative bacterium Zymomonas mobilis (MIC = 7 µg/ml)
Anoplin是一种短的天然阳离子抗微生物肽,它来源于单独的黄蜂Anoplius samariensis的毒液囊。由于序列短,G 1 LLKR 5 IKT 8 LL-NH 2,因此非常适合用于研究测试。在这项研究中,制备了新型的Anoplin类似物,并检查了它们的抗微生物,溶血活性和蛋白水解稳定性。在氨基酸Gly 1,Arg 5和Thr 8中引入了特定的取代基为了研究这些修饰如何影响其抗菌活性,在N末端具有不同长度的亲脂基团和亲脂基团。这些阳离子类似物显示出比天然肽更高的抗菌活性。它们在最小抑菌浓度(MIC)值下也无毒,并且对酶促降解具有抵抗力。取代的肽GLLKF 5 IKK 8 LL-NH 2对革兰氏阴性菌运动发酵单胞菌具有高活性(MIC = 7 µg / ml),并且在其N末端插入辛酸,癸酸和十二酸残基会增加对革兰氏阳性和革兰氏阴性细菌的抗菌活性(MIC = 5 µg / ml)。通过