Design and Synthesis of Amphiphilic Basic Peptides with Antibacterial Activity and Their Interaction with Model Membrane
作者:Hisakazu Mihara、Tatsuhiko Kanmera、Mutsuo Yoshida、Sannamu Lee、Haruhiko Aoyagi、Tetsuo Kato、Nobuo Izumiya
DOI:10.1246/bcsj.60.697
日期:1987.2
Twelve peptides having 4 to 6 basic amino acid residues in the hydrophobic amino acid sequence were designed and synthesized by the solution method to find peptides with potential activity against Gram-positive and -negative bacteria. CD study of the peptides demonstrated that they formed α-helical structures in the presence of phospholipid liposomes consequently to have amphiphilic property along
通过溶液法设计并合成了疏水氨基酸序列中具有4至6个碱性氨基酸残基的12个肽,以寻找对革兰氏阳性和阴性细菌具有潜在活性的肽。肽的 CD 研究表明,它们在磷脂脂质体存在下形成 α-螺旋结构,因此沿螺旋轴具有两亲性。这些肽还诱导了磷脂囊泡中染料羧基荧光素的渗漏,表明这些肽具有扰乱膜结构的能力。这些肽对革兰氏阳性菌显示出抗菌活性,其中一些肽对革兰氏阴性菌也有活性。讨论了合成肽的结构与抗菌活性之间的关系。