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破坏非极性面上疏水残基之间的相互作用是降低溶血作用并增强α-螺旋两亲性肽抗菌活性的关键决定因素。

Disruption of interactions between hydrophobic residues on nonpolar faces is a key determinant in decreasing hemolysis and increasing antimicrobial activities of α-helical amphipathic peptides.

作者信息

Son Mieon, Lee Yuri, Hwang Heeyong, Hyun Soonsil, Yu Jaehoon

机构信息

Department of Chemistry & Education, Seoul National University, Gwanak-ro 1, Gwanak-gu, Seoul 151-742 (Korea).

出版信息

ChemMedChem. 2013 Oct;8(10):1638-42. doi: 10.1002/cmdc.201300264. Epub 2013 Jul 25.

DOI:10.1002/cmdc.201300264
PMID:23894079
Abstract

To design antimicrobial peptides with decrease pore-forming activity in eukaryotic (host) membranes, an amphipathic α-helical model peptide composed of Leu and Lys was modified to probe the balance in antimicrobial and hemolytic activities. Among analogues with broken hydrophobic interactions, L8N derivative exhibited an 8000-fold decrease in hemolytic activity and an eightfold improvement in antimicrobial activity, affording a 64 000-fold increase in therapeutic index against E. coli.

摘要

为了设计在真核（宿主）膜中具有降低成孔活性的抗菌肽，对由亮氨酸和赖氨酸组成的两亲性α-螺旋模型肽进行修饰，以探究抗菌活性和溶血活性之间的平衡。在疏水相互作用被破坏的类似物中，L8N衍生物的溶血活性降低了8000倍，抗菌活性提高了8倍，对大肠杆菌的治疗指数提高了64000倍。

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