Hu Wan-Ning, Jiao Wen-Jing, Ma Zhi, Dong Na, Ma Qing-Quan, Shao Chang-Xuan, Shan An-Shan
Laboratory of Molecular Nutrition and Immunity, Institute of Animal Nutrition, Northeast Agricultural University, Harbin, 150030, P.R. China.
Protein Pept Lett. 2013 Nov;20(11):1189-99. doi: 10.2174/09298665113209990042.
In this study, the influence of isoleucine and arginine on the biological activity and peptide-membrane interactions of linear avian β-defensin-4 (RL38) analogs was investigated. Results of biological activities showed that the antimicrobial activities of AvBD-4 analogs were closely related to hydrophobicity and amphipathicity. The peptide GLI19 with high hydrophobicity value and amphipathicity displayed broad spectrum antimicrobial activity against both gram-negative and gram-positive, whereas GLR19 with increasing multiple charges only exhibited activity against gram-negative. The interaction between peptides and the liposome membrane demonstrated that the peptides preferentially bound to negatively charged phospholipids over zwitterionic phospholipids, which supported the antimicrobial activity data. The outer membranes assay further demonstrated that GLI19 had a greater capacity than the other tested peptides to penetrate the cell membrane at a low concentration. Collectively, the peptides derived from the bactericidal domain of linear β- defensins by truncation and hydrophobic amino acid substitution may be effective high-potential antibacterial agents.
在本研究中，研究了异亮氨酸和精氨酸对线性禽β-防御素-4（RL38）类似物的生物活性及肽-膜相互作用的影响。生物活性结果表明，禽β-防御素-4类似物的抗菌活性与疏水性及两亲性密切相关。具有高疏水性值和两亲性的肽GLI19对革兰氏阴性菌和革兰氏阳性菌均表现出广谱抗菌活性，而带电荷增加的GLR19仅对革兰氏阴性菌有活性。肽与脂质体膜之间的相互作用表明，肽优先结合带负电荷的磷脂而非两性离子磷脂，这支持了抗菌活性数据。外膜试验进一步表明，在低浓度下，GLI19穿透细胞膜的能力比其他测试肽更强。总体而言，通过截短和疏水氨基酸取代从线性β-防御素的杀菌结构域衍生的肽可能是有效的高潜力抗菌剂。
