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首页> 外文期刊>The FEBS journal >Comparative mode of action of novel hybrid peptide CS-1a and its rearranged amphipathic analogue CS-2a
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Comparative mode of action of novel hybrid peptide CS-1a and its rearranged amphipathic analogue CS-2a

机译：新型杂合肽CS-1a及其重排的两亲类似物CS-2a的作用比较模式

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摘要

Cell selective, naturally occurring, host defence cationic peptides present a good template for the design of novel peptides with the aim of achieving a short length with improved antimicrobial potency and selectivity. A novel, short peptide CS-1a (14 residues) was derived using a sequence hybridization approach on sarcotoxin I (39 residues) and cecropin B (35 residues). The sequence of CS-1a was rearranged to enhance amphipathicity with the help of a Schiffer–Edmundson diagram to obtain CS-2a. Both peptides showed good antibacterial activity in the concentration range 4–16 lgmL 1 against susceptible as well as drug-resistant bacterial strains, including the clinically relevant pathogens Acenatobacter sp. and methicillin-resistant Staphylococcus aureus. The major thrust of these peptides is their nonhaemolytic activity against human red blood cells up to a high concentration of 512 lgmL 1 . Compared to CS-1a, amphipathic peptide CS-2a showed a more pronounced a-helical conformation, along with a better membrane insertion depth in bacterial mimic 1,2-dipalmitoylsn-glycero-3- phosphocholine/1,2-dipalmitoyl-sn-glycero-3-phospho-(1′-rac-glycerol) small unilamellar vesicles. With equivalent lipid-binding af?nity, the two peptides assumed different pathways of membrane disruption, as demonstrated by calcein leakage and the results of transmission electron microscopy on model bacterial mimic large unilamellar vesicles. Extending the work from model membranes to intact Escherichia coli cells, differences in membrane perturbation were visible in microscopic images of peptide-treated E. coli. The present study describes two novel short peptides with potent activity, cell selectivity and divergent modes of action that will aid in the future design of peptides with better therapeutic potential.
机译：细胞选择性的天然存在的宿主防御阳离子肽为设计新型肽提供了一个很好的模板，目的是实现较短的长度，同时具有增强的抗菌效力和选择性。使用序列杂交方法，在肌毒素I（39个残基）和天蚕素B（35个残基）上获得了一种新颖的短肽CS-1a（14个残基）。 CS-1a的序列经过重排以增强两亲性，借助Schiffer-Edmundson图获得CS-2a。两种肽在4-16 lgmL 1的浓度范围内均表现出良好的抗菌活性，对易感和耐药菌菌株，包括与临床相关的病原菌Acenatobacter sp。和耐甲氧西林的金黄色葡萄球菌。这些肽的主要推力是它们对人红细胞的非溶血活性，浓度高达512 lgmL 1。与CS-1a相比，两亲性肽CS-2a在细菌模拟的1,2-二棕榈酰sn-glycero-3-磷酸胆碱/ 1,2-二棕榈酰-sn-中表现出更明显的a-螺旋构象，以及更好的膜插入深度。甘油-3-磷酸-（1'-rac-甘油）单层小囊泡。在等效的脂质结合亲和力下，这两种肽假定了不同的膜破坏途径，如钙黄绿素泄漏和模型细菌模拟的大单层囊泡的透射电子显微镜结果所证明。将工作从模型膜扩展到完整的大肠杆菌细胞，在肽处理的大肠杆菌的显微图像中可见膜扰动的差异。本研究描述了两种新型的短肽，它们具有强大的活性，细胞选择性和不同的作用方式，将有助于未来设计具有更好治疗潜力的肽。

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