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首页> 外文期刊>Journal of medical bacteriology. >Solid Phase Chemical Synthesis and Structure - Activity Study of Brevinin - 2R and Analogues as Antimicrobial Peptides
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Solid Phase Chemical Synthesis and Structure - Activity Study of Brevinin - 2R and Analogues as Antimicrobial Peptides

机译：固相化学合成与结构-Brevinin-2R及其抗菌肽类似物的活性研究。

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Background: Brevinin-2R, as 25 amino acids peptide of the skin of Rana ridibunda frog, possesses potent antimicrobial and low hemolytic activity. It has an N-terminal hydrophilic region and a C-terminal loop that is delineated by an intra-disulfide bridge. In our study, Brevinin-2R and its diastereomer as well as its cyclic analogue were synthesized and characterized in order to investigate its structural features and biological implications.Methods: MIC determination is based on the recommended classical method of national comittee for labratory safety standard (NCLSS) and standard by Hancock With some change on cationic peptides. In this study All bacterial strains were obtained from Industrial-Scientific Research center.Results: Both analogues showed lower antimicrobial activities compared to Brevinin-2R. In spite of Brevinin-2R peptide which shows low hemolytic activity, these analogues failed to show any hemolytic activity even at higher concentrations (up to 400 μ g/ml). Based on proteolytic stability measurements,diastereomer and cyclic analogues displayed 90% and 60% residual antimicrobial activity, respectively, while antimicrobial activity of Brevinin-2R was 20%. The CD analysis revealed that amphipathic α-helical conformation of the synthesized peptides is involved in antimicrobial effects.Conclusion: CD studies and HPLC based measurement of retention time using a reverse phase column indicated that the Brevinin-2R can form an amphipathic loop resulting in an enhanced hydrophobicity. The hemolytic activity of Brevinin-2R and its analogues appeared to correlate with the retention time as well as the α-helicity. Accordingly, it seems that the combination of incorporating of D-amino acids into lytic peptides and their cyclization may result in developing new antimicrobial peptides with improved properties for treating infectious diseases.
机译：背景：Brevinin-2R是蛙蛙蛙皮肤中25个氨基酸的肽，具有强大的抗菌作用和低溶血活性。它具有一个N端亲水区和一个C端环，该环由二硫键构成。在我们的研究中，合成并表征了Brevinin-2R及其非对映异构体及其环状类似物，以研究其结构特征和生物学意义。方法：MIC的测定是基于国家实验室推荐的经典方法制定的实验室安全标准（ NCLSS）和Hancock的标准品。在本研究中，所有细菌菌株均从工业科学研究中心获得。结果：与Brevinin-2R相比，两种类似物均显示出较低的抗菌活性。尽管Brevinin-2R肽显示出低溶血活性，但即使在较高浓度（高达400μg / ml）下，这些类似物也没有表现出任何溶血活性。根据蛋白水解稳定性测量，非对映异构体和环状类似物分别显示出90％和60％的残留抗菌活性，而Brevinin-2R的抗菌活性为20％。 CD分析表明，合成肽的两亲性α-螺旋构象与抗菌作用有关。结论：CD研究和基于HPLC反相色谱柱的保留时间测量表明，Brevinin-2R可以形成两亲环，导致疏水性增强。 Brevinin-2R及其类似物的溶血活性似乎与保留时间以及α-螺旋有关。因此，似乎将D-氨基酸掺入到裂解肽中和它们的环化的组合可以导致开发具有改善的用于治疗传染病的特性的新的抗菌肽。

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