Short Photoswitchable Antibacterial Peptides.,ChemMedChem

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Short Photoswitchable Antibacterial Peptides.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-06-17 , DOI: 10.1002/cmdc.202000280
Yuan Qi Yeoh ₁ , John R Horsley ₁ , Jingxian Yu ₁ , Steven W Polyak _{2,

3} , Blagojce Jovcevski ₄ , Andrew D Abell ₁

Affiliation

Three photoswitchable tetrapeptides, based on a known synthetic antibacterial, were designed and synthesized to determine activity against Staphylococcus aureus. Each peptide contains an azobenzene photoswitch incorporated into either the N‐terminal side chain (1), C‐terminal side chain (2), or the C‐terminus (3) to allow reversible switching between cis‐ and trans‐enriched photostationary states. Biological assays revealed that the C‐terminus azobenzene (3) possessed the most potent antibacterial activity, with an MIC of 1 μg/mL. In this study, net positive charge, hydrophobicity, position of the azobenzene, secondary structure, and amphiphilicity were all found to contribute to antibacterial activity, with each of these factors likely facilitating the peptide to disrupt the negatively charged bacterial lipid membrane. Hence, these short photoswitchable antibacterial tetrapeptides provide insights for the future design and synthesis of antibiotics targeting S. aureus.

中文翻译：

短光开关抗菌肽。

设计并合成了三种基于已知合成抗菌剂的可光转换四肽，以确定其对金黄色葡萄球菌的活性。每个肽都包含一个掺入N末端侧链（1），C末端侧链（2）或C末端（3）的偶氮苯光开关，以允许在富顺式和反式富集的光平稳状态之间可逆转换。生物学分析表明C末端偶氮苯（3）具有最强的抗菌活性，MIC为1μg/ mL。在这项研究中，发现净净正电荷，疏水性，偶氮苯的位置，二级结构和两亲性均有助于抗菌活性，所有这些因素均可能促进肽破坏带负电荷的细菌脂质膜。因此，这些短的可光转换的抗菌四肽为靶向金黄色葡萄球菌的抗生素的未来设计和合成提供了见识。

更新日期：2020-08-21

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