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Synthesis and cellular penetration properties of new phosphonium based cationic amphiphilic peptides†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-05-09 00:00:00 , DOI: 10.1039/c8md00113h Ezequiel Silva Nigenda 1 , Tobias M Postma 1 , Mohammed Hezwani 1 , Alin Pirvan 1 , Susan Gannon 1 , Carol-Anne Smith 2 , Mathis Riehle 2 , Rob M J Liskamp 1
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-05-09 00:00:00 , DOI: 10.1039/c8md00113h Ezequiel Silva Nigenda 1 , Tobias M Postma 1 , Mohammed Hezwani 1 , Alin Pirvan 1 , Susan Gannon 1 , Carol-Anne Smith 2 , Mathis Riehle 2 , Rob M J Liskamp 1
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A new category of phosphonium based cationic amphiphilic peptides has been developed and evaluated as potential antimicrobial peptides and cell penetrating peptides. The required building blocks were conveniently accessible from cysteine and could be applied in a solid phase peptide synthesis protocol for incorporation into peptide sequences. Evaluation of the antimicrobial properties and cellular toxicity of these phosphonium based peptides showed that these “soft” cationic side-chain containing peptides have poor antimicrobial properties and most of them were virtually non toxic (on HEK cells tested at 256 and 512 μM) and non-haemolytic (on horse erythrocytes tested at 512 μM), hinting at an interesting potential application as cell penetrating peptides. This possibility was evaluated using fluorescent peptide derivatives and showed that these phosphonium based peptide derivatives were capable of entering HEK cells and depending on the sequence confined to specific cellular areas.
中文翻译：
新型鏻基阳离子两亲肽的合成和细胞渗透特性†
一类新的基于磷的阳离子两亲肽已被开发并评估为潜在的抗菌肽和细胞穿透肽。所需的构建模块可以方便地从半胱氨酸中获得，并且可以应用于固相肽合成方案中以掺入肽序列中。对这些基于磷鎓的肽的抗菌特性和细胞毒性的评估表明，这些含有“软”阳离子侧链的肽具有较差的抗菌特性，并且其中大多数实际上是无毒的（在 256 和 512 μM 下测试的 HEK 细胞上）并且无毒。 -溶血性（在 512 μM 下测试的马红细胞），暗示着作为细胞穿透肽的有趣的潜在应用。使用荧光肽衍生物评估了这种可能性，并表明这些基于磷鎓的肽衍生物能够进入HEK细胞，并且取决于限制在特定细胞区域的序列。
更新日期：2018-05-09
中文翻译：
新型鏻基阳离子两亲肽的合成和细胞渗透特性†
一类新的基于磷的阳离子两亲肽已被开发并评估为潜在的抗菌肽和细胞穿透肽。所需的构建模块可以方便地从半胱氨酸中获得，并且可以应用于固相肽合成方案中以掺入肽序列中。对这些基于磷鎓的肽的抗菌特性和细胞毒性的评估表明，这些含有“软”阳离子侧链的肽具有较差的抗菌特性，并且其中大多数实际上是无毒的（在 256 和 512 μM 下测试的 HEK 细胞上）并且无毒。 -溶血性（在 512 μM 下测试的马红细胞），暗示着作为细胞穿透肽的有趣的潜在应用。使用荧光肽衍生物评估了这种可能性，并表明这些基于磷鎓的肽衍生物能够进入HEK细胞，并且取决于限制在特定细胞区域的序列。
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