Amphiphilic small peptides for delivery of plasmid DNAs and siRNAs,Chemical Biology & Drug Design

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Amphiphilic small peptides for delivery of plasmid DNAs and siRNAs
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-13 , DOI: 10.1111/cbdd.13122
Eun-Kyoung Bang ₁ , Hanna Cho ₂ , Sean S.-H. Jeon ₂ , Na Ly Tran _{1,

3} , Dong-Kwon Lim ₂ , Wooyoung Hur ₁ , Taebo Sim _{1,

2}

Affiliation

Although various delivery systems for nucleic acids have been reported, development of an efficient and non‐toxic delivery carrier is still a key subject for gene therapy. To find new efficient delivery carriers for nucleic acids, we synthesized amphiphilic peptides composed of a guanidino group, an oleyl group, and a cysteine. We prepared both linear and branched types of peptides and found that the linear peptides were superior to the branched peptides as nucleic acid carriers. Our study also suggested that the intermolecular cysteine disulfides might allow the linear peptides to form the optimal particle sizes with nucleic acids for cellular uptake. The incorporation of a benzoyl group to the linear peptide gave rise to smaller, less suitable particle size with plasmid DNA, which greatly reduced the efficiency of plasmid DNA delivery. On the other hand, the benzoyl modification maintained the optimal particle size with siRNA, and interestingly it significantly enhanced the siRNA delivery. The higher efficiency is because the hydrophobicity from the benzoyl group might assist in interacting with the hydrophobic cell membrane. This demonstrates that a small structural change can modulate the preference of the carriers. Our study may provide an insight designing efficient delivery carriers.

中文翻译：

两亲小肽，用于传递质粒DNA和siRNA

尽管已经报道了各种核酸递送系统，但是开发高效无毒的递送载体仍然是基因治疗的关键课题。为了找到新的高效核酸递送载体，我们合成了由胍基，油基和半胱氨酸组成的两亲性肽。我们制备了线性和支链类型的肽，发现线性肽作为核酸载体优于支链肽。我们的研究还表明，分子间半胱氨酸二硫键可能使线性肽与核酸形成最佳粒径，以供细胞摄取。苯甲酰基基团结合到线性肽中导致质粒DNA的粒径变小，不太合适，这大大降低了质粒DNA的输送效率。另一方面，苯甲酰基修饰可通过siRNA保持最佳粒径，有趣的是，它显着增强了siRNA的传递。较高的效率是因为来自苯甲酰基的疏水性可能有助于与疏水性细胞膜相互作用。这表明小的结构变化可以调节载体的偏好。我们的研究可能为设计高效的运送载体提供见解。

更新日期：2017-11-13

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