New Amphiphilic Amino Acid Derivatives for Efficient DNA Transfection <i>in Vitro</i>

• 作者: Antonella Giorello Carolina M. I. Veaute Claudio C. Prieto Diana M. Müller Lucía C. Pe?a María F. Argara?á María M. De Zan Sebastián Antu?a
• 来源期刊: 化学工程与科学期刊(英文)
• 学科: 医学
• 关键词: AMPHIPHILE N-Acylated CYSTEINE Gemini ORNITHINE Transfection
• 年，卷（期）: 2017,（2）
• 页码范围: 191-205
• 页数: 15页
• 分类号: R73

摘要

Nucleic acids-based therapies have recently developed as next-generation agents for treating and preventing viral infection, cancer, and genetic disorders, but their use is still limited due to its relatively poor delivery into targeted cells. We designed and synthesized new amphiphilic amino acid derivatives (cysteine-based) of low molecular weight, formed by the same pentapeptide (AG2: WWCOO) N-acylated, with different hydrophobic chains containing from 12 to 18 carbons, named AG2-Cn (N), which dimerize by oxidation in the presence of pLenti-CMV-GFP Puro plasmid (P) in the respective gemini. We determined transfection efficiency, critical micelle concentration, particle size, ζ-potential and cytotoxicity for the derivatives obtained. We found that all the synthesized compounds were active for DNA delivery and had greater ability to transfect CHO-K1 cells. In particular, AG2-C18 is a promising carrier for gene delivery because it showed no cytotoxicity and its activity was greater than or equal to the commercial actives currently used.