关键词: amphipathic structure cell-penetrating peptide helical structure plasmid DNA (pDNA) delivery unnatural amino acid

Mesh : Cell-Penetrating Peptides / chemistry Plasmids Humans DNA / chemistry RNA, Small Interfering / chemistry administration & dosage Glycine / chemistry Transfection HeLa Cells Cell Survival / drug effects

来  源:   DOI:10.1248/cpb.c24-00221

Abstract:
Cell-penetrating peptides (CPPs) serve as potent vehicles for delivering membrane-impermeable compounds, including nucleic acids, into cells. In a previous study, we reported the successful intracellular delivery of small interfering RNAs (siRNAs) with negligible cytotoxicity using a peptide containing an unnatural amino acid (dipropylglycine). In the present study, we employed the same seven peptides as the previous study to evaluate their efficacy in delivering plasmid DNA (pDNA) intracellularly. Although pDNA and siRNA are nucleic acids, they differ in size and biological function, which may influence the optimal peptide sequences for their delivery. Herein, three peptides demonstrated effective pDNA transfection abilities. Notably, only one of the three peptides previously exhibited efficient gene-silencing effect with siRNA. These findings validate our hypothesis and offer insights for the personalized design of CPPs for the delivery of pDNA and siRNA.
摘要:
细胞穿透肽(CPPs)作为强效载体,用于递送膜不可渗透的化合物,包括核酸,进入细胞。在之前的研究中,我们报道了使用含有非天然氨基酸(二丙基甘氨酸)的肽,细胞毒性可忽略不计的小干扰RNA(siRNA)的成功细胞内递送.在本研究中,我们使用了与先前研究相同的7种肽来评估其在细胞内递送质粒DNA(pDNA)方面的功效。虽然pDNA和siRNA是核酸,它们的大小和生物学功能不同,这可能会影响其递送的最佳肽序列。在这里,三种肽证明了有效的pDNA转染能力。值得注意的是,这三种肽中只有一种以前用siRNA表现出有效的基因沉默效果。这些发现验证了我们的假设,并为pDNA和siRNA递送的CPPs的个性化设计提供了见解。
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