Investigation on Single-strand Peptide-miRNA Conjugate Encapsulated by Cytosine-based Amphiphile

• 作 者: Yuan Ma Wenting Zhao Shuang Liu Chao Wang Zhu Guan Zhenjun Yang
• 机 构: State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking Univer
• 出 处: 中国化学会第十届全国化学生物学学术会议
• 发表日期: 2017年10期
• 关键词: ss-miRNA peptide conjugation DNCA antiproliferative activity

　　Nucleic acid drug is challenging for their delivery efficiency,and cationic lipid is generally cytotoxic.In this paper,we described a novel cytosine-based amphiphile(DNCA)could bound to single-stranded miRNA(ss-miRNA)ss-miR-122,obviously enhanced the cellular uptake of the nanoparticles and stability in serum with low cytotoxicity.In addition,the peptide conjugation of ss-miR-122(p-ss-miR-122)might regulate the self-assembly process encapsulated by DNCA,which promoted the formation of suitable nanoparticles and enhanced the gene silencing and antiproliferative activity.