Novel Lipid-Oligonucleotide Conjugates Containing Long-Chain Sulfonyl Phosphoramidate Groups: Synthesis and Biological Properties

被引:10
|
作者
Derzhalova, Alina [1 ,2 ]
Markov, Oleg [2 ]
Fokina, Alesya [1 ,3 ]
Shiohama, Yasuo [4 ]
Zatsepin, Timofei [5 ,6 ]
Fujii, Masayuki [7 ]
Zenkova, Marina [2 ]
Stetsenko, Dmitry [1 ,3 ]
机构
[1] Novosibirsk State Univ, Dept Phys, Novosibirsk 630090, Russia
[2] Russian Acad Sci, Siberian Branch, Inst Chem Biol & Fundamental Med, Novosibirsk 630090, Russia
[3] Russian Acad Sci, Inst Cytol & Genet, Siberian Branch, Novosibirsk 63090, Russia
[4] Univ Ryukyus, Trop Biosphere Res Ctr, Nishihara, Okinawa 9030213, Japan
[5] Skolkovo Inst Sci & Technol, Innovat Ctr Skolkovo, Moscow 121205, Russia
[6] Lomonosov Moscow State Univ, Dept Chem, Moscow 119991, Russia
[7] Kindai Univ, Dept Biol & Environm Chem, Iizuka, Fukuoka 8208555, Japan
来源
APPLIED SCIENCES-BASEL | 2021年 / 11卷 / 03期
基金
俄罗斯科学基金会; 俄罗斯基础研究基金会;
关键词
therapeutic nucleic acid; drug delivery; nanoparticles; cytotoxicity; macrophages; cellular uptake; small interfering RNA; multiple sclerosis; repulsive guidance molecule a; CELLULAR UPTAKE; ANTISENSE OLIGONUCLEOTIDES; RNA; DERIVATIVES; INHIBITION; EFFICIENCY; DELIVERY; THERAPY; SIRNAS; GENE;
D O I
10.3390/app11031174
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
New lipid conjugates of DNA and RNA incorporating one to four [(4-dodecylphenyl)sulfonyl]phosphoramidate or (hexadecylsulfonyl)phosphoramidate groups at internucleotidic positions near the 3 ' or 5 '-end were synthesized and characterized. Low cytotoxicity of the conjugates and their ability to be taken up into cells without transfection agents were demonstrated. Lipid-conjugated siRNAs targeting repulsive guidance molecules a (RGMa) have shown a comparable gene silencing activity in PK-59 cells to unmodified control siRNA when delivered into the cells via Lipofectamine mediated transfection.
引用
收藏
页码:1 / 15
页数:15
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