Combinatorial library of lipidoids for in vitro DNA delivery.

Combinatorial library of lipidoids for in vitro DNA delivery.
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DOI:
10.1021/bc200572w
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发表时间:
2012-01-18
影响因子:
4.7
通讯作者:
Xu, Qiaobing
Xu, Qiaobing
中科院分区:
化学2区
文献类型:
--
作者:
Sun, Shuo;Wang, Ming;Knupp, Sarah A.;Soto-Feliciano, Yadira;Hu, Xiao;Kaplan, David L.;Langer, Robert;Anderson, Daniel G.;Xu, Qiaobing

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构建了一个类胡萝卜素组合文库,并研究了其体外基因递送。通过使市售胺与亲脂性丙烯酸酯、丙烯酰胺或环氧化物反应来合成类胡萝卜素文库。衍生自胺86(N,N-双(2-羟乙基)乙二胺)和胺87(N-(3-氨基丙基)二乙胺)的类脂质在DNA递送中显示出高效率,其中一些具有比Lipofectamine 2000更高的转染效率,Lipofectamine 2000是用于体外基因递送的常用商业金标准。关于化学结构的小变化和所产生的体外DNA递送效率,进一步研究了类胡萝卜素之间的结构-活性关系。由于这些类胡萝卜素易于合成,并且不需要用于有效DNA递送的共脂质,因此它们可以为其他常用的商业基因递送载体提供廉价但有效的替代品。
A combinatorial library of lipidoids was constructed and studied for in vitro gene delivery. The library of lipidoids was synthesized by reacting commercially available amines with lipophilic acrylates, acrylamides, or epoxides. Lipidoids derived from amine 86 (N,N-Bis(2-hydroxyethyl)ethylene diamine) and amine 87 (N-(3-aminopropyl)diethaneamine) showed high efficiency in DNA delivery, some with a higher transfection efficiency than Lipofectamine 2000, a commonly used commercial gold standard for in vitro gene delivery. The structure-activity relationship between the lipidoids was further studied with respect to small variations in chemical structures and the resulting efficiency in DNA delivery in vitro. Since these lipidoids are easy to synthesize and do not require a co-lipid for efficient DNA delivery, they could offer an inexpensive but effective alternative to other commonly used commercial gene delivery carriers.
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