Synthesis of a polyamidoamine dendron-bearing lipid having sugar moieties and its use for preparation of nonviral gene vectors

Synthesis of a polyamidoamine dendron-bearing lipid having sugar moieties and its use for preparation of nonviral gene vectors
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DOI:
10.1007/s11164-009-0083-z
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发表时间:
2009-10
影响因子:
3.3
通讯作者:
Toshinari Takahashi;E. Yuba;C. Kojima;Atsushi Harada;K. Kono
Toshinari Takahashi;E. Yuba;C. Kojima;Atsushi Harada;K. Kono
中科院分区:
化学3区
文献类型:
--
作者:
Toshinari Takahashi;E. Yuba;C. Kojima;Atsushi Harada;K. Kono

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到目前为止,我们已经开发了一种新型的阳离子脂质,它由一个胺封端的聚(酰胺胺)树枝化和两个长的烷基链。在本研究中,我们设计了一种在树枝状分子末端修饰糖基作为配体的树枝状分子脂质(DL),以提高转染活性。我们在DL的每个树突状分支的末端结合乳糖酸以产生半乳糖部分附着的DL(Gal-DL)。含Gal-DL的脂质复合物对HepG 2细胞的转染有增强作用。此外,Gal-DL显着促进包括聚乙二醇连接的树枝状脂质(PEG-DL)在内的脂复合物的转染活性。
We have so far developed a new type of cationic lipid that consists of an amine-terminated poly(amidoamine) dendron and two long alkyl chains. In this study, we designed a dendron-bearing lipid (DL) modified with sugar moieties as the ligand at the terminal groups of the dendron to improve the transfection activities. We combined lactobionic acid at the end of every dendritic branch of the DL to produce galactose moieties-attached DL (Gal-DL). The lipoplexes containing Gal-DL exhibited enhancement of transfection of HepG2 cells. Moreover, Gal-DL significantly promoted the transfection activity of the lipoplexes including poly(ethylene glycol)-attached dendron-bearing lipid (PEG-DL).