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Coordinative Amphiphiles as Tunable siRNA Transporters

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Title
Coordinative Amphiphiles as Tunable siRNA Transporters
Author(s)
Jin Bum Kim; Yeong Mi Lee; Jooyeon Ryu; Eunji Lee; Won Jong Kim; Gyochang Keum; Eun Kyoung Bang
Publication Date
2016-08
Journal
BIOCONJUGATE CHEMISTRY, v.27, no.8, pp.1850 - 1856
Publisher
AMER CHEMICAL SOC
Abstract
In this study, we developed coordinative amphiphiles for use as novel siRNA transporters. As a modification of a conventional cationic lipid structure, we replaced the cationic head with zinc(II)-dipicolylamine complex (Zn/DPA) as a phosphate directing group, and used various membrane-directing groups in the place of the hydrophobic tails. These simple amphiphiles are readily synthesized and easy to modify. The Zn/DPA head groups bind to the phosphate backbones of siRNAs, and to our surprise, they prevented the enzymatic degradation of siRNAs by RNase A. Interestingly, the Zn/DPA head itself exhibited moderate transfection efficiency, and its combination with a membrane-directing group-oleoyl (CA1), pyrenebutyryl (CA2), or biotin (CA3)-enhanced the delivery efficiency without imparting significant cytotoxicity. Notably, the uptake pathway was tunable depending on the nature of the membrane-directing group. CA1 delivered siRNAs mainly through caveolae-mediated endocytosis, and CA2 through clathrin- and caveolin-independent endocytosis; CA3 recruited siRNAs specifically into biotin receptor-positive HepG2 cells through receptor-mediated endocytosis. Thus, it appears possible to develop tunable siRNA transporters simply by changing the membrane-directing parts. These are the first examples of amphiphilic siRNA transporters accompanying coordinative interactions between the amphiphiles and siRNAs. © 2016 American Chemical Society
URI
https://pr.ibs.re.kr/handle/8788114/2991
ISSN
1043-1802
Appears in Collections:
Center for Self-assembly and Complexity(복잡계 자기조립 연구단) > Journal Papers (저널논문)
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