Coordinative Amphiphiles as Tunable siRNA Transporters
SCIE
SCOPUS
- Title
- Coordinative Amphiphiles as Tunable siRNA Transporters
- Authors
- Kim, Jin Bum; Lee, Yeong Mi; Ryu, Jooyeon; Lee, Eunji; Kim, Won Jong; Keum, Gyochang; Bang, Eun-Kyoung
- Date Issued
- 2016-08
- 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.
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/103563
- DOI
- 10.1021/acs.bioconjchem.6b00260
- ISSN
- 1043-1802
- Article Type
- Article
- Citation
- BIOCONJUGATE CHEMISTRY, vol. 27, no. 8, page. 1850 - 1856, 2016-08
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