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Structure-activity relationship between Zn2+-chelated alkylated poly(1-vinylimidazole) and gene transfection
Shoichiro Asayama1, Mizuki Sakata1, Hiroyoshi Kawakami1
1Department of Applied Chemistry, Tokyo Metropolitan University, 1-1 Minami-Osawa, Hachioji, Tokyo 192-0397, Japan.
Abstract:
The structure-activity relationship between Zn2+-chelated alkylated poly(1-vinylimidazole) (PVIm) and gene transfection has been demonstrated. From a chemical structure perspective, ethylated PVIm (PVIm-Et) chelated the most Zn2+ ions compared to methylated PVIm (PVIm-Me) and butylated PVIm (PVIm-Bu). The resulting Zn2+-chelated PVIm-Et formed more stable complexes with plasmid DNA complex than non-chelated PVIm-Et. From a biological activity perspective, the Zn2+-chelated PVIm-Et delivered the highest amount of Zn2+ ions inside the cell, corresponding to the highest gene transfection. These results suggest that PVIm-Et is the optimal sequence for the chelation of Zn2+ ions to enhance the gene transfection activity. The structure-activity relationship in this study is expected to offer a unique molecular design for drug/gene delivery systems.
