Structure-activity relationship between Zn2+-chelated alkylated poly(1-vinylimidazole) and gene transfection

J Inorg Biochem. 2017 Aug:173:120-125. doi: 10.1016/j.jinorgbio.2017.05.007. Epub 2017 May 10.

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.

Keywords: Alkylated poly(1-vinylimidazole); Chelation; Gene transfection; Structure-activity relationship; Zinc ion (Zn(2+)).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylating Agents / chemistry*
  • Chelating Agents / chemistry*
  • Imidazoles / chemistry*
  • Polyvinyls / chemistry*
  • Structure-Activity Relationship
  • Transfection
  • Zinc / chemistry*

Substances

  • Alkylating Agents
  • Chelating Agents
  • Imidazoles
  • Polyvinyls
  • poly(1-vinylimidazole)
  • Zinc