Cyclen-based lipidic oligomers as potential gene delivery vehicles

Acta Biomaterialia
Wen-Jing YiXiao-Qi Yu

Abstract

A series of cyclen-based linear oligomers bearing hydrophobic long chains (lipopolymers Cy-LC, where Cy and LC represent cyclen-based linear backbone and hydrophobic long chain substituents, respectively) were designed and synthesized. The effects of type and degree of substitution (DS) of hydrophobic long chains on the transfection efficiency were systematically studied. The nitrogen atoms with relatively strong basicity on the cyclen ensure their good DNA binding ability, which was confirmed by gel retardation and ethidium bromide exclusion assays. Lipopolyplexes could be formed as nanoparticles with suitable sizes and zeta potentials for gene transfection. In vitro gene delivery experiments revealed that the linoleic acid (LIN) substituted material Cy-LIN has better transfection efficiency than 25 kDa polyethylenimine in the absence or in the presence of serum. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and hemolysis assays showed low cytotoxicity and good biocompatibility of the lipopolyplexes. Fluorescent labeled DNA was used to study the cellular uptake and intracellular distribution of transfected DNA. Flow cytometry results suggested that a long chain is necessary for efficient cellular uptake, and ima...Continue Reading

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Citations

Nov 14, 2015·Bioorganic & Medicinal Chemistry Letters·Li-Ting ZhengZhi-Gang Zhao
May 15, 2015·Chemical Biology & Drug Design·Wen-Jing YiZhi-Gang Zhao
Apr 15, 2016·ACS Applied Materials & Interfaces·Chao-Ran LuanXiao-Qi Yu
Aug 30, 2016·Bioorganic & Medicinal Chemistry Letters·Rong-Chuan SuZhi-Gang Zhao
May 17, 2017·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Rong-Chuan SuZhi-Gang Zhao
Apr 1, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qiang LiuZhi-Gang Zhao
Nov 6, 2014·Organic & Biomolecular Chemistry·Zheng HuangXiao-Qi Yu
Aug 25, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Sudhakar GodeshalaKaushal Rege
Sep 7, 2016·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Zheng HuangXiao-Qi Yu
Aug 22, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Guo-Qing LinZhi-Gang Zhao
May 9, 2014·Chemical Communications : Chem Comm·Wen-Jing YiXiao-Qi Yu
Jan 21, 2019·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Qing-Ying YuXiao-Qi Yu
May 14, 2021·ACS Applied Materials & Interfaces·Fang TangMing-Di Xu
Nov 18, 2017·ACS Applied Materials & Interfaces·Yun-Xia SunXian-Zheng Zhang

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