Zn(II)-dipicolylamine-based metallo-lipids as novel non-viral gene vectors

Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry
Rong-Chuan SuZhi-Gang Zhao

Abstract

In this study, a series of Zn(II)-dipicolylamine (Zn-DPA) based cationic lipids bearing different hydrophobic tails (long chains, α-tocopherol, cholesterol or diosgenin) were synthesized. Structure-activity relationship (SAR) of these lipids was studied in detail by investigating the effects of several structural aspects including the type of hydrophobic tails, the chain length and saturation degree. In addition, several assays were used to study their interactions with plasmid DNA, and results reveal that these lipids could condense DNA into nanosized particles with appropriate size and zeta-potentials. MTT-based cell viability assays showed that lipoplexes 5 had low cytotoxicity. The in vitro gene transfection studies showed the hydrophobic tails clearly affected the TE, and hexadecanol-containing lipid 5b gives the best TE, which was 2.2 times higher than bPEI 25k in the presence of 10% serum. The results not only demonstrate that these lipids might be promising non-viral gene vectors, but also afford us clues for further optimization of lipidic gene delivery materials.

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Citations

May 30, 2020·Pharmaceutics·José Antonio LebrónPilar López-Cornejo
Jan 21, 2019·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Qing-Ying YuXiao-Qi Yu

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Methods Mentioned

BETA
transfection
NMR
electrophoresis
dynamic light scattering
flow cytometry
protein assay
column chromatography
ELISA
fluorescence microscopy

Software Mentioned

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