Synthesis and Comparative Evaluation of Novel Cationic Amphiphile C12-Man-Q as an Efficient DNA Delivery Agent in Vitro
Molecules 2018
Gunita Apsite, Irena Timofejeva, Aleksandra Vezane, Brigita Vīgante, Martins Rucins, Arkadij Sobolev, Māra Plotniece, Kārlis Pajuste, Tatjana Kozlovska, Aiva Plotniece

New amphiphilic 1,4-DHP derivative C12-Man-Q with remoted cationic moieties at positions 2 and 6 was synthesised to study DNA delivery activity. The results were compared with data obtained for cationic 1,4-DHP derivative D19, which is known to be the most efficient one among the previously tested 1,4-DHP amphiphiles. Transmission electron microscopy data confirms that lipoplexes formed by the compound C12-Man-Q were quite uniform, vesicular like structures with sizes of about 50nm, and lipoplexes produced by compound D19 were of irregular shapes, varied in size in the range of 20-80 nm. Confocal microscopy results revealed that both amphiphiles effectively delivered green fluorescent protein expression plasmid into BHK-21 cells and produced a fluorescent signal with satisfactory efficiency, although compound C12-Man-Q was more cytotoxic to the BHK-21 cells with an increase of concentration. Compound D19 showed higher transfection efficiency to transfect BHK-21 and Cos-7 cell lines. The compound C12-Man-Q showed modest delivery activity in all used cell lines, and higher activity was obtained in the case of H2-35 and B16 cells.


Keywords
cationic amphiphiles, 1,4-dihydropyridines, lipoplexes, gene delivery, cytotoxicity
DOI
10.3390/molecules23071540
Hyperlink
https://www.mdpi.com/1420-3049/23/7/1540

Apsite, G., Timofejeva, I., Vezane, A., Vīgante, B., Rucins, M., Sobolev, A., Plotniece, M., Pajuste, K., Kozlovska, T., Plotniece, A. Synthesis and Comparative Evaluation of Novel Cationic Amphiphile C12-Man-Q as an Efficient DNA Delivery Agent in Vitro. Molecules, 2018, Vol. 23, No. 7, pp.1-18. ISSN 1420-3049. Available from: doi:10.3390/molecules23071540

Publication language
English (en)
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