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Molecules 2018, 23(7), 1540; https://doi.org/10.3390/molecules23071540

Synthesis and Comparative Evaluation of Novel Cationic Amphiphile C12-Man-Q as an Efficient DNA Delivery Agent In Vitro

1
Latvian Biomedical Research and Study Centre, Ratsupites iela 1, LV-1067 Riga, Latvia
2
Latvian Institute of Organic Synthesis, Aizkraukles iela 21, LV-1006 Riga, Latvia
3
Rīga Stradiņš University, Dzirciema iela 16, LV-1007 Riga, Latvia
*
Author to whom correspondence should be addressed.
Received: 28 May 2018 / Revised: 15 June 2018 / Accepted: 21 June 2018 / Published: 26 June 2018
(This article belongs to the Special Issue Gene Delivery)
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Abstract

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. We analysed the effects of C12-Man-Q concentration, complexation media, and complex/cell contact time on the gene delivery effectiveness and cell viability. Transmission electron microscopy data confirms that lipoplexes formed by the compound C12-Man-Q were quite uniform, vesicular-like structures with sizes of about 50 nm, and lipoplexes produced by compound D19 were of irregular shapes, varied in size in the range of 25–80 nm. Additionally, 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. It can be concluded that optimal conditions for C12-Man-Q lipoplexes delivery in BHK-21 cells were the serum free media without 0.15 M NaCl, at an N/P ratio of 0.9. Compound D19 showed higher transfection efficiency to transfect BHK-21 and Cos-7 cell lines, when transfecting active proliferating cells. Although D19 was not able to transfect all studied cell lines we propose that it could be cell type specific. 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. The transfection efficiency in cell lines MCF-7, HeLa, and Huh-7 appears to be comparable to the reference compound D19 and minimal in the HepG2 cell line. View Full-Text
Keywords: cationic amphiphiles; 1,4-dihydropyridines; lipoplexes; DNA transfection; gene delivery; cytotoxicity cationic amphiphiles; 1,4-dihydropyridines; lipoplexes; DNA transfection; gene delivery; cytotoxicity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Apsite, G.; Timofejeva, I.; Vezane, A.; Vigante, 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, 23, 1540.

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