Preprint Short Note Version 1 Preserved in Portico This version is not peer-reviewed

1,28-Di[(cholest-5-en-3β-yl)disulfanyl]-4,25-dioxo-3,8,12,17,21,26-hexaazaoctacosane tetrahydrochloride

Version 1 : Received: 9 January 2018 / Approved: 10 January 2018 / Online: 10 January 2018 (09:12:03 CET)

A peer-reviewed article of this Preprint also exists.

Puchkov, P.A.; Shmendel, E.V.; Andreeva, V.D.; Morozova, N.G.; Zenkova, M.A.; Maslov, M.A. A Novel Disulfide-Containing Polycationic Amphiphile: 1,28-Di[(cholest-5-en-3β-yl)disulfanyl]-4,25-dioxo-3,8,12,17,21,26-hexaazaoctacosane Tetrahydrochloride. Molbank 2018, 2018, M981. Puchkov, P.A.; Shmendel, E.V.; Andreeva, V.D.; Morozova, N.G.; Zenkova, M.A.; Maslov, M.A. A Novel Disulfide-Containing Polycationic Amphiphile: 1,28-Di[(cholest-5-en-3β-yl)disulfanyl]-4,25-dioxo-3,8,12,17,21,26-hexaazaoctacosane Tetrahydrochloride. Molbank 2018, 2018, M981.

Abstract

The absence of highly effective delivery systems is a major challenge for gene therapy. Our work was aimed at the development of novel cationic liposomes possessing high transfection efficiency. For this purpose, a novel disulfide polycationic amphiphile 2S4 was synthesized. Cationic liposomes based on 2S4 and a helper lipid DOPE were formed by the thin film hydration method and exhibited effective pDNA delivery into the HEK293 cells, with a maximal transfection activity superior to that of the commercial agent Lipofectamine® 2000. Our results suggest that the polycationic amphiphile 2S4 is a promising candidate for in vitro nucleic acid delivery.

Keywords

redox-sensitive; disulfide linker; gemini amphiphiles; gene therapy

Subject

Chemistry and Materials Science, Medicinal Chemistry

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