A single thiourea group is not enough to get stable thiourea lipoplexes

Eihab Kabha; Claire Jacquement; Gaëlle Pembouong; Nathalie Mignet; Daniel Scherman; Jean Herscovici

doi:10.1016/j.bmc.2008.01.029

A single thiourea group is not enough to get stable thiourea lipoplexes

Eihab Kabha, Claire Jacquement, Gaëlle Pembouong, Nathalie Mignet, Daniel Scherman, Jean Herscovici

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

Abstract

The preparation of a new family of lipothiourea is reported using an automatic synthetic workstation. In these compounds the headgroups were made from single thiourea derivatives. The physicochemical properties and the transfection efficiency of several members of the family were studied. It was found that in the presence of DMPC small lipoplexes could be prepared. In opposite to the previously described di- and tri-lipothioureas most of these liposomes are unstable overtime. In addition, even the stable ones show no transfecting efficiency. All these data demonstrate that at least two thiourea groups are necessary to produce stable lipoplexes, to condense DNA and to give efficient transfection.

Original language	English
Pages (from-to)	4003-4008
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	16
Issue number	7
DOIs	https://doi.org/10.1016/j.bmc.2008.01.029
State	Published - 1 Apr 2008
Externally published	Yes

Bibliographical note

Funding Information:
This work was financially supported by INSERM, CNRS, MNERT, the Région Ile de France (SESAME, CPER). E.K. thanks the French Government for a Chateaubriand Post-doctoral fellowship.

Funding

This work was financially supported by INSERM, CNRS, MNERT, the Région Ile de France (SESAME, CPER). E.K. thanks the French Government for a Chateaubriand Post-doctoral fellowship.

Funders	Funder number
French government
Institut national de la santé et de la recherche médicale
Centre National de la Recherche Scientifique
Cancéropôle Ile de France

Keywords

DNA condensation
Lipoplexes
Liposomes
Thiourea

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10.1016/j.bmc.2008.01.029

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title = "A single thiourea group is not enough to get stable thiourea lipoplexes",

abstract = "The preparation of a new family of lipothiourea is reported using an automatic synthetic workstation. In these compounds the headgroups were made from single thiourea derivatives. The physicochemical properties and the transfection efficiency of several members of the family were studied. It was found that in the presence of DMPC small lipoplexes could be prepared. In opposite to the previously described di- and tri-lipothioureas most of these liposomes are unstable overtime. In addition, even the stable ones show no transfecting efficiency. All these data demonstrate that at least two thiourea groups are necessary to produce stable lipoplexes, to condense DNA and to give efficient transfection.",

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author = "Eihab Kabha and Claire Jacquement and Ga{\"e}lle Pembouong and Nathalie Mignet and Daniel Scherman and Jean Herscovici",

note = "Funding Information: This work was financially supported by INSERM, CNRS, MNERT, the R{\'e}gion Ile de France (SESAME, CPER). E.K. thanks the French Government for a Chateaubriand Post-doctoral fellowship.",

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AU - Kabha, Eihab

AU - Jacquement, Claire

AU - Pembouong, Gaëlle

AU - Mignet, Nathalie

AU - Scherman, Daniel

AU - Herscovici, Jean

N1 - Funding Information: This work was financially supported by INSERM, CNRS, MNERT, the Région Ile de France (SESAME, CPER). E.K. thanks the French Government for a Chateaubriand Post-doctoral fellowship.

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N2 - The preparation of a new family of lipothiourea is reported using an automatic synthetic workstation. In these compounds the headgroups were made from single thiourea derivatives. The physicochemical properties and the transfection efficiency of several members of the family were studied. It was found that in the presence of DMPC small lipoplexes could be prepared. In opposite to the previously described di- and tri-lipothioureas most of these liposomes are unstable overtime. In addition, even the stable ones show no transfecting efficiency. All these data demonstrate that at least two thiourea groups are necessary to produce stable lipoplexes, to condense DNA and to give efficient transfection.

AB - The preparation of a new family of lipothiourea is reported using an automatic synthetic workstation. In these compounds the headgroups were made from single thiourea derivatives. The physicochemical properties and the transfection efficiency of several members of the family were studied. It was found that in the presence of DMPC small lipoplexes could be prepared. In opposite to the previously described di- and tri-lipothioureas most of these liposomes are unstable overtime. In addition, even the stable ones show no transfecting efficiency. All these data demonstrate that at least two thiourea groups are necessary to produce stable lipoplexes, to condense DNA and to give efficient transfection.

KW - DNA condensation

KW - Lipoplexes

KW - Liposomes

KW - Thiourea

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IS - 7

ER -

A single thiourea group is not enough to get stable thiourea lipoplexes

Abstract

Bibliographical note

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Keywords

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