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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Efficient nucleic acid transduction with lipoplexes containing novel piperazine- and polyamine-conjugated cholesterol derivatives
Bioorganic and Medicinal Chemistry Letters, Volume 19, No. 1, Year 2009
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Description
To advance the use of cationic lipids for non-viral nucleic acid vector formulation, a panel of novel nitrogen heterocycle cholesteryl derivatives containing a biodegradable carbamate linker was synthesised. Optimally acting piperazine and cyclen compounds had nucleic acid-binding and lipoplex nanoparticle formation properties that were suitable for their use as non-viral vectors. It was found that the lipoplexes formed were capable of efficient non-toxic nucleic acid delivery to cells in culture. The chemical structure of individual cationic lipids, which is likely to influence lipoplex formation, affected efficiency of DNA or RNA transfection. The results indicated that the cyclen containing compound possessing two cholesteryl moieties resulted in efficient siRNA-mediated target gene silencing but was a poor reagent for DNA transfection. © 2008 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Islam, Rafique Ul
South Africa, Johannesburg
School of Clinical Medicine
South Africa, Johannesburg
University of the Witwatersrand
Hean, Justin
South Africa, Johannesburg
School of Clinical Medicine
van Otterlo, Willem A. L.
South Africa, Johannesburg
University of the Witwatersrand
de Koning, Charles Bernard D.E.
South Africa, Johannesburg
University of the Witwatersrand
Arbuthnot, Patrick B.
South Africa, Johannesburg
School of Clinical Medicine
Statistics
Citations: 32
Authors: 5
Affiliations: 2
Identifiers
Doi:
10.1016/j.bmcl.2008.11.009
ISSN:
0960894X
Research Areas
Environmental
Genetics And Genomics