Information de reference pour ce titreAccession Number: | 00006623-201009000-00016.
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Author: | Dong, Yanmei 1,2; Li, Jing 1; Wu, Chao 1; Oupicky, David 1
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Institution: | (1)Department of Pharmaceutical Sciences, Wayne State University, Detroit, Michigan 48202, USA (2)Department of Chemistry, University of Montreal, Montreal, Canada
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Title: | Bisethylnorspermine Lipopolyamine as Potential Delivery Vector for Combination Drug/Gene Anticancer Therapies.[Article]
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Source: | Pharmaceutical Research. 27(9):1927-1938, September 2010.
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Abstract: | Purpose: To design novel synthetic gene delivery system in which the carrier molecule functions dually as a carrier and a cytotoxic agent targeting dysregulated polyamine metabolism in cancer.
Methods: Bisethylnorspermine (BENSpm) lipopolyamine was synthesized and its toxicity evaluated by MTS assay in MCF-7 and MCF-10A cells. Transfection activity was determined using luciferase plasmid DNA.
Results: Asymmetrical lipid analogue of polyamine anticancer drug BENSpm was synthesized using nucleophilic ring opening of azetidinium ion. The synthesized LipoBENSpm showed cytotoxicity comparable to that of parent BENSpm in human breast cancer cell line MCF-7 but mediated 3-4 orders magnitude higher transfection activity. Importantly, cytostatic activity of BENSpm, typically in a low [mu]M range, falls within a relevant and typical concentration range required for efficient gene delivery.
Conclusions: These findings make gene delivery vectors based on BENSpm promising candidates for combination drug/gene approaches to the treatment of cancer.
(C)2010 Kluwer Academic Publishers
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Author Keywords: | drug combination; drug delivery; gene delivery; lipid; transfection.
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Language: | English.
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Document Type: | Research Paper: PDF Only.
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Journal Subset: | Pharmacology.
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ISSN: | 0724-8741
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NLM Journal Code: | phs, 8406521
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DOI Number: | https://dx.doi.org/10.1007/s1109...- ouverture dans une nouvelle fenêtre
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