Abstract
The synthetic DOX-LNA conjugate was characterized by proton nuclear magnetic resonance and mass spectrometry. In addition, the purity of the conjugate was analyzed by reverse-phase high-performance liquid chromatography. The cellular uptake, intracellular distribution, and cytotoxicity of DOX-LNA were assessed by flow cytometry, fluorescence microscopy, liquid chromatography/electrospray ionization tandem mass spectrometry, and the tetrazolium dye assay using the in vitro cell models. The DOX-LNA conjugate showed substantially higher tumor-specific cytotoxicity compared with DOX.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Chromatography, Liquid / methods
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Doxorubicin / pharmacology*
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Doxorubicin / toxicity
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Drug Design
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Endocytosis
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Flow Cytometry / methods
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Humans
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Inhibitory Concentration 50
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Microscopy, Fluorescence / methods
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Models, Chemical
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Neoplasms / drug therapy*
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Neoplasms / metabolism*
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Spectrometry, Mass, Electrospray Ionization / methods
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Tetrazolium Salts / chemistry
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Thiazoles / chemistry
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alpha-Linolenic Acid / chemistry*
Substances
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Tetrazolium Salts
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Thiazoles
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alpha-Linolenic Acid
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Doxorubicin
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thiazolyl blue