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Aptamer-mediated selective delivery of a cytotoxic cationic NHC-Au(I) complex to cancer cells

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Abstract

A novel cationic NHC-Au(I) complex was synthesized and studied for its antitumor activity. For all the cell lines tested, cationic NHC-Au(I) complex 2 shows much higher cytotoxicity than its neutral analogue 1. To achieve selective cancer cell targeting, complex 2 was covalently conjugated to aptamer AS1411, a DNA aptamer with strong binding affinity for nucleolin. The successful conjugation was confirmed by HPLC, gel electrophoresis, fluorescence spectroscopy and UV-Vis absorption. Conjugate AS1411-2 was then examined for its specific targeting and binding ability towards cancer cells over human normal cells using flow cytometry analysis and confocal microscopy. The cytotoxicity of AS1411-2 was then estimated by MTS assay. It was found that AS1411-2 exhibits higher activity than complex 2 towards targeted cells. Importantly, AS1411-2 exhibits much lower cytotoxicity towards healthy normal cell lines. Concurrently, the control groups without the AS1411 aptamer or without the NHC-Au(I) complex do have significant impact on cancer cell viability.

Graphical abstract: Aptamer-mediated selective delivery of a cytotoxic cationic NHC-Au(i) complex to cancer cells

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Publication details

The article was received on 18 Jul 2017, accepted on 20 Nov 2017 and first published on 20 Nov 2017


Article type: Paper
DOI: 10.1039/C7DT02616A
Citation: Dalton Trans., 2018, Advance Article
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    Aptamer-mediated selective delivery of a cytotoxic cationic NHC-Au(I) complex to cancer cells

    W. Niu, I. Teng, X. Chen, W. Tan and A. S. Veige, Dalton Trans., 2018, Advance Article , DOI: 10.1039/C7DT02616A

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