Aptamer-mediated selective delivery of a cytotoxic cationic NHC-Au(i) complex to cancer cells. Issue 1 (1st December 2017)

• Record Type: Journal Article
• Authors: Niu, Weijia; Teng, I-Ting; Chen, Xigao; Tan, Weihong; Veige, Adam S.
• Is Part Of: Dalton transactions. Volume 47:Issue 1(2017)
• Page Start: 120
• Page End: 126
• Publication Date: 2017-12-01
• Subjects: Chemistry, Inorganic -- Periodicals; Chemistry, Physical and theoretical -- Periodicals; Chemistry, Inorganic -- Periodicals; 546.05
• DOI: 10.1039/c7dt02616a
• Languages: English
• ISSNs: 1477-9226

Abstract

Abstract : A novel cationic NHC-Au(i ) complex was synthesized and studied for its antitumor activity. 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 ) complex2 shows much higher cytotoxicity than its neutral analogue1 . To achieve selective cancer cell targeting, complex2 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 complex2 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.