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Cytotoxicity and biodistribution studies of luminescent Au(i) and Ag(i) N-heterocyclic carbenes. Searching for new biological targets


Visbal Acevedo, Renso Raul
Fernández Moreira, Vanesa
Marzo, Isabel
Laguna, Antonio
Gimeno, María Concepción

Artículo de revista

2016

Dalton Transactions

https://doi.org/https://doi.org/10.1039/C6DT02878K

14779226

Cell cultureBuscar en Repositorio UMECIT
Cell deathBuscar en Repositorio UMECIT
Chlorine compoundsBuscar en Repositorio UMECIT
FluorescenceBuscar en Repositorio UMECIT
GoldBuscar en Repositorio UMECIT
Gold compoundsBuscar en Repositorio UMECIT
LigandsBuscar en Repositorio UMECIT
LuminescenceBuscar en Repositorio UMECIT
Organic compoundsBuscar en Repositorio UMECIT
SilverBuscar en Repositorio UMECIT

A range of fluorescent and biologically compatible gold(i)-N-heterocyclic carbenes bearing acridine as a wingtip group and either a 2-mercaptopyridine or a tetra-O-acetyl-1-thio-β-d-glucopyranoside as an ancillary ligand has been synthesised. Their luminescence, cytotoxicity and biodistribution have been investigated together with those of analogous gold(i) and silver(i) chloride- and bis-NHC complexes. All complexes displayed emissions based on IL transitions centred on the acridine moiety. The cytotoxic activity measured in lung, A549, and pancreatic, MiaPaca2, carcinoma cell lines revealed a general cytotoxicity pattern (thiolate > biscarbene > chloride derivatives) and flow cytometry assays pointed towards apoptosis as the cell death mechanism. Moreover, fluorescence cell microscopy disclosed an unusual biodistribution behavior, being mainly localised in lysosomes and to a lesser extent in the nucleus. Preliminary DNA interaction experiments suggested the metal fragment and not the acridine moiety as responsible for such biodistribution, which widen the scope for new biological targets.

http://hdl.handle.net/11323/1417

  • Artículos científicos [2634]

Descripción: Cytotoxicity and biodistribution studies of luminescent Au(i).pdf
Título: Cytotoxicity and biodistribution studies of luminescent Au(i).pdf
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