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Highly luminescent metallacages featuring bispyridyl ligands functionalised with BODIPY for imaging in cancer cells

Woods, Ben, Dollerer, Daniel, Aikman, Brech, Wenzel, Margot ORCID:, Sayers, Edward J. ORCID:, Kühn, Fritz E., Jones, Arwyn T. ORCID: and Casini, Angela ORCID: 2019. Highly luminescent metallacages featuring bispyridyl ligands functionalised with BODIPY for imaging in cancer cells. Journal of Inorganic Biochemistry 199 , 110781. 10.1016/j.jinorgbio.2019.110781

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Recently, 3-dimentional supramolecular coordination complexes of the metallacage type have been shown to hold promise as drug delivery systems for different cytotoxic agents, including the anticancer drug cisplatin. However, so far only limited information is available on their uptake and sub-cellular localisation in cancer cells. With the aim of understanding the fate of metallacages in cells by fluorescence microscopy, three fluorescent Pd2L4 metallacages were designed and synthesised by self-assembly of two types of bispyridyl ligands (L), exo-functionalised with boron dipyrromethene (BODIPY) moieties, with Pd(II) ions. The cages show high quantum yields and are moderately stable in the presence of physiologically relevant concentration of glutathione. Furthermore, the cages are able to encapsulate the anticancer drug cisplatin, as demonstrated by NMR spectroscopy. Preliminary cytotoxicity studies in a small panel of human cancer cells showed that the metallacages are scarcely toxic in vitro. The marked fluorescence due to BODIPY allowed us to visualise the cages' uptake and sub-cellular localisation inside melanoma cells using fluorescence microscopy, highlighting uptake via active transport mechanisms and accumulation in cytoplasmic vesicles.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Publisher: Elsevier
ISSN: 0162-0134
Funders: German Excellence Initiative and the European Union Seventh Framework Program
Date of First Compliant Deposit: 23 July 2019
Date of Acceptance: 14 July 2019
Last Modified: 18 May 2024 08:08

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