Cellular uptake and cytotoxicity of octahedral rhenium cluster complexes

Soo Jin Choi, Konstantin A. Brylev, Jing Zhe Xu, Yuri V. Mironov, Vladimir E. Fedorov, Youn Soo Sohn, Sung Jin Kim, Jin Ho Choy

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64 Scopus citations

Abstract

Cellular uptake behavior of a novel class of octahedral rhenium cluster compounds, hexahydroxo complexes K4[{Re6S8}(OH)6] · 8H2O (1) and K4[{Re6Se8}(OH)6] · 8H2O (2), was evaluated in human cervical adenocarcinoma HeLa cells. Confocal microscopy and flow cytometry studies demonstrated that rhenium cluster 1 was not internalized into cell, while rhenium cluster 2 was. Conjugation of a polymer to rhenium cluster 1, namely the derivative K4[{Re6S8}(OH)5L] (3) (L is amphiphilic diblock copolymer MPEG550-CH2CONH-GlyPheLeuGlyPheLeu-COO-), considerably enhanced cellular uptake in a concentration-dependent manner and was predominantly localized in the cytoplasm and nucleus upon incubation time. The uptake of rhenium cluster 2 was mediated by energy-dependent endocytosis, whereas rhenium cluster 3 was directly ingested into cells by cell-fusion-like mechanism. According to the cytotoxicity evaluation test, both rhenium clusters 2 and 3 did not exhibit acute cytotoxic effects up to 50 μM, at the practical concentration level of biological applications. It is, therefore, expected that the rhenium cluster complexes can be promising potential candidates as diagnostic agents for medical treatment.

Original languageEnglish
Pages (from-to)1991-1996
Number of pages6
JournalJournal of Inorganic Biochemistry
Volume102
Issue number11
DOIs
StatePublished - Nov 2008

Bibliographical note

Funding Information:
This work was supported by the Korea Science and Engineering Foundation (KOSEF) grant funded by the Korea government (MEST) (No. R11-2005-008-00000-0), by the Korea Research Foundation Grant Funded by the Ministry of Education and Human Resource Development (Grant KRF-2005-210-C00015) and by Goskontrakt 02.513.11.3047/2007-3-1.3-07-01-093.

Keywords

  • Amphiphilic diblock copolymer
  • Cellular uptake
  • Cytotoxicity
  • Octahedral rhenium cluster complexes
  • Uptake mechanism

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