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Intracellular Transport Studies of Picolinate Macrocyclic Copper and Lanthanide Complexes
Author(s) -
Porqueras Diego Santo Domingo,
Beyler Maryline,
Tripier Raphaël,
Salerno Milena
Publication year - 2016
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201600990
Subject(s) - intracellular , chemistry , efflux , extracellular , permeability (electromagnetism) , lanthanide , biophysics , in vivo , cell permeability , cytotoxicity , kinetics , metal , combinatorial chemistry , stereochemistry , in vitro , biochemistry , membrane , organic chemistry , biology , ion , physics , microbiology and biotechnology , quantum mechanics
In vivo molecular imaging involves different techniques to image cellular biochemical processes. Metal complexes can be used as cell‐permeable medical imaging agents. In this work we studied the cytotoxicity and the cellular incorporation kinetics of two recently synthesized picolinate macrocyclic complexes, [Eu(do2pa)] + and [Cu(te1pa)] + . Both complexes are able to enter inside the cells. The intracellular concentration (Ci) of [Eu(do2pa)] + is ∼5 times the extracellular concentration (Ce). In the case of [Cu(te1pa)] + , the ratio Ci/Ce is approximately 1.4. Furthermore, the results suggest that these complexes are not substrates of P‐gp, an efflux transport protein involved in the mechanisms of multidrug resistance in cancer cells and in the low permeability of blood‐brain barrier. The results obtained here, added to their physicochemical properties, let us propose that the complexes studied could be suitable platforms for the synthesis of cell‐permeable MRI contrast agents or PET tracers.