Cellular Uptake of the ATSM-Cu(II) Complex under Hypoxic Conditions.
ATSM−Cu(II)
cancer
copper homeostasis
copper toxicity
Journal
ChemistryOpen
ISSN: 2191-1363
Titre abrégé: ChemistryOpen
Pays: Germany
ID NLM: 101594811
Informations de publication
Date de publication:
04 2021
04 2021
Historique:
revised:
08
03
2021
received:
22
02
2021
entrez:
28
4
2021
pubmed:
29
4
2021
medline:
8
9
2021
Statut:
ppublish
Résumé
The Cu(II)-diacetyl-bis (N4-methylthiosemicarbazone) complex (ATSM-Cu(II)) has been suggested as a promising positron emission tomography (PET) agent for hypoxia imaging. Several in-vivo studies have shown its potential to detect hypoxic tumors. However, its uptake mechanism and its specificity to various cancer cell lines have been less studied. Herein, we tested ATSM-Cu(II) toxicity, uptake, and reduction, using four different cell types: (1) mouse breast cancer cells (DA-3), (2) human embryonic kidney cells (HEK-293), (3) breast cancer cells (MCF-7), and (4) cervical cancer cells (Hela) under normoxic and hypoxic conditions. We showed that ATSM-Cu(II) is toxic to breast cancer cells under normoxic and hypoxic conditions; however, it is not toxic to normal HEK-293 non-cancer cells. We showed that the Cu(I) content in breast cancer cell after treatment with ATSM-Cu(II) under hypoxic conditions is higher than in normal cells, despite that the uptake of ATSM-Cu(II) is a bit higher in normal cells than in breast cancer cells. This study suggests that the redox potential of ATSM-Cu(II) is higher in breast cancer cells than in normal cells; thus, its toxicity to cancer cells is increased.
Identifiants
pubmed: 33908707
doi: 10.1002/open.202100044
pmc: PMC8080296
doi:
Substances chimiques
Coordination Complexes
0
Copper Radioisotopes
0
Copper Transporter 1
0
Copper-64
0
Organometallic Compounds
0
SLC31A1 protein, human
0
Slc31a1 protein, mouse
0
Thiosemicarbazones
0
copper (II) diacetyl-di(N(4)-methylthiosemicarbazone)
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
486-492Informations de copyright
© 2021 The Authors. Published by Wiley-VCH GmbH.
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