Hydroxychloroquine Does Not Function as a Direct Zinc Ionophore.

COVID-19 clioquinol hydroxychloroquine ionophore zinc

Journal

Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003

Informations de publication

Date de publication:
20 Apr 2022
Historique:
received: 18 03 2022
revised: 11 04 2022
accepted: 15 04 2022
entrez: 28 5 2022
pubmed: 29 5 2022
medline: 29 5 2022
Statut: epublish

Résumé

Drug-mediated correction of abnormal biological zinc homeostasis could provide new routes to treating neurodegeneration, cancer, and viral infections. Designing therapeutics to facilitate zinc transport intracellularly is hampered by inadequate concentrations of endogenous zinc, which is often protein-bound in vivo. We found strong evidence that hydroxychloroquine, a drug used to treat malaria and employed as a potential treatment for COVID-19, does not bind and transport zinc across biological membranes through ionophoric mechanisms, contrary to recent claims. In vitro complexation studies and liposomal transport assays are correlated with cellular zinc assays in A549 lung epithelial cells to confirm the indirect mechanism of hydroxychloroquine-mediated elevation in intracellular zinc without ionophorism. Molecular simulations show hydroxychloroquine-triggered helix perturbation in zinc-finger protein without zinc chelation, a potential alternative non-ionophoric mechanism.

Identifiants

pubmed: 35631485
pii: pharmaceutics14050899
doi: 10.3390/pharmaceutics14050899
pmc: PMC9147311
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Science Foundation Ireland
ID : 12/RC/2275_P2
Pays : Ireland

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Auteurs

Oisín N Kavanagh (ON)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
School of Pharmacy, Newcastle University, Newcastle upon Tyne NE1 7RU, UK.
Department of Chemical Sciences, Bernal Institute, University of Limerick, V94 T9PX Limerick, Ireland.
Department of Chemistry, Maynooth University (National University of Ireland), W23 F2H6 Maynooth, Ireland.
National Institute for Cellular Biotechnology, Dublin City University, D09 NR58 Dublin, Ireland.

Shayon Bhattacharya (S)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Department of Physics, Bernal Institute, University of Limerick, V94 T9PX Limerick, Ireland.

Luke Marchetti (L)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Department of Chemistry, Maynooth University (National University of Ireland), W23 F2H6 Maynooth, Ireland.

Robert Elmes (R)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Department of Chemistry, Maynooth University (National University of Ireland), W23 F2H6 Maynooth, Ireland.

Finbarr O'Sullivan (F)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
National Institute for Cellular Biotechnology, Dublin City University, D09 NR58 Dublin, Ireland.

John P Farragher (JP)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.

Shane Robinson (S)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Janssen Pharmaceutical Sciences, T45 P663 Cork, Ireland.

Damien Thompson (D)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Department of Physics, Bernal Institute, University of Limerick, V94 T9PX Limerick, Ireland.

Gavin M Walker (GM)

SSPC, The Science Foundation Ireland Research Centre for Pharmaceuticals, V94 T9PX Limerick, Ireland.
Department of Chemical Sciences, Bernal Institute, University of Limerick, V94 T9PX Limerick, Ireland.

Classifications MeSH