Genotoxic effects of the antimalarial drug lumefantrine in human lymphocytes in vitro and computational prediction of the mechanism associated with its interaction with DNA

Genotoxic effects of the antimalarial drug lumefantrine in human lymphocytes in vitro and computational prediction of the mechanism associated with its interaction with DNA

Lumefantrine (LF) is an aryl‐amino alcohol antimalarial drug used in artemisinin‐based combination therapies against malaria worldwide. In this study, we investigated the genotoxic effects of LF in human lymphocytes in vitro, and the potential noncovalent interaction of LF with DNA using a 3D DNA‐do...

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Veröffentlicht in:Environmental and molecular mutagenesis 2015-07, Vol.56 (6), p.556-562
Hauptverfasser: de Lucca, Renato M.R., Batista Júnior, João, Fontes, Cor J. Fernandes, de Oliveira Bahia, Marcelo, Bassi-Branco, Carmen L.
Format: Artikel
Sprache:eng
Schlagworte:
Adult
Antimalarials - chemistry
Antimalarials - toxicity
Cells, Cultured
Comet Assay
computational analysis
DNA - chemistry
DNA - metabolism
DNA minor groove agent
Ethanolamines - chemistry
Ethanolamines - metabolism
Ethanolamines - toxicity
Female
Fluorenes - chemistry
Fluorenes - metabolism
Fluorenes - toxicity
Humans
Lymphocytes - drug effects
malaria
Male
micronucleus
Micronucleus Tests
Molecular Docking Simulation
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Zusammenfassung:Lumefantrine (LF) is an aryl‐amino alcohol antimalarial drug used in artemisinin‐based combination therapies against malaria worldwide. In this study, we investigated the genotoxic effects of LF in human lymphocytes in vitro, and the potential noncovalent interaction of LF with DNA using a 3D DNA‐docking model. The number of DNA breaks and the frequency of nuclear buds (NBUDS) was significantly increased (P 
ISSN:0893-6692
1098-2280
DOI:10.1002/em.21942