Determination of antiplasmodial activity and binding affinity of curcumin and demethoxycurcumin towards PfTrxR.
Nat Prod Res
; 28(6): 359-64, 2014.
Article
em En
| MEDLINE
| ID: mdl-24443991
ABSTRACT
In our study, the inhibitory activity of curcuminoids towards Plasmodium falciparum thioredoxin reductase (PfTrxR) was determined using LC-MS-based functional assay and showed that only demethoxycurcumin (DMC) inhibited PfTrxR (IC50 2 µM). In silico molecular modelling was used to ascertain and further confirm that the binding affinities of curcumin and DMC are towards the dimer interface of PfTrxR. The in vitro antiplasmodial activities of curcumin and DMC were evaluated and shown to be active against chloroquine (CQ)-sensitive (D6 clone) and moderately active against CQ-resistant (W2 clone) strains of Plasmodium falciparum while no cytotoxicity was observed against Vero cells.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
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Tiorredoxina Dissulfeto Redutase
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Curcumina
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Antimaláricos
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article