Antimalarial Properties of Dunnione Derivatives as NQO2 Substrates.
Molecules
; 24(20)2019 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-31618826
ABSTRACT
Dunnione, a natural product isolated from the leaves of Streptocarpus dunnii (Gesneriaceae), acts as a substrate for quinone-reductases that may be associated with its antimalarial properties. Following our exploration of reactive oxygen species-producing compounds such as indolones, as possible new approaches for the research of new ways to treat this parasitosis, we explored derivatives of this natural product and their possible antiplasmodial and antimalarial properties, in vitro and in vivo, respectively. Apart from one compound, all the products tested had weak to moderate antiplasmodial activities, the best IC50 value being equal to 0.58 µM. In vivo activities in the murine model were moderate (at a dose of 50 mg/kg/mice, five times higher than the dose of chloroquine). These results encourage further pharmacomodulation steps to improve the targeting of the parasitized red blood cells and antimalarial activities.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinona Redutases
/
Naftoquinonas
/
Antimaláricos
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article