8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a non-competitive inhibitor of trypanothione reductase
Mem. Inst. Oswaldo Cruz
;
98(4): 565-568, June 2003. ilus, tab, graf
Artigo
em Inglês
| LILACS
| ID: lil-344256
RESUMO
The enzyme trypanothione reductase is a recognised drug target in trypanosomatids and has been used in the search of new compounds with potential activity against diseases such as leishmaniasis, Chagas disease and African trypanosomiasis. 8-Methoxy-naphtho [2,3-b] thiophen-4,9-quinone was selected in a screening of natural and synthetic compounds using an in vitro assay with the recombinant enzyme from Trypanosoma cruzi. Its mode of inhibition fits a non-competitive model with respect to the substrate (trypanothione) and to the co-factor (NADPH), with Ki-values of 5 and 3.6 æM, respectively. When tested against human glutathione reductase, this compound did not display any significant inhibition at 100 æM, indicating a good selectivity against the parasite enzyme
Texto completo:
DisponíveL
Índice:
LILACS (Américas)
Assunto principal:
Tiofenos
/
Trypanosoma cruzi
/
Naftoquinonas
/
Inibidores Enzimáticos
/
NADP
Tipo de estudo:
Estudo prognóstico
Limite:
Animais
/
Humanos
Idioma:
Inglês
Revista:
Mem. Inst. Oswaldo Cruz
Assunto da revista:
Medicina Tropical
/
Parasitologia
Ano de publicação:
2003
Tipo de documento:
Artigo
País de afiliação:
Brasil
/
Reino Unido
Instituição/País de afiliação:
Fiocruz/BR
/
University of Dundee/GB
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