Antileishmanial activity of lapachol analogues
Mem. Inst. Oswaldo Cruz
;
99(7): 757-761, Nov. 2004. ilus, tab, graf
Article
in English
| LILACS
| ID: lil-391608
RESUMO
The antileishmanial activity of lapachol, isolapachol, and dihydrolapachol, along with soluble derivatives (potassium salt) and acetate was obtained. All the compounds were assayed against metacyclic promastigotes of two different species of Leishmania associated to tegumentar leishmaniasis L. amazonensis and L. braziliensis. All compounds presented significant activity, being isolapachol acetate the most active against promastigotes, with IC50/24h = 1.6 ± 0.0 µg/ml and 3.4 ± 0.5 µg/ml for, respectively, L. amazonensis and L. braziliensis. This compound was also assayed in vivo against L. amazonensis and showed to be active. Its toxicity in vitro was also established, and at concentration similar to the IC50, no toxicity was evidenced. In all experiments, pentamidine isethionate was used as a reference drug. The present results reinforce the potential use of substituted hydroxyquinones and derivatives as promising antileishmanial drugs and suggest a continuing study within this class of compounds.
Full text:
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Index:
LILACS (Americas)
Main subject:
Leishmania braziliensis
/
Macrophages, Peritoneal
/
Antiprotozoal Agents
Limits:
Animals
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2004
Type:
Article
Affiliation country:
Brazil
Institution/Affiliation country:
Fiocruz/BR
/
Universidade Federal de Alagoas/BR
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