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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060
EISSN: 1678-8060
Vol. 99, No. 7, 2004, pp. 757-761
Bioline Code: oc04153
Full paper language: English
Document type: Research Article
Document available free of charge

Memórias do Instituto Oswaldo Cruz, Vol. 99, No. 7, 2004, pp. 757-761

 en Antileishmanial Activity of Lapachol Analogues
Nadja MF Lima; Clariane S Correia; Leonor L Leon; Gérzia MC Machado; Maria de Fátima Madeira; Antônio Euzébio G Santana & Marília OF Goulart

Abstract

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.

Keywords
Leishmania amazonensis - Leishmania braziliensis - lapachol - isolapachol - antileishmanial activity - naphthoquinones

 
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