Antileishmanial activity of lapachol analogues

Memórias do Instituto Oswaldo Cruz

Nadja Mf Lima²  Clariane S Correia²  Leonor L Leon¹  Gérzia Mc Machado¹  Maria De Fátima Madeira¹  Antônio Euzébio G Santana²  Marília Of Goulart² 

[1] ,Universidade Federal de Alagoas Centro de Ciências Exatas e Naturais Departamento de QuímicaMaceió AL ,Brasil

关键词: Leishmania amazonensis;    Leishmania braziliensis;    lapachol;    isolapachol;    antileishmanial activity;    naphthoquinones;   

DOI  :  10.1590/S0074-02762004000700017

来源: SciELO

【 摘 要 】

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.

【 授权许可】

CC BY   
 All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License