Thymol and eugenol derivatives as potential antileishmanial agents

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art_MORAIS_Thymol_and_eugenol_derivatives_as_potential_antileishmanial_agents_2014.PDF (310.53 KB)
Citações na Scopus
101
Tipo de produção
article
Data de publicação
2014
DOI
Scopus
Web of Science
PubMed
Título da Revista
ISSN da Revista
Título do Volume
Editora
PERGAMON-ELSEVIER SCIENCE LTD
Autores
MORAIS, Selene Maia de
VILA-NOVA, Nadja Soares
BEVILAQUA, Claudia Maria Leal
RONDON, Fernanda Cristina
LOBO, Carlos Henrique
MOURA, Arlindo de Alencar Araripe Noronha
SALES, Antonia Debora
RODRIGUES, Ana Paula Ribeiro
FIGUEREIDO, Jose Ricardo de
CAMPELLO, Claudio Cabral
Citação
BIOORGANIC & MEDICINAL CHEMISTRY, v.22, n.21, p.6250-6255, 2014
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
Resumo
In Northeastern Brazil visceral leishmaniasis is endemic with lethal cases among humans and dogs. Treatment is toxic and 5-10% of humans die despite treatment. The aim of this work was to survey natural active compounds to find new molecules with high activity and low toxicity against Leishmania infantum chagasi. The compounds thymol and eugenol were chosen to be starting compounds to synthesize acetyl and benzoyl derivatives and to test their antileishmanial activity in vitro and in vivo against L. i. chagasi. A screening assay using luciferase-expressing promastigotes was used to measure the growth inhibition of promastigotes, and an ELISA in situ was performed to evaluate the growth inhibition of amastigote. For the in vivo assay, thymol and eugenol derivatives were given IP to BALB/c mice at 100 mg/kg/day for 30 days. The thymol derivatives demonstrated the greater activity than the eugenol derivatives, and benzoyl-thymol was the best inhibitor (8.67 +/- 0.28 mu g/mL). All compounds demonstrated similar activity against amastigotes, and acetyl-thymol was more active than thymol and the positive control drug amphotericin B. Immunohistochemistry demonstrated the presence of Leishmania amastigote only in the spleen but not the liver of mice treated with acetyl-thymol. Thus, these synthesized derivatives demonstrated anti-leishmanial activity both in vitro and in vivo. These may constitute useful compounds to generate new agents for treatment of leishmaniasis.
Palavras-chave
Leishmania infatum chagasi, Thymol, Eugenol
URI
https://observatorio.fm.usp.br/handle/OPI/9100
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Coleções
Artigos e Materiais de Revistas Científicas - FM/MPT
Artigos e Materiais de Revistas Científicas - LIM/49