Journal article
Thymol and eugenol derivatives as potential antileishmanial agents
Bioorganic & medicinal chemistry, Vol.22(21), pp.6250-6255
11/01/2014
DOI: 10.1016/j.bmc.2014.08.020
PMCID: PMC5106290
PMID: 25281268
Abstract
Thymol and eugenol derivatives as anti-leishmanial agents
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 100mg/kg/day for 30days. The thymol derivatives demonstrated the greater activity than the eugenol derivatives, and benzoyl-thymol was the best inhibitor (8.67±0.28μg/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.
Details
- Title: Subtitle
- Thymol and eugenol derivatives as potential antileishmanial agents
- Creators
- Selene Maia de Morais - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilNadja Soares Vila-Nova - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilClaudia Maria Leal Bevilaqua - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilFernanda Cristina Rondon - Laboratório de Doenças Parasitárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilCarlos Henrique Lobo - Laboratório de Biologia da Reprodução, Universidade Federal do Ceará, Av. Mister Hull s/n, Campus do Pici, 60021-970 Fortaleza, Ceará, BrazilArlindo de Alencar Araripe Noronha Moura - Laboratório de Biologia da Reprodução, Universidade Federal do Ceará, Av. Mister Hull s/n, Campus do Pici, 60021-970 Fortaleza, Ceará, BrazilAntônia Débora Sales - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilAna Paula Ribeiro Rodrigues - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilJosé Ricardo de Figuereido - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilClaudio Cabral Campello - Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, BrazilMary E Wilson - Department of Internal Medicine, University of Iowa and the VA Medical Center, Iowa City, IA 52242, USAHeitor Franco de Andrade - Laboratório de Protozoologia, Universidade de São Paulo, Avenida Eneas de Carvalho Aguiar, 470, 05403-000 São Paulo, SP, Brazil
- Resource Type
- Journal article
- Publication Details
- Bioorganic & medicinal chemistry, Vol.22(21), pp.6250-6255
- DOI
- 10.1016/j.bmc.2014.08.020
- PMID
- 25281268
- PMCID
- PMC5106290
- NLM abbreviation
- Bioorg Med Chem
- ISSN
- 0968-0896
- eISSN
- 1464-3391
- Publisher
- Elsevier Ltd
- Language
- English
- Date published
- 11/01/2014
- Academic Unit
- Microbiology and Immunology; International Programs; Epidemiology; Internal Medicine
- Record Identifier
- 9984001148702771
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