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Molecules 2017, 22(5), 815; doi:10.3390/molecules22050815

Leishmanicidal Activity and Structure-Activity Relationships of Essential Oil Constituents

1
Department of Pharmacy, Federal University of Sergipe, 49100-000 São Cristóvão, Sergipe, Brazil
2
Laboratory of Molecular Biology of Pathogenic Bioagents, Department of Morphology, Federal University of Sergipe, 49100-000 São Cristóvão, Sergipe, Brazil
3
Department of Parasitology, Biological Sciences Institute, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Minas Gerais, Brazil
4
Health Science Center, Federal University of Roraima, Av. Cap. Ene Garcez, 69310-000 Boa Vista, Roraima, Brazil
5
Department of Pharmaceutical Products, Federal University of Minas Gerais, 31270-901 Belo Horizonte, Minas Gerais, Brazil
6
Department of Pharmaceutical Sciences, Federal University of Paraíba, 58051-900 João Pessoa, Paraíba, Brazil
7
Laboratory of Parasitology and Tropical Entomology, Department of Morphology, Federal University of Sergipe, 49100-000 São Cristóvão, Sergipe, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 17 March 2017 / Revised: 9 May 2017 / Accepted: 11 May 2017 / Published: 16 May 2017
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Abstract

Several constituents of essential oils have been shown to be active against pathogens such as bacteria, fungi, and protozoa. This study demonstrated the in vitro action of ten compounds present in essential oils against Leishmania amazonensis promastigotes. With the exception of p-cymene, all evaluated compounds presented leishmanicidal activity, exhibiting IC50 between 25.4 and 568.1 μg mL−1. Compounds with the best leishmanicidal activity presented a phenolic moiety (IC50 between 25.4 and 82.9 μg mL−1). Alicyclic alcohols ((−)-menthol and isoborneol) and ketones ((−)-carvone) promoted similar activity against the parasite (IC50 between 190.2 and 198.9 μg mL−1). Most of the compounds showed low cytotoxicity in L929 fibroblasts. Analysis of the structure-activity relationship of these compounds showed the importance of the phenolic structure for the biological action against the promastigote forms of the parasite. View Full-Text
Keywords: monoterpenes; Leishmania amazonensis; leishmanicidal activity; essential oil monoterpenes; Leishmania amazonensis; leishmanicidal activity; essential oil
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Silva, A.R.S.T.; Scher, R.; Santos, F.V.; Ferreira, S.R.; Cavalcanti, S.C.H.; Correa, C.B.; Bueno, L.L.; Alves, R.J.; Souza, D.P.; Fujiwara, R.T.; Dolabella, S.S. Leishmanicidal Activity and Structure-Activity Relationships of Essential Oil Constituents. Molecules 2017, 22, 815.

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