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.

Highlights

  • Leishmaniasis is a disease of worldwide distribution, present in Africa, Latin America, Asia, and Europe

  • There are several limitations related to their use, such as high financial cost and amphotericin

  • L. amazonensis, unlike the two hydroxylated derivatives that exhibited better results. These results suggest that the lack of a polar hydroxyl group in the p-menthane ring template, as well as the absence of aromaticity might render monoterpenes inactive

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Summary

Introduction

Leishmaniasis is a disease of worldwide distribution, present in Africa, Latin America, Asia, and Europe. Leishmaniasis can be caused by different protozoa species of the genus Leishmania, and the development of the disease is influenced by factors such as parasite species, Molecules 2017, 22, 815; doi:10.3390/molecules22050815 www.mdpi.com/journal/molecules. Bare arethe the first-choice drugs forthe the treatment ofleishmaniasis leishmaniasis Antimonials and. B first-choice drugs for treatment of in Antimonials and amphotericin are the first-choice drugs for the treatment of leishmaniasis inin most countries. There are several limitations related to their use, such as high financial cost and amphotericin. Bare the first-choice drugs the treatment leishmaniasis in most Antimonials countries. There are several limitations related to for their use, such as of high financial cost mostcountries

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