Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/12092
Title: In vitro evaluation of (−)α-bisabolol as a promising agent against Leishmania amazonensis
Authors: Rottini, Mariana Margatto
Amaral, Ana Claudia Fernandes
Ferreira, Jose Luiz Pinto
Silva, Jefferson Rocha de Andrade
Taniwaki, Noemi Nosomi
Souza, Celeste da Silva Freitas de
d’Escoffier, Luiz Ney
Souza, Fernando Almeida
Hardoim, Daiana de Jesus
Costa, Sylvio Celso Gonçalves da
Calabrese, Kátia da Silva
Affilliation: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Farmanguinhos. Laboratório de Plantas Medicinais e Derivados. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Farmanguinhos. Laboratório de Plantas Medicinais e Derivados. Rio de Janeiro, RJ, Brasil.
UFAM. Departamento de Química. Laboratório de Cromatografia. Manaus, AM, Brasil.
Instituto Adolfo Lutz. Núcleo de Microscopia Eletrônica. São Paulo, SP, Brasil
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil.
Abstract: Current treatments for leishmaniasis present some difficulties due to their toxicity, the use of the intravenous route for administration and therapy duration, which may lead to treatment discontinuation. The aim of this study is to investigate new treatment alternatives to improve patients well being. Therefore, we evaluated the inhibitory effect of (−)α-bisabolol, a sesquiterpene alcohol found in various essential oils of different plant species, against the promastigotes and intracellular amastigotes forms of Leishmania amazonensis, as well as the cytotoxic, morphological and ultrastructural alterations of treated cells. Promastigotes forms of L. amazonensis were incubated with (−)α-bisabolol to determine the antileishmanial activity of this compound. The cytotoxicity effect was evaluated by testing against J774.G8 cells. After these tests, the infected and uninfected cells with L. amazonensis were used to determine if the (−)α- bisabolol was able to kill intracellular parasites and to cause some morphological changes in the cells. The (−)α-bisabolol compound showed significant antileishmanial activity against promastigotes with a 50% effective concentration of 8.07 μg/ml (24 h) and 4.26 μg/ml (48 h). Against intracellular amastigotes the IC50 (inhibitory concentration) of (−)α-bisabolol (24 h) was 4.15 μg/ml. The (−)α-bisabolol also showed a cytotoxic effect against the macrophage strain J774.G8. The value of 50% cytotoxic concentration was 14.82 μg/ml showing that (−)α-bisabolol is less toxic to macrophages than to the parasite. Ultrastructural studies of treated promastigotes and amastigotes showed several alterations, such as loss of cytoplasmic organelles, including the nucleus, and the presence of lipid inclusions. This study showed that (−)α- bisabolol has promising antileishmanial properties, as it can act against the promastigote forms and is able to penetrate the cell, and is also active against the amastigote forms. About 69% of the promastigotes forms suffered mitochondrial membrane damage after treatment with IC50 of (-)α-bisabolol, suggesting inhibition of the metabolic activity of parasites. These results open new prospects for research that can contribute to the development of products based on essential oils or isolated compounds from plants for the treatment of cutaneous leishmaniasis.
Keywords: (−)α-bisabolol
Leishmania amazonensis
Promastigotes
Cutaneous leishmaniasis
DeCS: Leishmania
Leishmaniose
Leishmaniose Cutânea
Issue Date: 2015
Publisher: Elsevier
Citation: ROTTINI, Mariana Morgatto; et al. In vitro evaluation of (−)α-bisabolol as a promising agent against Leishmania amazonensis. Experimental Parasitology, v.148, p.66-72, Jan. 2015.
DOI: 10.1016/j.exppara.2014.10.001
ISSN: 0014-4894
Copyright: restricted access
Appears in Collections:Farmanguinhos - Artigos de Periódicos
IOC - Artigos de Periódicos

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