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Cytotoxic and Antileishmanial Effects of the Monoterpene β-Ocimene

Pharmaceuticals, ISSN: 1424-8247, Vol: 16, Issue: 2
2023
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Investigators from Laboratory for Infectious Diseases Target Pharmaceuticals (Cytotoxic and Antileishmanial Effects of the Monoterpene Beta-ocimene)

2023 APR 12 (NewsRx) -- By a News Reporter-Staff News Editor at NewsRx Drug Daily -- New research on Drugs and Therapies - Pharmaceuticals is

Article Description

Leishmaniasis is a group of infectious-parasitic diseases with high mortality rates, and endemic in many regions of the globe. The currently available drugs present serious problems such as high toxicity, costs, and the emergence of drug resistance. This has stimulated research into new antileishmania drugs based on natural products and their derivatives. β-Ocimene is a monoterpene found naturally in the essential oils of many plant species which presents antileishmanial activity, and which has not yet been evaluated for its potential to inhibit the etiological agent of leishmaniasis. The aim of this work was to evaluate the activity of β-ocimene against Leishmania amazonensis, its cytotoxicity, and potential mechanisms of action. β-Ocimene presented direct activity against the parasite, with excellent growth inhibition of promastigotes (IC = 2.78 μM) and axenic amastigotes (EC = 1.12 μM) at concentrations non-toxic to RAW 264.7 macrophages (CC = 114.5 µM). The effect is related to changes in membrane permeability and resulting abnormalities in the parasitic cell shape. These were, respectively, observed in membrane integrity and atomic force microscopy assays. β-Ocimene was also shown to act indirectly, with greater activity against intra-macrophagic amastigotes (EC = 0.89 μM), increasing TNF-α, nitric oxide (NO), and reactive oxygen species (ROS), with lysosomal effects, as well as promoting decreases in IL-10 and IL-6. Against intra-macrophagic amastigote forms the selectivity index was higher than the reference drugs, being 469.52 times more selective than meglumine antimoniate, and 42.88 times more selective than amphotericin B. Our results suggest that β-ocimene possesses promising in vitro antileishmania activity and is a potential candidate for investigation in in vivo assays.

Bibliographic Details

Sousa, Julyanne Maria Saraiva de; Nunes, Thaís Amanda de Lima; Rodrigues, Raiza Raianne Luz; Sousa, João Paulo Araújo de; Val, Maria da Conceição Albuquerque; Coelho, Francisco Alex da Rocha; Santos, Airton Lucas Sousa Dos; Maciel, Nicolle Barreira; Souza, Vanessa Maria Rodrigues de; Machado, Yasmim Alves Aires; Sousa, Paulo Sérgio de Araújo; Araújo, Alyne Rodrigues de; Rocha, Jefferson Almeida; Sousa, Damião Pergentino de; Silva, Marcos Vinicius da; Arcanjo, Daniel Dias Rufino; Rodrigues, Klinger Antônio da Franca

MDPI AG

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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