Abstract
Background This investigation was designed to evaluate the insecticidal, antiplasmodial, anti-leishmanial, and cytotoxic effects of Capparis spinosa essential oil (CSEO) and its main components, methyl isothiocyanate, hexadecanoic acid, and limonene. Methods Insecticidal activity of CSEO and its main components, methyl isothiocyanate, hexadecanoic acid, and limonene, was determined against Aedes aegypti 4th-instar larvae at 25 ± 2°C. Antiplasmodial and anti-leishmanial effects of CSEO and its main components were carried out against chloroquine-resistant Plasmodium falciparum K1 strain and Leishmania major amastigotes based on the Malstat method and the macrophage model, respectively. We also performed the cytotoxic activity of CZEO and its main components against J774A1 macrophage cells using the colorimetric MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. In addition, the plasma membrane permeability and caspase-3-like activity CSEO and its main components were evaluated against L. major. Results CSEO and its main components showed considerable (p < 0.001) larvicidal activity against Ae. aegypti larva. The 50% lethal concentration values for CSEO, methyl isothiocyanate, hexadecanoic acid, and limonene were 21.6, 30.9, 41.6, and 35.3 μg/mL, respectively. By antiplasmodial effects, the 50% inhibitory concentration (IC50) values for CSEO, methyl isothiocyanate, hexadecanoic acid, and limonene were 7.4, 14.5, 19.6, and 21.3 μg/mL, respectively, while these values for their anti-leishmanial effects were 9.1, 20.7, 23.3, and 18.6 μg/mL, respectively. The 50% cytotoxic concentration values for CSEO, methyl isothiocyanate, hexadecanoic acid, and limonene were 93.7, 216.2, 199.4, and 221.3 μg/mL, respectively. Different concentrations of CSEO and its main components significantly (p < 0.05) increased the plasma membrane permeability and caspase-3-like activity against L. major promastigote level as dose-dependent response. Conclusion Based on the obtained results, C. spinosa essential oil and its main components, methyl isothiocyanate, hexadecanoic acid, and limonene, displayed insecticidal, antiplasmodial, and anti-leishmanial activity against healthy 4th-instar larvae of A. aegypti, chloroquine-resistant P. falciparum K1 strain, and L. major amastigotes, respectively. However, further surveys are required to display the mechanisms of action mode of tested drugs and their efficacy in animal model and clinical settings.
Highlights
Mosquitoes are considered as the main vectors of a wide range of important human infectious diseases including malaria, dengue, filariasis, encephalitis, and yellow fever, which cause high mortality around the world [1]
To evaluate the anti-leishmanial effects of Capparis spinosa essential oil (CSEO) and its main components, methyl isothiocyanate, hexadecanoic acid, and limonene (3.125, 6.25, 12.5, 25, 50, and 100 μg/mL), against the intracellular amastigote of L. major (MRHO/IR/75/ER), J774A1 macrophage cells (5 × 105 cells/ml) were poured in sterile 6-well plates and incubated at 37°C for 24 hours with 5% CO2 to adhere to macrophages
Evaluating the Caspase-3-Like Activity of Extract-Treated Promastigotes. e effects of CSEO, methyl isothiocyanate, hexadecanoic acid, and limonene on the induction of apoptosis were evaluated by the colorimetric protease (Sigma, Germany) method according to the manufacturer recommendations
Summary
Mosquitoes are considered as the main vectors of a wide range of important human infectious diseases including malaria, dengue, filariasis, encephalitis, and yellow fever, which cause high mortality around the world [1]. A number of synthetic agents are applied to treat leishmaniasis; recent reviews have proven that most of the synthetic and chemical anti-leishmanial compounds have some limitations (e.g., drug resistance and long-term treatment), toxicity, and side effects [13]. Natural products and their derivatives as an inexpensive, accessible, and useful alternative medicine are broadly applied for the treatment of a wide range of diseases such as infectious ones [14]. E current investigation was designed to evaluate the insecticidal, antiplasmodial, anti-leishmanial, and cytotoxic effects of C. spinosa essential oil and its main components, methyl isothiocyanate, hexadecanoic acid, and limonene
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