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The search for new compounds with biocidal potential was carried out, focusing on the longipinenes 1-7 from the plant species Santolina viscosa Lag. Compounds 1, 2, and 5 showed remarkable molecular diversity when treated in acidic reaction conditions. Protonic, Lewis, and heterogeneous compounds were used in the treatment. Three main models of reaction have been observed: isomerization of the double bond (8-10); rearrangements to longibornane-based skeleton (11-15) and ring-opening to himachalane-based skeleton (16-18). Secolongibornane aldehydes 23 and 24 were obtained after epoxide opening under the same reaction conditions. The elucidation of the structures of the new compounds was carried out using spectroscopic data and was supported by computational theoretical calculations of 13C NMR spectra. Additionally, high-resolution mass spectrometry and single-crystal X-ray diffraction analysis were employed for certain compounds. Natural longipinenes 4-7, methyl esters 1-3 of corresponding natural carboxylic acids and the isomerized and derivatives compounds 8-19 exhibit moderate to high insecticidal activity against R. padi and M. persicae insects. Longipinene 5 shows potent inhibition against the root growth of the plants L. perenne and L. sativa, as well as compound 2 on the leaves of L. perenne. Furthermore, significant ixocidal and nematicidal activity was found for this latter compound.
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Insecticidas , Animales , Insecticidas/química , Insecticidas/farmacología , Catálisis , Estructura Molecular , Norbornanos/química , Norbornanos/farmacologíaRESUMEN
[This corrects the article DOI: 10.3389/fpls.2022.804104.].
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The continuous search for natural product-based biopesticides from fungi isolated from untapped sources is an effective tool. In this study, we studied a pre-selected fungal endophyte, isolate Aa22, from the medicinal plant Artemisia absinthium, along with the antifungal, insect antifeedant and nematicidal compounds present in the extract. The endophyte Aa22 was identified as Stemphylium solani by molecular analysis. The antifungal activity was tested by broth microdilution against Fusarium solani, F. oxysporum, F. moniliforme and Botrytis cinerea, the insect antifeedant by choice bioassays against Spodoptera littoralis, Myzus persicae and Rhopalosiphum padi and the in vitro mortality against the root-knot nematode Meloiydogyne javanica. The structures of bioactive compounds were determined on the basis of 1D and 2D NMR spectroscopy and mass spectrometry. The ethyl acetate extract obtained from the solid rice fermentation showed mycelial growth inhibition of fungal pathogens (EC50 0.08-0.31 mg/mL), was antifeedant to M. persicae (99%) and nematicidal (68% mortality). A bioguided fractionation led to the isolation of the new compound stempholone A (1), and the known stempholone B (2) and stemphol (3). These compounds exhibited antifeedant (EC50 0.50 mg/mL), antifungal (EC50 0.02-0.43 mg/L) and nematicidal (MLD 0.5 mg/mL) activities. The extract activities can be explained by 3 (antifungal), 1-3 (antifeedant) and 1 (nematicidal). Phytotoxicity tests on Lolium perenne and Lactuca sativa showed that the extract and 1 increased L. sativa root growth (121-130%) and 1 reduced L. perenne growth (48-49%). These results highlight the potential of the endophytic fungi Aa22 as biotechnological source of natural product-based biopesticides.
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Antifúngicos , Antinematodos , Endófitos , Animales , Endófitos/química , Antifúngicos/farmacología , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Antinematodos/farmacología , Antinematodos/aislamiento & purificación , Antinematodos/química , Fusarium/efectos de los fármacos , Spodoptera/efectos de los fármacos , Spodoptera/crecimiento & desarrollo , Ascomicetos/efectos de los fármacos , Botrytis/efectos de los fármacos , Botrytis/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana , Tylenchoidea/efectos de los fármacosRESUMEN
This work presents the biocidal effects and chemical compositions of two essential oils (EOs) obtained by hydrodistillation of Eucalyptus flocktoniae subsp. flocktoniae and E. flocktoniae subsp. hebes. The two subspecies studied had different chemical composition, when analysed by gas chromatography coupled to mass spectrometry with 1,8-cineole (56.98%), trans-pinocarveol (20.38%) and α-pinene (5.86%) being the major components of E. flocktoniae subsp. flocktoniae and spathulenol (25.09%), p-cymene (21.20%), 1,8-cineole (10.74%) and α-pinene (8.93%) are the major components of E. flocktoniae subsp. hebes. These oils were evaluated for their insect antifeedant, nematicidal and phytotoxic activities. The biocidal tests showed that E. flocktoniae subsp. hebes was the most active against Myzus persicae and Rhopalosiphum padi. While, E. flocktoniae subsp. flocktoniae was not antifeedant. None of the investigated EOs were active against both Spodoptera littoralis and Meloidogyne javanica root-knot nematode. Moreover, the EOs extracted from these two subspecies showed a significant phytotoxic effect.
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The chemical composition, insect antifeedant, in vtro/in vivo nematicidal activity, phytotoxicity, and in silico nematicidal activity of the essential oil (EO) of the African medicinal plant Drypetes gossweileri were studied. Chemical analysis using GC/MS indicated that benzyl isothiocyanate (96.23%) was the major compound, followed by benzyl cyanide (1.38%). The biocidal effects of this oil were tested against insect pests and root-knot nematodes. All the insect species tested were significantly affected by the oil according to their feeding adaptations (Spodoptera littoralis and Myzus persicae were less affected than Rhopalosiphum padi) with efficient doses (EC50) of 29.4 8.3 µg/cm2, 14.744 8.3 µg/cm2, and 8.3 µg/cm2, respectively. The oil was highly effective against juveniles J2 of the nematode Meloidogyne javanica, with LC50-LC90 values of 0.007 mg/mL-0.0113 mg/mL. D. gossweileri EO at minimum lethal concentrations (MLC) and below strongly inhibited egg hatching in vitro, whereas soil treatment caused a strong suppression of nematode population, infection frequency, and multiplication rate. The EO inhibited ryegrass (Lolium perenne) germination at 0.4 mg/mL, while at 0.1 mg/mL, its effects on germination, root and leaf growth were moderate (32.4%, 8.4%, and 18.3%, respectively). The tomato (Solanum lycopersicum) germination was not affected by the EO, but the root growth was reduced (56% at 0.1 mg/mL) at a dose 10 times higher than the LD50 calculated for M. javanica J2 mortality. Molecular docking of the nematicidal effects of the oil using PyRx revealed a strong interaction between potassium chloride transporting KCC3 (PDB ID: 7D90) and benzyl cyanide at a distance of 2.20 A° with GLN C:350, followed by benzyl isothiocyanate at a distance of 2.78 A° with ARG B:294. The in vivo nematicidal effects of D. gossweileri EO on M. javanica penetration and reproduction in tomato roots further support the potential of this EO as a nematicidal agent with insect antifeedant effects, which could be used by local farmers for crop protection.
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Kinetoplastida is a group of flagellated protozoa characterized by the presence of a kinetoplast, a structure which is part of a large mitochondria and contains DNA. Parasites of this group include genera such as Leishmania, that cause disease in humans and animals, and Phytomonas, that are capable of infecting plants. Due to the lack of treatments, the low efficacy, or the high toxicity of the employed therapeutic agents there is a need to seek potential alternative treatments. In the present work, the antiparasitic activity on Leishmania infantum and Phytomonas davidi of 23 essential oils (EOs) from plants of the Lamiaceae and Asteraceae families, extracted by hydrodistillation (HD) at laboratory scale and steam distillation (SD) in a pilot plant, were evaluated. The chemical compositions of the EOs were determined by gas chromatography-mass spectrometry. Additionally, the cytotoxic activity on mammalian cells of the major components from the most active EOs was evaluated, and their anti-Phytomonas and anti-Leishmania effects analyzed. L. infantum was more sensitive to the EOs than P. davidi. The EOs with the best anti-kinetoplastid activity were S. montana, T. vulgaris, M. suaveolens, and L. luisieri. Steam distillation increased the linalyl acetate, ß-caryophyllene, and trans-α-necrodyl acetate contents of the EOs, and decreased the amount of borneol and 1,8 cineol. The major active components of the EOs were tested, with thymol being the strongest anti-Phytomonas compound followed by carvacrol. Our study identified potential treatments against kinetoplastids.
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Aceites Volátiles , Plantas Medicinales , Trypanosomatina , Humanos , Animales , Aceites Volátiles/química , Vapor , Timol/análisis , Aceites de Plantas/química , MamíferosRESUMEN
Cannabis has been used for decades as a palliative therapy in the treatment of cancer. This is because of its beneficial effects on the pain and nausea that patients can experience as a result of chemo/radiotherapy. Tetrahydrocannabinol and cannabidiol are the main compounds present in Cannabis sativa, and both exert their actions through a receptor-mediated mechanism and through a non-receptor-mediated mechanism, which modulates the formation of reactive oxygen species. These oxidative stress conditions might trigger lipidic changes, which would compromise cell membrane stability and viability. In this sense, numerous pieces of evidence describe a potential antitumor effect of cannabinoid compounds in different types of cancer, although controversial results limit their implementation. In order to further investigate the possible mechanism involved in the antitumoral effects of cannabinoids, three extracts isolated from Cannabis sativa strains with high cannabidiol content were analyzed. Cell mortality, cytochrome c oxidase activity and the lipid composition of SH-SY5Y cells were determined in the absence and presence of specific cannabinoid ligands, with and without antioxidant pre-treatment. The cell mortality induced by the extracts in this study appeared to be related to the inhibition of the cytochrome c oxidase activity and to the THC concentration. This effect on cell viability was similar to that observed with the cannabinoid agonist WIN55,212-2. The effect was partially blocked by the selective CB1 antagonist AM281, and the antioxidant α-tocopherol. Moreover, certain membrane lipids were affected by the extracts, which demonstrated the importance of oxidative stress in the potential antitumoral effects of cannabinoids.
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Cannabis , Neuroblastoma , Extractos Vegetales , Humanos , Cannabidiol/análisis , Cannabinoides/análisis , Cannabis/química , Dronabinol/farmacología , Complejo IV de Transporte de Electrones/metabolismo , Neuroblastoma/tratamiento farmacológico , Extractos Vegetales/química , Extractos Vegetales/uso terapéuticoRESUMEN
In this work, we have studied the benzofurans of Pericallis echinata (aerial parts and transformed roots), P. steetzii (aerial parts and transformed roots), P. lanata (aerial parts), and P. murrayi (aerial parts and roots). This work has permitted the isolation of the new benzofurans 10-ethoxy-11-hydroxy-10,11-dihydroeuparin (10), (-)-eupachinin A ethyl ether (12), 11,15-didehydro-eupachinin A (13), 10,12-dihydroxy-11-angelyloxy-10,11-dihydroeuparin (14), 2,4-dihydroxy-5-formyl-acetophenone (15) isolated for the first time as a natural product, 11-angelyloxy-10,11-dihydroeuparin (16), and 12-angelyloxyeuparone (17), along with several known ones (1-9, 11). In addition, the incubation of the abundant component, 6-hydroxytremetone (1), with the fungus Mucor plumbeus has been studied. Benzofurans in the tremetone series (1, 1a, 2-5, 18, 18a), the euparin series (6, 7, 7a, 8-10, 14, 16), and the eupachinin-type (11, 12) were tested for antifeedant effects against the insect Spodoptera littoralis. The antifeedant compounds (1, 4, 6, 11, 12) were further tested for postingestive effects on S. littoralis larvae. The most antifeedant compounds were among the tremetone series, with 3-ethoxy-hydroxy-tremetone (4) being the strongest antifeedant. Glucosylation of 1 by its biotransformation with Mucor plumbeus gave inactive products. Among the euparin series, the dihydroxyangelate 14 was the most active, followed by euparin (6). The eupachinin-type compounds (11, 12) were both antifeedants. Compounds 4, 11, and 12 showed antifeedant effects without postingestive toxicity to orally dosed S. littoralis larvae. Euparin (6) had postingestive toxicity that was enhanced by the synergist piperonyl butoxide.
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Benzofuranos , Insecticidas , Animales , Insectos , Mucor , Larva , Benzofuranos/farmacología , Spodoptera , Insecticidas/farmacologíaRESUMEN
The development of Cannabis sativa strains with high cannabidiol (CBD) and low tetrahydrocannabinol (THC) content is a growing field of research, both for medical and recreational use. However, the mechanisms behind clinical actions of cannabinoids are still under investigation, although there is growing evidence that mitochondria play an important role in many of them. Numerous studies have described that cannabinoids modulate mitochondrial activity both through activation of mitochondrial cannabinoid receptors and through direct action on other proteins such as mitochondrial complexes involved in cellular respiration. Thus, the aim of this study was to determine the actions of a panel of extracts, isolated from high-CBD varieties of Cannabis sativa, on the activity of the mitochondrial electron transport chain complex IV, cytochrome c oxidase (CCO), in order to select those with a safer profile. After demonstrating that Cannabis sativa strains could be identified by cannabinoids content, concentration-response curves were performed with a collection of extracts from strains with high-CBD and low-THC content using bovine CCO. The CCO rate was clearly modified by specific extracts of Cannabis sativa plants compared to others. Half maximal inhibitory concentrations (IC50) of extracts and the inhibitory effects evoked at 1 × 10-4 g/mL displayed a significant correlation with the THC. Therefore, the screening of extracts based on CCO activity provides a powerful and rapid methodology to identify those plants with higher mitochondrial toxicity or even mito-protective actions.
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Cannabidiol , Cannabinoides , Cannabis , Animales , Bovinos , Dronabinol/farmacología , Complejo IV de Transporte de Electrones , Extractos Vegetales/farmacología , Cannabinoides/farmacología , Cannabidiol/farmacología , Biomarcadores , MitocondriasRESUMEN
Trichomonas gallinae is a flagellated protozoan that parasitizes the upper digestive tract of various bird species and causes avian trichomonosis. The emergence of resistant strains to the standard treatment, based on nitroimidazoles, increases the need to find alternative therapies. In this study, 36 essential oils (EOs) from Lamiaceae and Asteraceae plant families were tested against T. gallinae trophozoites using the 3-(4,5-dimethylthiazol-2-yl-)-2,5-dipheniltetrazolium bromide (MTT) reduction assay. Among them, EOs from distinct species of Lamiaceae, including the genera Lavandula, Salvia, Thymus, Origanum, and Satureja were the ones reporting better anti-trichomonal activity, and were selected for further analysis, including chemical composition and in vitro assays. The chemical composition of the selected EOs was determined by gas chromatography followed by mass spectrometry and 19 pure compounds were tested against the protozoa, according to their higher abundance in the active EOs. Pure compounds which displayed the highest activity against T. gallinae trophozoites, ordered by highest to lowest activity, were α and ß-thujones, camphene, ß-pinene, linalyl acetate, thymol, 4-terpineol, γ-terpinene, α-pinene, p-cymene, D-fenchone and ß-caryophyllene. A dose dependent effect was observed in most of the EOs and pure compounds tested. The toxicity test conducted in eukaryotic cell cultures with the anti-trichomonal active pure compounds showed that ß-caryophyllene, camphene, α-pinene, and ß-pinene were slightly toxic for Vero cells, and the selectivity index was calculated. Based on the anti-trichomonal activity and the absence of cytotoxicity results, natural products from Lamiaceae plants could be useful as alternative therapy against avian trichomonosis, mainly those containing linalyl acetate, thymol, 4-terpinenol, γ-terpinene, p-cymene and D-fenchone.
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Active metabolites from plants are considered safer than synthetic chemicals for the control of plant-parasitic nematodes of the genus Meloidogyne. In the present work, 75 aqueous extracts (AEs) from different vegetative parts of 34 native plant species of the Yucatan Peninsula were evaluated against second-stage juveniles (J2s) of Meloidogyne incognita and M. javanica in microdilution assays. The highest mortality (M) against both Meloidogyne species was produced by the foliar AE from Alseis yucatanensis (M ≥ 94%) and Helicteres baruensis (M ≥ 77%) at 3% w/v after 72 h. Other active AEs at 3% were from the leaves of Croton itzaeus and stems of H. baruensis (M: 87-90%) on M. javanica and the stems of Annona primigenia and the leaves of Morella cerifera on M. incognita (M: 92-97%). The AEs from A. yucatanensis had the lowest LD50 against M. incognita (0.36% w/v), and against M. javanica (3.80% w/v). In an acute ecotoxicity assay of the most promising AEs using non-target earthworms (Eisenia fetida), the AE of A. yucatanensis had slight acute toxicity (LD50: 2.80% w/v), and the rest of the most active AEs were not ecotoxic. These tropical plants are potential candidates for further studies as biorational agents for controlling Meloidogyne species.
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Plant essential oils (EOs) are gaining interest as biopesticides for crop protection. EOs have been recognized as important ingredients of plant protection products including insecticidal, acaricidal, fungicidal, and nematicidal agents. Considering the growing importance of EOs as active ingredients, the domestication and cultivation of Medicinal and Aromatic Plants (MAPs) to produce chemically stable EOs contributes to species conservation, provides the sustainability of production, and decreases the variations in the active ingredients. In addition to these direct effects on plant pests and diseases, EOs can induce plant defenses (priming effects) resulting in better protection. This aspect is of relevance considering that the EU framework aims to achieve the sustainable use of new plant protection products (PPPs), and since 2020, the use of contaminant PPPs has been prohibited. In this paper, we review the most updated information on the direct plant protection effects of EOs, focusing on their modes of action against insects, fungi, and nematodes, as well as the information available on EOs with plant defense priming effects.
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The chemical composition of essential oils (EOs) from ten Peruvian Piper species (Piper coruscans, Pc; P. tuberculatum, Pt; P. casapiense, Pcs; P. obliquum, Po; P. dumosum, Pd; P. anonifolium, Pa; P. reticulatum, Pr; P. soledadense, Ps; P. sancti-felicis, Psf and P. mituense, Pm) has been studied, along with their antifungal and phytotoxic activities. These EOs contained ß-bisabolene/nerolidol (Pc), ß-bisabolene/δ-cadinene/caryophyllene (Pt), caryophyllene oxide (Pcs), bicyclogermacrene/10-epi-Elemol (Po), bicyclogermacrene/germacrene-D/apiol (Pd), caryophyllene/germacrene-D (Pa), germacrene-D (Pr), limonene/apiol (Ps), apiol (Psf), and apiol/bicyclogermacrene (Pm) as major components, and some are described here for the first time (Ps, Pcs, Pm). A composition-based dendrogram of these Piper species showed four major groups (G1: Pc and Pt, G2: Pcs, Po, Pd, Pa, and Pr, G3: Ps, and G4: Psf and Pm). The spore germination effects (Aspergillus niger, Botrytis cinerea, and Alternaria alternate) and phytotoxicity (Lolium perenne and Lactuca sativa) of these EOs were studied. Most of these Piper essential oils showed important activity against phytopathogenic fungi (except G1), especially against B. cinerea. Similarly, most of the essential oils were phytotoxic against L. perenne (except G1), with P. sancti-felicis (G4), P. casapiense (G2), and P. reticulatum (G2) being the most effective. Caryophyllene oxide, ß-caryophyllene, ß-pinene, limonene, α-humulene, and apiol were evaluated against B. cinerea, with the most effective compounds being ß-pinene, apiol, and limonene. This work demonstrates the species-dependent potential of essential oils from Peruvian Piper species as fungicidal and herbicidal agents.
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The hydrolate byproduct resulting from the industrial essential oil extraction of Spanish purple garlic has been studied against the root-knot nematode Meloidogyne javanica by in vitro and in vivo bioassays. The essential oil, the hydrolate and its organic fraction caused high mortality of juveniles, suppressed egg hatch, and reduced nematode infection and reproduction on tomato plants. The nematicidal compounds of garlic oil, diallyl disulfide and diallyl trisulfide, were the major components of the hydrolate organic fraction. These findings have important implications for the development of new nematode control products based on garlic hydrolate compounds and highlight the recovery of waste from essential oils extraction, promoting a circular economy.
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In this work, we studied the direct and indirect plant protection effects of an Artemisia absinthium essential oil (AEO) on tomato seedlings against Fusarium oxysporum sp. oxysporum radicis lycopersici (Fol). AEO exhibited a toxic effect in vitro against Fol. Additionally, tomato seedlings germinated from seeds pretreated with AEO and grown hydroponically were protected against Fol. Plant disease symptoms, including, water and fresh weight loss, tissue necrosis, and chlorosis were less pronounced in AEO-treated seedlings. AEO also contributed to plant defenses by increasing callose deposition and the production of reactive oxygen species (ROS) on seed surfaces without affecting seed germination or plant development. The essential oil seed coating also primed a durable tomato seedling defense against the fungus at later stages of plant development. RNA-seq and metabolomic analysis performed on seedlings after 12 days showed that the AEO treatment on seeds induced transcriptomic and metabolic changes. The metabolomic analysis showed an induction of vanillic acid, coumarin, lycopene, oleamide, and an unknown metabolite of m/z 529 in the presence of Fol. The StNRPD2 gene, the second largest component of RNA polymerases IV and V directly involved in de novo cytosine methylation by RNA-directed DNA methylation (RdDM), was highly induced in the presence of AEO. The host methionine cycle (MTC) controlling trans-methylation reactions, was also altered by AEO through the high induction of S-adenosyl methionine transferases (SAMts). Our results suggest that AEO treatment could induce de novo epigenetic changes in tomato, modulating the speed and extent of its immune response to Fol. The EO-seed coating could be a new strategy to prime durable tomato resistance, compatible with other environmentally friendly biopesticides.
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In the present work, 27 triterpene derivatives have been subjected to 3D-QSAR, ADME-Tox, and molecular docking for their insecticidal activity. The selected derivatives are previously semi-synthesized based on compounds obtained from Euphorbia resinifera and Euphorbia officinarum latex. The in silico studies were used to predict and to evaluate the antibacterial and insecticidal properties of the 3D structure of triterpene derivatives. The 3D-QSAR models are developed using CoMFA and CoMSIA techniques, and they have showed excellent statistical results (R 2 = 0.99; Q 2 = 0.672; R 2 pred = 0.91 for CoMFA and R 2 = 0.97; Q2 = 0.61; R 2 pred = 0.94 for CoMSIA). The results indicate that the built models are able to describe the relationship between the structure of triterpene derivatives and the pLD50 bioactivity. Based on contour maps obtained from CoMFA and CoMSIA models, 38 new molecules are designed and their pLD50 activities are predicted. The drug-like and ADME-Tox properties of the molecule designed are examined and led to the selection of four molecules (55, 56, 59, 64) as promising antibacterial and insecticidal agents. Compounds 55, 56, 59, and 64 are able to inhibit the MurE (PDB code: 1E8C) and EcR (PDB code: 1R20) proteins involved in the process of antibacterial and insecticidal activities. This hypothesis is confirmed by the implementation of a molecular docking test. This test predicted the most important referential interactions that occur between the structure of triterpene derivatives and the targeted receptors. Among the four docked molecules, three molecules (55, 56, and 59) showed greater stability than the reference molecule 16 inside the MurE and EcR receptors pocket. Therefore, the structure of the three new triterpene derivatives can be adopted as reference for the synthesis of antibacterial drugs and also in the development of insecticides.
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In this work, we have investigated the accumulation of ryanoids in different plant parts (leaves, stems and roots) of aeroponically grown Persea indica cloned trees (one-year-old cloned individuals) and a selected mature, wild tree. We tested the insect antifeedant (against Spodoptera littoralis, Myzus persicae and Rhopalosiphum padi) and nematicidal (against Meloidogyne javanica) effects of ethanolic extracts from these different plant parts. The HPLC-MS analysis of P. indica extracts showed that mature tree (wild) leaves had two times more chemical diversity than stems. Aeroponic plants showed fewer differences in chemical diversity between leaves and stems, with the lowest diversity found in the roots. Ryanodane epiryanodol (1) was present in all the plant parts, with the mature stems (wild) containing the highest amount. The aeroponic stems also accumulated ryanoids including 1, cinnzeylanol (2) and cinnzeylanone (4). The insect Spodoptera littoralis was strongly affected by the stem extracts, while leaf extracts were moderately active. Based on predicted vs. real antifeedant values, we concluded that the ryanoid content (1 or a combination of 2, 4 and 1) explained the antifeedant effects of the stem extracts, while additional components contributed to the activity of the leaf extracts. Therefore, careful individual selection of P. indica seedlings should be carried out prior to proceeding with aeroponic cultivation in order to obtain ryanodane-rich stem or leaf extracts with strong antifeedant effects on S. littoralis.
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The production of reactive oxygen species (ROS) increases considerably in situations of cellular stress, inducing lipid peroxidation and multiple alterations in proteins and nucleic acids. However, sensitivity to oxidative damage varies between organs and tissues depending on the triggering process. Certain drugs used in the treatment of diverse diseases such as malaria have side effects similar to those produced by oxidative damage, although no specific study has been conducted. For this purpose, cell membrane microarrays were developed and the superoxide production evoked by the mitochondrial activity was assayed in the presence of specific inhibitors: rotenone, antimycin A and azide. Once the protocol was set up on cell membrane isolated from rat brain areas, the effect of six antimalarial drugs (atovaquone, quinidine, doxycycline, mefloquine, artemisinin, and tafenoquine) and two essential oils (Rosmarinus officinalis and Origanum majoricum) were evaluated in multiple human samples. The basal activity was different depending on the type of tissue, the liver, jejunum and adrenal gland being the ones with the highest amount of superoxide. The antimalarial drugs studied showed specific behavior according to the type of human tissue analyzed, with atovaquone and quinidine producing the highest percentage of superoxide formation, and doxycycline the lowest. In conclusion, the analysis of superoxide production evaluated in cell membranes of a collection of human tissues allowed for the characterization of the safety profile of these antimalarial drugs against toxicity mediated by oxidative stress.
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Tick control is a priority in order to prevent the transmission of vector-borne diseases. Industrial chemical acaricides and repellents have been the most efficient tools against hard ticks for a long time. However, the appearance of resistances has meant the declining effectiveness of the chemicals available on the market. The trend today is to develop alternative control methods using natural products to replace nonefficient pesticides and to preserve the efficient ones, hoping to delay resistance development. Traditional in vitro evaluation of acaricidal activity or resistance to synthetic pesticides have been reviewed and they mainly focus on just one species, the one host tick (Rhipicephalus (Boophilus) microplus (Acari: Ixodidae)). Recent reports have called for the standardization of natural product components, extraction techniques, and experimental design to fully discover their acaricidal potential. This study reviews the main variables used in the bibliography about the efficiency of natural products against ticks, and it proposes a unification of variables relating to ticks, practical development of bioassays, and estimation of ixodicidal activity.