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1.
Chem Biodivers ; 18(9): e2100242, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34242481

RESUMEN

Most of the hematophagous insects act as disease vectors, including Aedes aegypti, responsible for transmitting some of the most critical arboviruses globally, such as Dengue. The use of repellents based on natural products is a promising alternative for personal protection compared to industrial chemical repellents. In this study, the repellent effect of essential oils extracted from Lippia thymoides, Lippia alba, Cymbopogon winterianus, and Eucalyptus globulus leaves was evaluated. Essential oils used showed repellent activity against Ae. aegypti in laboratory bioassays, obtaining protection rates above 70 % from 3.75 mg/mL and higher concentration for all analyzed oils. GC/MS identified 57 constituents, which were used in the ligand-based pharmacophore model to expose compounds with requirements for repellents that modulate mosquitoes behavior through odorant-binding protein 1 Ae. aegypti. Ligand-based pharmacophore model approach results suggested that repellent activity from C. winterianus, L. alba, and L. thymoides essential oils' metabolites is related to Citronelal (QFIT=26.77), Citronelol (QFIT=11.29), Citronelol acetate (QFIT=52.22) and Geranil acetate (QFIT=10.28) with synergistic or individual activity. E. globulus essential oil's repellent activity is associated with Ledol (0.94 %; QFIT=41.95). Molecular docking was applied to understand the binding mode and affinity of the essential oils' data set at the protein binding site. According to molecular docking, Citronelol (ChemPLP=60.98) and geranyl acetate (ChemPLP=60.55) were the best-classified compounds compared to the others and they can be explored to develop new repellents.


Asunto(s)
Aedes/efectos de los fármacos , Insecticidas/farmacología , Simulación del Acoplamiento Molecular , Aceites Volátiles/farmacología , Animales , Bioensayo , Cymbopogon/química , Eucalyptus/química , Insecticidas/química , Insecticidas/aislamiento & purificación , Lippia/química , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Hojas de la Planta/química
2.
Anal Bioanal Chem ; 406(26): 6691-700, 2014 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-25171830

RESUMEN

Visceral leishmaniasis (VL) is a zoonosis whose etiologic agent in the Americas is Leishmania infantum, and dogs are the main host. Research and innovation in diagnostic techniques are essential to improve the surveillance and control of VL in endemic areas. The present study investigates the profile of the volatile organic compounds (VOCs) emitted by healthy dogs and by dogs infected by L. infantum to detect variations in the VOCs that may be used as biomarkers in the diagnosis of VL. In total, 36 dogs were selected from an endemic area and divided into three groups: G1, not infected with L. infantum; G2, infected without clinical signs of VL; and G3, infected with clinical signs of VL. To analyze the profiles of the VOCs emitted by dogs from the three groups, solid-phase microextraction (SPME) combined with gas chromatography-mass spectrometry (GC-MS) was used. Variations were observed between the profiles of the VOCs emitted in the three groups studied, and they also differentiated infected animals with or without clinical signs. Six VOCs were identified as potential biomarkers of infection, with significant variations between healthy dogs (G1) and infected dogs (G2 + G3). The detection of variations between groups G2 and G3 suggested that the profiles of some VOCs may be related to the type of immune response and the parasite load of the infected dogs. This study demonstrated the possibility of analysis of VOCs as biomarkers of VL in diagnostic, clinical, and epidemiological work.


Asunto(s)
Perros/parasitología , Cabello/microbiología , Leishmania infantum/aislamiento & purificación , Leishmaniasis Visceral/veterinaria , Compuestos Orgánicos Volátiles/análisis , Animales , Biomarcadores/análisis , Cromatografía de Gases y Espectrometría de Masas , Cabello/química , Humanos , Leishmaniasis Visceral/diagnóstico , Leishmaniasis Visceral/parasitología , Microextracción en Fase Sólida
3.
Artículo en Inglés | MEDLINE | ID: mdl-39031313

RESUMEN

This article reviews the literature on the consumption, street drug analysis, distribution, and main environmental impacts of illicit drugs in Brazil and analyzes the III National Survey on Drug Use by the Brazilian Population. The literature review is based on articles published in national and international journals between 2018 and 2023. This review consists of two analyses, the first of which addresses publications from the last 6 years on the monitoring of illicit drugs in Brazil and a second analysis based on the III National Survey on Drug Use that addresses the different possibilities of contact with drugs. The results revealed that the Southeast region of Brazil has the highest number of studies on the subject, especially in the state of São Paulo, while the North and Northeast regions have the lowest number of studies. The Midwest regions only have studies in the federal capital city, Brasília, while no studies were found in states bordering countries that produce illicit drugs, such as Paraguay and Bolivia. Analytical methods that use the concept of miniaturization, green chemistry, and the adoption of acceptance methods are frequent in most articles. Chemometric and statistical tools are widely used for the analysis, development, and conclusion of identification and quantification methods. Among the articles studied, there was a predominance in the analysis of cocaine metabolites and cannabis metabolites in the aquatic environment, where their concentrations ranged from 0.01 to 2000 ng L-1. Studies also reported bioaccumulation in marine biota with concentrations of up to 4.58 µg kg-1 for mussels and sediments, posing a risk to algae, crustaceans, and fish. Furthermore, the data show that the consumption of illicit drugs is increasing in Brazil, especially among young people.

4.
Int J Pharm ; 639: 122965, 2023 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-37084836

RESUMEN

Ivermectin (IVM) is a potent antiparasitic widely used in human and veterinary medicine. However, the low oral bioavailability of IVM restricts its therapeutic potential in many parasitic infections, highlighting the need for novel formulation approaches. In this study, poly(ε-caprolactone) (PCL) nanocapsules containing IVM were successfully developed using the nanoprecipitation method. Pumpkin seed oil (PSO) was used as an oily core in the developed nanocapsules. Previously, PSO was chemically analyzed by headspace solid-phase microextraction coupled to gas chromatography/mass spectrometry (HS-SPME/GC-MS). The solubility of IVM in PSO was found to be 4266.5 ± 38.6 µg/mL. In addition, the partition coefficient of IVM in PSO/water presented a logP of 2.44. A number of nanocapsule batches were produced by factorial design resulting in an optimized formulation. Negatively charged nanocapsules measuring around 400 nm demonstrated unimodal size distribution, and presented regular spherical morphology under transmission electron microscopy. High encapsulation efficiency (98-100%) was determined by HPLC. IVM-loaded capsules were found to be stable in nanosuspensions at 4 °C and 25 °C, with no significant variations in particle size observed over a period of 150 days. Nanoencapsulated IVM (0.3 mM) presented reduced toxicity to J774 macrophages and L929 fibroblasts compared to free IVM. Moreover, IVM-loaded nanocapsules also demonstrated enhanced in vitro anthelmintic activity against Strongyloides venezuelensis in comparison to free IVM. Collectively, the present findings demonstrate the promising potential of PCL-PSO nanocapsules to improve the antiparasitic effects exerted by IVM.


Asunto(s)
Ivermectina , Nanocápsulas , Humanos , Ivermectina/farmacología , Ivermectina/química , Antiparasitarios/farmacología , Antiparasitarios/química , Nanocápsulas/química , Polímeros , Poliésteres/química
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