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1.
Int J Mol Sci ; 23(19)2022 Sep 22.
Artículo en Inglés | MEDLINE | ID: mdl-36232474

RESUMEN

Aedes aegypti L. (Diptera: Culicidae) is an important transmitter of diseases in tropical countries and controlling the larvae of this mosquito helps to reduce cases of diseases such as dengue, zika and chikungunya. Thus, the present study aimed to evaluate the larvicidal potential of the essential oil (EO) of Ocimum basilicum var. minimum (L.) Alef. The EO was extracted by stem distillation and the chemical composition was characterized by gas chromatography coupled with mass spectrometry (GC/MS and GC-FID). The larvicidal activity of EO was evaluated against third instar Ae. aegypti following World Health Organization (WHO) standard protocol and the interaction of the major compounds with the acetylcholinesterase (AChE) was evaluated by molecular docking. The predominant class was oxygenated monoterpenes with a concentration of 81.69% and the major compounds were limonene (9.5%), 1,8-cineole (14.23%), linalool (24.51%) and methyl chavicol (37.41%). The O. basilicum var. minimum EO showed unprecedented activity against third instar Ae. aegypti larvae at a dose-dependent relationship with LC50 of 69.91 (µg/mL) and LC90 of 200.62 (µg/mL), and the major compounds were able to interact with AChE in the Molecular Docking assay, indicating an ecological alternative for mosquito larvae control.


Asunto(s)
Aedes , Insecticidas , Ocimum basilicum , Aceites Volátiles , Infección por el Virus Zika , Virus Zika , Acetilcolinesterasa , Animales , Eucaliptol , Cromatografía de Gases y Espectrometría de Masas , Insecticidas/química , Insecticidas/farmacología , Larva , Limoneno , Simulación del Acoplamiento Molecular , Monoterpenos , Aceites Volátiles/química , Aceites Volátiles/farmacología , Fitoquímicos/farmacología
2.
Pharmaceuticals (Basel) ; 14(9)2021 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-34577555

RESUMEN

Hancornia speciosa Gomes is a tree native to Brazil and has therapeutic potential for several diseases. Ethnopharmacological surveys have reported that the plant is used as a hypoglycemic agent and to lose weight. This study aimed to evaluate the effects of the aqueous extract from H. speciosa latex (LxHs) in a zebrafish model of diabetes. The extract was evaluated through high-performance thin-layer chromatography (HTPLC), nuclear magnetic resonance (NMR), and Fourier-transform infrared spectroscopy (FT-IR). We then tested treatments with LxHs (500, 1000, and 1500 mg/kg) by assessing blood glucose levels in alloxan-induced diabetic animals, and metformin was used as a control. The toxicity was evaluated through histopathology of the pancreas and biochemical assessment of serum levels of AST, ALT, creatinine, and urea. The extract was also assessed for acute toxicity through several parameters in embryos and adult animals. Finally, we performed in silico analysis through the SEA server and docking using the software GOLD. The phytochemical study showed the compounds cornoside, dihydrocornoide, and 1-O-methyl-myoinositol (bornesitol). The treatment with all doses of LxHs significantly decreased alloxan-induced hyperglycemia without any significant histological or biochemical abnormalities. No significant frequency of teratogenesis was observed in the embryos exposed to the extract, and no significant behavioral changes or deaths were observed in adult animals. In silico, the results showed a potential interaction between inositol and enzymes involved in carbohydrates' metabolism. Overall, the results show a hypoglycemic activity of the extract in vivo, with no apparent toxicity. The computational studies suggest this could be at least partially due to the presence of bornesitol, since inositols can interact with carbohydrates' enzymes.

3.
Biol Pharm Bull ; 34(9): 1499-500, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21881240

RESUMEN

The present work aimed to investigate the vasorelaxant effect of isotirumalin, a dihydroflavonol isolated from Derris urucu (Leguminosae). The vasorelaxant effect of isotirumalin was investigated in the rat aorta, in the presence and in the absence of a functional endothelium. The production of nitric oxide (NO) induced by isotirumalin was measured simultaneously with its vasorelaxation using carbon microsensors. In endothelium-intact aortic rings, isotirumalin induced a concentration-dependent vasodilator effect the concentration required to produce 30% of relaxation (pIC30=4.84±0.24) that was abolished in endothelium-denuded aortic rings or in the presence of Nω-nitro-L-arginine-methyl-ester (L-NAME; 300 µM). In addition, isotirumalin (100 µM) induced a simultaneous and significant increase on NO production, which was blunted in the presence of L-NAME. The present results demonstrate that isotirumalin is a vasodilator in the rat aorta and act by a mechanism dependent on the presence of a functional endothelium and on NO production.


Asunto(s)
Aorta/efectos de los fármacos , Derris/química , Endotelio Vascular/efectos de los fármacos , Flavonoles/farmacología , Óxido Nítrico/fisiología , Vasodilatadores/farmacología , Animales , Aorta/fisiología , Endotelio Vascular/fisiología , Técnicas In Vitro , Masculino , Ratas , Ratas Wistar
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