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1.
Neurochem Res ; 34(5): 973-83, 2009 May.
Artículo en Inglés | MEDLINE | ID: mdl-18853256

RESUMEN

Considering the important role of oxidative stress in the pathogenesis of several neurological diseases, and the growing evidence of the presence of compounds with antioxidant properties in the plant extracts, the aim of the present study was to investigate the antioxidant capacity of three plants used in Brazil to treat neurological disorders: Melissa officinalis, Matricaria recutita and Cymbopogon citratus. The antioxidant effect of phenolic compounds commonly found in plant extracts, namely, quercetin, gallic acid, quercitrin and rutin was also examined for comparative purposes. Cerebral lipid peroxidation (assessed by TBARS) was induced by iron sulfate (10 microM), sodium nitroprusside (5 microM) or 3-nitropropionic acid (2 mM). Free radical scavenger properties and the chemical composition of plant extracts were assessed by 1'-1' Diphenyl-2' picrylhydrazyl (DPPH) method and by Thin Layer Chromatography (TLC), respectively. M. officinalis aqueous extract caused the highest decrease in TBARS production induced by all tested pro-oxidants. In the DPPH assay, M. officinalis presented also the best antioxidant effect, but, in this case, the antioxidant potencies were similar for the aqueous, methanolic and ethanolic extracts. Among the purified compounds, quercetin had the highest antioxidant activity followed by gallic acid, quercitrin and rutin. In this work, we have demonstrated that the plant extracts could protect against oxidative damage induced by various pro-oxidant agents that induce lipid peroxidation by different process. Thus, plant extracts could inhibit the generation of early chemical reactive species that subsequently initiate lipid peroxidation or, alternatively, they could block a common final pathway in the process of polyunsaturated fatty acids peroxidation. Our study indicates that M. officinalis could be considered an effective agent in the prevention of various neurological diseases associated with oxidative stress.


Asunto(s)
Antioxidantes/farmacología , Cymbopogon/química , Melissa/química , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Compuestos Ferrosos/farmacología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Ácido Gálico/farmacología , Técnicas In Vitro , Masculino , Nitrocompuestos/farmacología , Nitroprusiato/farmacología , Fenoles/análisis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Propionatos/farmacología , Quercetina/análogos & derivados , Quercetina/farmacología , Ratas , Ratas Wistar , Rutina/farmacología , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo
2.
Biomed Pharmacother ; 84: 476-484, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27685791

RESUMEN

Caused by Trichomonas vaginalis, trichomoniasis is the most common non-viral STD worldwide. Currently, metronidazole and tinidazole are the only drugs approved for treatment of the condition. However, problems such as metronidazole-resistant T. vaginalis isolates and allergic reactions have been reported. Based on data previously published by our group, structural changes in betulinic acid (1) were performed, generating three new compounds that were tested for in vitro anti-T.vaginalis activity in this study. Whereas derivative 2 did not demonstrate anti-T. vaginalis activity, derivatives 3 and 4 reduced trophozoite viability by 100%, with MIC values of 50µM. The structural difference of two compounds was performed only on the C-28 position. Derivative 3 showed low cytotoxicity against Vero cells in 24h; however, derivative 4 was highly cytotoxic, but efficient when associated with metronidazole in the synergism assay. ROS production by neutrophils was reduced, and derivative 3 showed anti-inflammatory effect. Collectively, the results of this study provide in vitro evidence that betulinic acid derivatives 3 and 4 are potential compounds with anti-T. vaginalis activity.


Asunto(s)
Antiprotozoarios/farmacología , Trichomonas vaginalis/efectos de los fármacos , Triterpenos/farmacología , Animales , Antiprotozoarios/química , Muerte Celular/efectos de los fármacos , Chlorocebus aethiops , Evaluación Preclínica de Medicamentos , Células HeLa , Hemólisis/efectos de los fármacos , Humanos , Cinética , Pruebas de Sensibilidad Microbiana , Neutrófilos/efectos de los fármacos , Parásitos/efectos de los fármacos , Triterpenos Pentacíclicos , Especies Reactivas de Oxígeno/metabolismo , Trichomonas vaginalis/aislamiento & purificación , Triterpenos/química , Células Vero , Ácido Betulínico
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