RESUMO
Alzheimer's disease (AD) is an age-related neurodegenerative disorder. Sever cognitive and memory impairments, huge increase in the prevalence of the disease, and lacking definite cure have absorbed worldwide efforts to develop therapeutic approaches. Since many drugs have failed in the clinical trials due to multifactorial nature of AD, symptomatic treatments are still in the center attention and now, nootropic medicinal plants have been found as versatile ameliorators to reverse memory disorders. In this work, anti-Alzheimer's activity of aqueous extract of areca nuts (Areca catechu L.) was investigated via in vitro and in vivo studies. It depicted good amyloid ß (Aß) aggregation inhibitory activity, 82% at 100 µg/mL. In addition, it inhibited beta-secretase 1 (BACE1) with IC50 value of 19.03 µg/mL. Evaluation of neuroprotectivity of the aqueous extract of the plant against H2O2-induced cell death in PC12 neurons revealed 84.5% protection at 1 µg/mL. It should be noted that according to our results obtained from Morris Water Maze (MWM) test, the extract reversed scopolamine-induced memory deficit in rats at concentrations of 1.5 and 3 mg/kg.
La enfermedad de Alzheimer (EA) es un trastorno neurodegenerativo relacionado con la edad. Los severos deterioros cognitivos y de la memoria, el enorme aumento de la prevalencia de la enfermedad y la falta de una cura definitiva han absorbido los esfuerzos mundiales para desarrollar enfoques terapéuticos. Dado que muchos fármacos han fallado en los ensayos clínicos debido a la naturaleza multifactorial de la EA, los tratamientos sintomáticos siguen siendo el centro de atención y ahora, las plantas medicinales nootrópicas se han encontrado como mejoradores versátiles para revertir los trastornos de la memoria. En este trabajo, se investigó la actividad anti-Alzheimer del extracto acuoso de nueces de areca (Areca catechu L.) mediante estudios in vitro e in vivo. Representaba una buena actividad inhibidora de la agregación de amiloide ß (Aß), 82% a 100 µg/mL. Además, inhibió la beta-secretasa 1 (BACE1) con un valor de CI50 de 19,03 µg/mL. La evaluación de la neuroprotección del extracto acuoso de la planta contra la muerte celular inducida por H2O2 en neuronas PC12 reveló una protección del 84,5% a 1 µg/mL. Cabe señalar que, de acuerdo con nuestros resultados obtenidos de la prueba Morris Water Maze (MWM), el extracto revirtió el déficit de memoria inducido por escopolamina en ratas a concentraciones de 1,5 y 3 mg/kg.
Assuntos
Animais , Ratos , Areca/química , Extratos Vegetais/administração & dosagem , Doença de Alzheimer/tratamento farmacológico , beta-Amilase/antagonistas & inibidores , Peptídeos beta-Amiloides/efeitos dos fármacos , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Ácido Aspártico Endopeptidases/efeitos dos fármacos , Fármacos Neuroprotetores , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Secretases da Proteína Precursora do Amiloide/efeitos dos fármacos , Doença de Alzheimer/enzimologia , Doença de Alzheimer/prevenção & controle , Teste do Labirinto Aquático de Morris , Medicina TradicionalRESUMO
Abstract In the present study, anthelmintic activities of Arundo (A.) donax L., Areca (Ar.) catechu L., and Ferula (F.) assa-foetida L. were determined. Leaves of A. donax L., latex of F. assa-foetida L. and seeds of Ar. catechu L. in different solvent fractions were subjected to in vitro (egg hatch assay; EHA, and adult motility assay; AMA) and in vivo (faecal egg count reduction test; FECRT) tests of anthelmintic activity using Haemonchus contortus model. In the AMA, crude aqueous methanol extracts (CAME) and ethyl acetate fractions of F. assa-foetida at 10 hr post-treatment showed maximum mortality of H. contortus at 12.5-50 mg mL-1. In the EHA, CAME of F. assa-foetida was identified as a potent ovicide based on its low LC50 (16.9 µg mL-1), followed in order by Ar. catechu and A. donax. Results from the FECRT also showed the extract of F. assa-foetida L. to be more effective than those of Ar. catechu L. and A. donax L., against the gastrointestinal parasitic nematodes. Chloroform and ethyl acetate fractions showed better anthelmintic activities against the adult worms in vitro, while CAME of these plants were better than their crude powders in vivo. It is recommended to document and investigate indigenous knowledge of possible medicinal plants to plan scientific trials that may justify their endorsement.
Resumo No presente estudo, as atividades anti-helmínticas de Arundo (A.) donax L., Areca (Ar.) Catechu L. e Ferula (F.) assa-foetida L. foram determinadas. Folhas de A. donax L., látex de F. assa-foetida L. e sementes de Ar. catechu L. em diferentes frações de solvente foram submetidos a testes in vitro (teste de eclosão de ovos, EHA e ensaio de motilidade em adultos, AMA); e in vivo (teste de redução da contagem de ovos fecais, FECRT) de atividade anti-helmíntica, usando-se Haemonchus contortus. Na AMA, extratos aquosos brutos de metanol (CAME) e frações de acetato de etila de F. assa-foetida. Dez horas pós-tratamento, apresentaram mortalidade máxima de H. contortus em 12,5-50 mg mL-1. No EHA, CAME de F. assa-foetida foi identificado como um ovicida potente baseado em seu baixo LC50 (16,9 µg mL-1), seguido em ordem por Ar. catechu e A. donax. Os resultados do FECRT também mostraram que o extrato de F. assa-foetida L. é mais eficaz do que o de Ar. catechu L. e A. donax L., contra nematoides parasitas gastrointestinais. As frações clorofórmio e acetato de etila mostraram melhores atividades anti-helmínticas contra vermes adultos in vitro, enquanto o CAME dessas plantas foi melhor do que o pó bruto in vivo. Recomenda-se documentar e investigar o conhecimento indígena de possíveis plantas medicinais para planejar ensaios científicos que possam justificar seu endosso.
Assuntos
Animais , Ferula , Haemonchus , Anti-Helmínticos/farmacologia , Areca , Extratos Vegetais/farmacologia , PoaceaeRESUMO
Areca catechu Linn belongs to Palm Arecaceaes family, popularly known as Betel palm, originated from tropical countries of Oceania and East Africa. Popularly known for its wide pharmacological activity, Areca catechu has also antibacterial, antihelmintic, antioxidant and detoxifying activity. In its composition is found carbohydrates, fibers, fats, flavonoids, tannins, alkaloids and minerals, and its nut is the main product with medicinal use. In this study, we tested the action of A. catechu L. on in vitro hatchability of eggs of sheep gastrointestinal nematode Haemonchus contortus. The seed was broken and dried at 37C, crushed in 2 mm size and its contents were extracted with a solution of acetone:water (70:30), filtered, rotoevaporated and freeze dried. For the main solution it was used 300 mg of plant extract, mixed at 2850 µl of distilled water and DMSO (150 µl), that was diluted in decreasing concentrations (50 mg/ml, 25 mg/mL, 12.5 mg/ml, 6.25 mg/ml, 3.12 mg/ml, 1.56 mg/ml and 0.78 mg/ml). A hundred eggs of H. contortus were added to different concentrations of A. catechu extract in 48-well plate, and incubated for 24 hours at 27C to evaluate their effectiveness. Data were analyzed with SAS Probit (SAS Inst., Inc., Cary, NC) estimating the LC50 and the independent variables (dose). The results showed that at doses of 7.45 mg/mL can inhibit 50% of the hatchability of eg
O artigo não possui resumo em português.
RESUMO
Areca catechu Linn belongs to Palm Arecaceaes family, popularly known as Betel palm, originated from tropical countries of Oceania and East Africa. Popularly known for its wide pharmacological activity, Areca catechu has also antibacterial, antihelmintic, antioxidant and detoxifying activity. In its composition is found carbohydrates, fibers, fats, flavonoids, tannins, alkaloids and minerals, and its nut is the main product with medicinal use. In this study, we tested the action of A. catechu L. on in vitro hatchability of eggs of sheep gastrointestinal nematode Haemonchus contortus. The seed was broken and dried at 37C, crushed in 2 mm size and its contents were extracted with a solution of acetone:water (70:30), filtered, rotoevaporated and freeze dried. For the main solution it was used 300 mg of plant extract, mixed at 2850 µl of distilled water and DMSO (150 µl), that was diluted in decreasing concentrations (50 mg/ml, 25 mg/mL, 12.5 mg/ml, 6.25 mg/ml, 3.12 mg/ml, 1.56 mg/ml and 0.78 mg/ml). A hundred eggs of H. contortus were added to different concentrations of A. catechu extract in 48-well plate, and incubated for 24 hours at 27C to evaluate their effectiveness. Data were analyzed with SAS Probit (SAS Inst., Inc., Cary, NC) estimating the LC50 and the independent variables (dose). The results showed that at doses of 7.45 mg/mL can inhibit 50% of the hatchability of eg
O artigo não possui resumo em português.