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1.
Chem Biol Interact ; 242: 273-9, 2015 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-26456888

RESUMO

The objective of this study was to evaluate the potential anticonvulsant effect of isopentyl ferulate, a new ester derived from ferulic acid in mice (Mus musculus) subjected to two models of induced seizures. According to the results obtained, the IF at doses of 25, 50 and 75 mg/kg (i.p.) showed protective effect against induced seizures by pilocarpine (400 mg/kg, i.p.) and pentylenetetrazole (70 mg/kg, i.p.). In the two animal models of seizures, the pretreatment of the IF (25, 50 and 75 mg/kg) with flumazenil blocked the anticonvulsant effect, suggesting that the mechanism of action of this ester derived of ferulic acid may be related to activity in the benzodiazepine-binding site of the GABAA receptor (γ-aminobutyric acid, type A). In addition to the anticonvulsant effect, behavioral changes as neurotoxicity indication were assessed by using the rota rod and open field tests. The results obtained showed that the IF (25, 50 and 75 mg/kg) does not induce significant changes in locomotor activity and motor coordination when compared with the control group, unlike the results presented by diazepam. Thus, these results demonstrate a new pharmacological knowledge of IF with potential application against epileptic seizures. However, further studies are needed to elucidate other neurobiological mechanisms underlying epilepsy.


Assuntos
Anticonvulsivantes/farmacologia , Comportamento Animal/efeitos dos fármacos , Ácidos Cumáricos/farmacologia , Animais , Anticonvulsivantes/química , Anticonvulsivantes/uso terapêutico , Ácidos Cumáricos/química , Ácidos Cumáricos/uso terapêutico , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Pentilenotetrazol/efeitos adversos , Pilocarpina/efeitos adversos , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Convulsões/fisiopatologia
2.
Chem Biol Interact ; 225: 47-53, 2015 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-25446849

RESUMO

Essential oils have played a prominent role in research on natural products, due to the high level of bioactive constituents, which include those derived from phenylpropanoids or terpenoids. This study aimed to evaluate the antioxidant capacity of isopentyl ferulate (IF) employing in vitro experimental models for elimination of the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS+), hydroxyl (OH) and nitric oxide (NO), as well as its capacity to electron transfer by reducing potential and inhibition of lipid peroxidation by TBARS (thiobarbituric acid reactive substances) method. In all in vitro antioxidants protocols, isopentyl ferulate showed to be potent in a concentration of 54.4 nM, presenting a percentage inhibition of 91.29±0.57, 92.63±0.28, 83.62±0.18, 77.07±0.72 and 79.51±0.32% for DPPH, ABTS+, hydroxyl, nitric oxide and TBARS level, respectively. The increase of absorbance at 700 nm in the concentrations of 3.4, 6.8, 13.6, 27.2 and 54.4 nM shows the reducing potential of IF. Similar results were obtained with Trolox (559 nM), a hydrophilic synthetic analogue of α-tocopherol, which is widely used as a standard antioxidant. The present study demonstrated that isopentyl ferulate has an antioxidant activity in vitro experimental models, suggesting that this compound could enhance the development of a new product with antioxidant properties. However, further in vivo studies are needed to assign possible implications in the treatment of diseases related with free radicals.


Assuntos
Ácidos Cumáricos/química , Sequestradores de Radicais Livres/química , Benzotiazóis/química , Compostos de Bifenilo/química , Radical Hidroxila/química , Óxido Nítrico/química , Oxirredução , Picratos/química , Ácidos Sulfônicos/química , Substâncias Reativas com Ácido Tiobarbitúrico/análise
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