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1.
Food Chem Toxicol ; 145: 111703, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32858133

RESUMO

Hippeastrum psittacinum, Amaryllidaceae, is used in traditional medicine as a purgative, aphrodisiac, and anticough remedy. The ethanol extract (EE) and alkaloid-rich fractions (ARF) from H. psittacinum bulbs were evaluated for their acetylcholinesterase (AChE) inhibition. The EE cytotoxic and anti-inflammatory effects in RAW 264.7 cells, and the neuroprotective and genotoxic activities in SH-SY5Y cells, were also estimated. Fifteen alkaloids were identified in the EE by gas chromatography-mass spectrometry. ARFs were less active for AChE inhibition than EE. The viability of both cell lines was higher than 70% with EE concentrations below 25 µg/mL. The EE decreased nitrite release in RAW cells stimulated with lipopolysaccharide, showing values of 83, 67, and 53% at 6.25, 12.5, and 25 µg/mL, respectively. Furthermore, the EE partially protected SH-SY5Y cells from hydrogen peroxide-mediated deleterious effects by approximately 50% at the same concentrations. The micronucleus assays showed that the extract caused chromosomal missegregation at concentrations above 12.5 µg/mL. The in silico analyses showed that some alkaloids presented properties of permeation of the blood-brain barrier and the intestine. Our findings present new evidence of the potential of H. psittacinum potential as an AChE inhibitor, as well as an anti-inflammatory and neuroprotective agent.


Assuntos
Amaryllidaceae/química , Anti-Inflamatórios/farmacologia , Inibidores da Colinesterase/farmacologia , Fármacos Neuroprotetores/farmacologia , Acetilcolinesterase/química , Alcaloides/química , Alcaloides/farmacologia , Alcaloides de Amaryllidaceae/química , Alcaloides de Amaryllidaceae/farmacologia , Animais , Anti-Inflamatórios/química , Linhagem Celular Tumoral , Inibidores da Colinesterase/química , Simulação por Computador , Flores/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Camundongos , Simulação de Acoplamento Molecular , Fármacos Neuroprotetores/química , Células RAW 264.7
2.
Food Chem Toxicol ; 109(Pt 2): 996-1002, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28238772

RESUMO

Eugenia dysenterica ex DC Mart. (Myrtaceae) is a Brazilian tree with pharmacological and biological properties. The aqueous leaf extract, rich in polyphenols, was tested in the human neuroblastoma cell line SH-SY5Y to evaluate its effect on cell viability. The extract and two isolated compounds were also assessed for the potential inhibitory activity on acetylcholinesterase, an enzyme related to Alzheimer's disease. A simple chromatographic method using Sephadex LH-20 was developed to separate catechin and quercetin from the aqueous leaf extract of E. dysenterica. Identification was carried out by spectroscopic techniques IR, UV, and 1H and 13C NMR. The IC50 values were obtained by constructing dose-response curves on a graph with percentage inhibition versus log of inhibitor concentration and compared with physostigmine, a well-known AChE inhibitor. The extract was toxic for SH-SY5Y cells at concentrations higher than 7.8 µg/ml given for 24 h. The decline in SH-SY5Y cell viability appears to be related to its antiproliferative activity. The extract also showed relatively moderate acetylcholinesterase inhibitory activity of 66.33% ± 0.52% at 1.0 mg/ml with an IC50 value of 155.20 ± 2.09 µg/ml. Physostigmine, quercetin, and catechin showed IC50 values of 18.69 ± 0.07, 46.59 ± 0.49, and 42.39 ± 0.67 µg/ml, respectively.


Assuntos
Inibidores da Colinesterase/química , Eugenia/química , Extratos Vegetais/química , Brasil , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Colinesterases/química , Humanos , Cinética , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química
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