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Pharm Biol ; 55(1): 1875-1883, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28629287

RESUMO

CONTEXT: There is an unmet need to discover new treatments for Alzheimer's disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of Carpolobia lutea G. Don (Polygalaceae). OBJECTIVE: The objective of this study is to quantify C. lutea anti-AChE, DPPH free radical scavenging, and antioxidant activities and cell cytotoxicity. MATERIALS AND METHODS: Plant stem, leaves and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0.02-200 µg/mL. Plant DPPH radical scavenging activity, reducing power, and total phenolic and flavonoid contents were determined, and cytotoxicity evaluated using human hepatocytes. RESULTS: Carpolobia lutea exhibited concentration-dependent anti-AChE activity. The most potent inhibitory activity for the stem was the crude ethanol extract and hexane stem fraction oil (IC50 = 140 µg/mL); for the leaves, the chloroform leaf fraction (IC50 = 60 µg/mL); and for roots, the methanol, ethyl acetate and aqueous root fractions (IC50 = 0.3-3 µg/mL). Dose-dependent free radical scavenging activity and reducing power were observed with increasing stem, leaf or root concentration. Total phenolic contents were the highest in the stem: ∼632 mg gallic acid equivalents/g for a hexane stem fraction oil. Total flavonoid content was the highest in the leaves: ∼297 mg quercetin equivalents/g for a chloroform leaf fraction. At 1 µg/mL, only the crude ethanol extract oil was significantly cytotoxic to hepatocytes. DISCUSSION AND CONCLUSIONS: Carpolobia lutea possesses anti-AChE activity and beneficial antioxidant capacity indicative of its potential development as a treatment of Alzheimer's and other diseases characterized by a cholinergic deficit.


Assuntos
Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Descoberta de Drogas , Hepatócitos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Óleos de Plantas/farmacologia , Polygalaceae/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Animais , Antioxidantes/efeitos adversos , Antioxidantes/química , Antioxidantes/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/efeitos adversos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Flavonoides/análise , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Células Hep G2 , Humanos , Masculino , Proteínas do Tecido Nervoso/antagonistas & inibidores , Proteínas do Tecido Nervoso/metabolismo , Nootrópicos/análise , Nootrópicos/química , Nootrópicos/isolamento & purificação , Nootrópicos/farmacologia , Fenóis/análise , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Óleos de Plantas/efeitos adversos , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Raízes de Plantas/química , Caules de Planta/química , Ratos Endogâmicos F344
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