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1.
Molecules ; 28(11)2023 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-37298835

RESUMO

Molecular docking is widely used in the assessment of the therapeutic potential of pharmaceutical agents. The binding properties of beta-carotene (BC) to acetylcholine esterase (AChE) proteins were characterized using the molecular docking method. The mechanism of AChE inhibition was assessed by an experimental in vitro kinetic study. In addition, the role of BC action was tested by the zebrafish embryo toxicity test (ZFET). The results of the docking ability of BC to AChE showed significant ligand binding mode. The kinetic parameter, i.e., the low AICc value shown as the compound was the competitive type of inhibition of AChE. Further, BC also showed mild toxicity at a higher dose (2200 mg/L) in ZFET assessment with changes in biomarkers. The LC50 value of BC is 1811.94 mg/L. Acetylcholine esterase (AChE) plays a pivotal role in the hydrolysis of acetylcholine, which leads to the development of cognitive dysfunction. BC possesses the regulation of acetylcholine esterase (AChE) and acid phosphatase (AP) activity to prevent neurovascular dysfunction. Therefore, the characterization of BC could be used as a pharmaceutical agent for the treatment of cholinergic neurotoxicity-associated neurovascular disorders such as developmental toxicity, vascular dementia, and Alzheimer's disease due to its AChE and AP inhibitory actions.


Assuntos
Doença de Alzheimer , Inibidores da Colinesterase , Animais , Inibidores da Colinesterase/química , Acetilcolina , beta Caroteno , Simulação de Acoplamento Molecular , Peixe-Zebra/metabolismo , Doença de Alzheimer/tratamento farmacológico , Acetilcolinesterase/metabolismo , Preparações Farmacêuticas
2.
Molecules ; 16(4): 3037-47, 2011 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-21478819

RESUMO

This study was designed to investigate the antimicrobial activity of Cinnamomum iners standardized leave methanolic extract (CSLE), its fractions and isolated compounds. CSLE and fractions were subjected to disc diffusion, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) tests using different Gram positive and Gram negative bacteria and yeast. Within the series of fractions tested, the ethyl acetate fraction was the most active, particularly against methicillin resistant Staphylococcus aureus (MRSA) and Escherichia coli, with MIC values of 100 and 200 µg/mL, respectively. The active compound in this fraction was isolated and identified as xanthorrhizol [5-(1, 5-dimethyl-4-hexenyl)-2-methylphenol] by various spectroscopic techniques. The overall results of this study provide evidence that Cinnamomum iners leaves extract as well as the isolated compound xanthorrhizol exhibit antimicrobial activity for both Gram negative and Gram positive pathogens, especially against MRSA strains.


Assuntos
Anti-Infecciosos/farmacologia , Cinnamomum/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Cromatografia Gasosa-Espectrometria de Massas , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier
3.
Nat Prod Res ; 27(10): 888-95, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-22574706

RESUMO

This review describes the morphological, phytochemical and pharmacological properties of Cinnamomum iners Reinw. ex Blume (Lauraceae). The plant grows wild in the lowland of Malaysia, India, Myanmar, Indonesia, Thailand, Singapore, Brunei and Philippines. This plant is commonly used for its carminative, analgesic and antipyretic properties, for postpartum treatment, rheumatism and digestive ailments. This article enumerates an overview of phytochemical and pharmacological aspects that is useful to researchers for further exploration necessary for the development of this potential herb.


Assuntos
Cinnamomum/química , Analgésicos/química , Analgésicos/uso terapêutico , Antipiréticos/química , Antipiréticos/uso terapêutico , Brunei , Sistema Digestório/efeitos dos fármacos , Índia , Indonésia , Malásia , Filipinas
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