Inhibitory effect of icariin on acetylcholinesterase / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1141-1146, 2012.
Artigo
em Chinês
| WPRIM
| ID: wpr-274686
ABSTRACT
Acetylcholinesterase (AChE) inhibitors are mainly used in the treatment of Alzheimer's disease (AD). The inhibitory effect of icariin on the activity of AChE was investigated by inhibition kinetics. The binding interaction and binding sites between icariin and AChE were also studied by using fluorimetry and molecular docking, respectively. The results showed that icariin could potently inhibit the activity of AChE, the IC50 value was determined to be 3.50 x 10(-8) mol x L(-1), and the determined IC50 value to tacrine was 0.75 x 10(-8) mol x L(-1). Kinetic analyses showed that icariin is a reversible and mixed type AChE inhibitor. The inhibition constants K1 and K(IS) were determined to be 2.67 x 10(-8) and 4.43 x 10(-8) mol x L(-1), respectively. Icariin binds selectively to the AChE peripheral anionic site via hydrogen bonds and Van der Waals forces.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Plantas Medicinais
/
Acetilcolinesterase
/
Sítios de Ligação
/
Flavonoides
/
Medicamentos de Ervas Chinesas
/
Cinética
/
Química
/
Inibidores da Colinesterase
/
Concentração Inibidora 50
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Artigo
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