Expression of recombinant human acetylcholinesterase and its application in screening its inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 50-54, 2014.
Artículo
en Inglés
| WPRIM
| ID: wpr-297972
ABSTRACT
This study is designed to obtain recombinant human acetylcholinesterase (rhAChE) and apply it in screening acetylcholinesterase inhibitors. The rhAChE was overexpressed in HEK293 cells transfected by plasmid of pCMV-AChE with the cationic liposome and rhAChE was found to be secreted into cell culture medium. AChE activity was assayed according to modified Ellman method to obtain kinetic parameters. IC so50 values for donepezil compounds of rhAChE were calculated to determine their activities of inhibition. The results showed that Km value was 151.9 micromol.L-1 donepezil inhibited rhAChE in a mixed competitive-noncompetitive way (Ki= 16.03 nmol.L-1, Ki = 18.36 nmol.L-1) and that most new compounds tested exhibited high activities of inhibition on rhAChE. The study suggests that rhAChE is available to be applied in screening AChE inhibitors in vitro.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Piperidinas
/
Plásmidos
/
Acetilcolinesterasa
/
Proteínas Recombinantes
/
Cinética
/
Transfección
/
Inhibidores de la Colinesterasa
/
Concentración 50 Inhibidora
/
Células HEK293
Tipo de estudio:
Estudio diagnóstico
/
Estudio de tamizaje
Límite:
Humanos
Idioma:
Inglés
Revista:
Acta Pharmaceutica Sinica
Año:
2014
Tipo del documento:
Artículo
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