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1.
Fitoterapia ; 155: 105060, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34637885

RESUMEN

In our efforts to find potential agents for the treatment of Alzheimer's disease in naturally occurring compounds, a systematic investigation for the active constituents of Flemingia philippinensis was carried out. Four new prenylated isoflavones, philippinone A-D (1-4), together with six known analogues (5-10), were obtained from the roots of Flemingia philippinensis. Their structures were established through extensive physical and spectroscopic data analysis. All the isolates were evaluated for their inhibitory effect of self-induced Aß aggregation among which compound 5 showed significant Aß aggregation inhibitory ability with the inhibitory rate of 70.56%. The results of molecular docking experiment for compounds 1 and 6 corresponded to that of the thioflavin-T assay. Moreover, the results further clarified the effects of different substituent group of tested compounds on the Aß aggregation inhibition. A preliminary structure-activity relationship is further discussed. Our results suggested that the isoflavonoids may mitigate the progression of AD and compounds 2 and 5 may be a candidate in the treatment of AD.


Asunto(s)
Péptidos beta-Amiloides/antagonistas & inhibidores , Fabaceae/química , Isoflavonas/farmacología , Agregado de Proteínas/efectos de los fármacos , China , Isoflavonas/aislamiento & purificación , Simulación del Acoplamiento Molecular , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Raíces de Plantas/química , Prenilación , Relación Estructura-Actividad
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