ß-Secretase inhibition by C-methylisoflavones from Abronia nana.
Nat Prod Res
; 33(12): 1705-1712, 2019 Jun.
Article
em En
| MEDLINE
| ID: mdl-29382223
ABSTRACT
The methanol extract of Abronia nana suspension cultures were subjected to column chromatography to identify potential inhibitors of ß-secretase, which is a major factor in Alzheimer's disease development. Two new C-methylisoflavones boeravinone T (1) and U (4) were isolated with three knowns boeravinone B (2), J (3) and X (5). The half-maximal inhibitory concentration (IC50) values of compounds 1-5 were 18.29, 8.57, 7.87, 12.02 and 5.30 µM, respectively. The most potent 5, non-competitively inhibited ß-secretase [inhibition constant (Ki) = 3.79 µM]. Compounds 1-5 did not inhibit other proteases such as chymotrypsin, trypsin and elastase at concentrations up to 1 mM, indicating that they were relatively specific inhibitors of ß-secretase. A free hydroxyl group at C-3 position of the C-methylisoflavone skeleton appeared to be responsible for the stronger inhibitory activity against ß-secretase.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Nyctaginaceae
/
Secretases da Proteína Precursora do Amiloide
Tipo de estudo:
Etiology_studies
/
Prognostic_studies
Limite:
Humans
Idioma:
En
Revista:
Nat Prod Res
Ano de publicação:
2019
Tipo de documento:
Article