Abstract The methanol extract of Abronia nana suspension cultures were subjected to column chromatography to identify potential inhibitors of β-secretase, which is a major factor in Alzheimer’s disease development. Two… Click to show full abstract
Abstract The methanol extract of Abronia nana suspension cultures were subjected to column chromatography to identify potential inhibitors of β-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 β-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 β-secretase. A free hydroxyl group at C-3 position of the C-methylisoflavone skeleton appeared to be responsible for the stronger inhibitory activity against β-secretase.
               
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