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beta-Secretase (BACE1) inhibitors from pomegranate (Punica granatum) husk
Hye-Min Kwak1, So-Young Jeon, Bang-Ho Sohng
1School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University, Daegu, Korea.
Abstract:
In the course of screening for anti-dementia agents from natural products, two beta-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activity-guided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 x10(-6) and 4.1x10(-7) M and Ki values of 2.4x10(-5) and 5.9x10(-7) M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.
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