β-Secretase (BACE1) Inhibitors from Pomegranate (Punica granatum) Husk

다국어 초록 (Multilingual Abstract)

In the course of screening for anti-dementia agents from natural products, two β-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activityguided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 ×10-6 and 4.1×10-7 M and Ki values of 2.4×10-5 and 5.9×10-7 M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to α-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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