β-Secretase(BACE1) inhibitors from pomegranate (Punica granatum) husk
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- Kwak, HM., Jeon, SY., Sohng, BH. et al. Arch Pharm Res (2005) 28: 1328. doi:10.1007/BF02977896
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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 activity-guided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 x10-6 and 4.1x10-7 M andKi 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 α-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.