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[ $\beta$ ]-Secretase (BACE1) Inhibitors from Pomegranate (Punica granatum) Husk  

Kwak Hye-Min (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Jeon So-Young (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Sohng Bang-Ho (College of Teachers, Kyungpook National University)
Kim Jong-Guk (School of Life Sciences & Biotechnology, Kyungpook National University)
Lee Jin-Man (Department of Herb & Food Science, Kyungpook College of Sciences)
Lee Kyung-Bok (School of Medicine, Konyang University)
Jeong Hyun­Hee (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Hur Jong-Moon (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Kang Young-Hwa (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Song Kyung-Sik (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University)
Publication Information
Archives of Pharmacal Research / v.28, no.12, 2005 , pp. 1328-1332 More about this Journal
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 $IC_{50}$ values of 3.9 $\times$$10^{-6}$ and 4.1$\times$$10^{-7}$ M and Ki values of 2.4$\times$$10^{-5}$and 5.9$\times$$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 $\alpha$-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.
Keywords
Pomegranate (Punica granatum); Ellagic acid; Punicalagin; Alzheimer's disease;
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