Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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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)
  • Published : 2005.12.01
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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

References

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