Archives of Pharmacal Research

, Volume 28, Issue 12, pp 1328–1332

β-Secretase(BACE1) inhibitors from pomegranate (Punica granatum) husk

  • Hye-Min Kwak
  • So-Young Jeon
  • Bang-Ho Sohng
  • Jong-Guk Kim
  • Jin-Man Lee
  • Kyung-Bok Lee
  • Hyun-Hee Jeong
  • Jong-Moon Hur
  • Young-Hwa Kang
  • Kyung-Sik Song
Articles Drug Design

DOI: 10.1007/BF02977896

Cite this article as:
Kwak, HM., Jeon, SY., Sohng, BH. et al. Arch Pharm Res (2005) 28: 1328. doi:10.1007/BF02977896

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 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.

Key words

Pomegranate (Punica granatum) Ellagic acid Punicalagin β-Secretase inhibitor Alzheimer’s disease 

Copyright information

© The Pharmaceutical Society of Korea 2005

Authors and Affiliations

  • Hye-Min Kwak
    • 5
  • So-Young Jeon
    • 5
  • Bang-Ho Sohng
    • 1
  • Jong-Guk Kim
    • 2
  • Jin-Man Lee
    • 3
  • Kyung-Bok Lee
    • 4
  • Hyun-Hee Jeong
    • 5
  • Jong-Moon Hur
    • 5
  • Young-Hwa Kang
    • 5
  • Kyung-Sik Song
    • 5
  1. 1.College of TeachersKyungpook National UniversityDaeguKorea
  2. 2.School of Life Sciences & BiotechnologyKyungpook National UniversityDaeguKorea
  3. 3.Department of Herb & Food ScienceKyungpook College of SciencesChilgokKorea
  4. 4.School of MedicineKonyang UniversityNonsan, ChungnamKorea
  5. 5.School of Applied Biosciences, College of Agriculture and Life SciencesKyungpook National UniversityDaeguKorea