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Archives of Pharmacal Research

, Volume 28, Issue 7, pp 799–803 | Cite as

β-Secretase (BACE1) inhibitors from Sanguisorbae Radix

  • Hee-Ju Lee
  • Yeon-Hee Seong
  • Ki-Hwan Bae
  • Soon-Ho Kwon
  • Hye-Min Kwak
  • Si-Kab Nho
  • Kyung-A Kim
  • Jong-Moon Hur
  • Kyung Bok Lee
  • Young-Hwa Kang
  • Kyung-Sik Song
Articles Drug Design

Abstract

In the course of screening anti-dementia agents from natural products, two β-secretase (BACE1) inhibitors were isolated from the ethyl acetate soluble fraction of Sanguisorbae Radix by the activity-guided purification using silica gel, Sephadex LH-20, and RP-HPLC. They were identified as 1,2,3-trigalloyl-4,6-hexahydroxydiphenoyl-β-d-glucopyranoside (Tellimagrandin II,1) and 1,2,3,4,6-pentagalloyl-β-d-glucopyranoside (2) and were shown to non-competitively inhibit β-secretase (BACE1) with the IC50 values of 3.10×10−6 M and 3.76×10−6 M, respectively. TheKi values of1 and2 were 6.84×10−6 M and 5.13×10−6 M. They were less inhibitory to α-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1.

Key words

β-Secretase (BACE1) Inhibitor Sanguisorbae Radix Tellimagrandin II 1,2,3,4,6-Pentagalloyl-β-d-glucopyranoside Alzheimer's disease 

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Copyright information

© The Pharmaceutical Society of Korea 2005

Authors and Affiliations

  • Hee-Ju Lee
    • 1
  • Yeon-Hee Seong
    • 2
  • Ki-Hwan Bae
    • 3
  • Soon-Ho Kwon
    • 1
  • Hye-Min Kwak
    • 1
  • Si-Kab Nho
    • 5
  • Kyung-A Kim
    • 5
  • Jong-Moon Hur
    • 1
  • Kyung Bok Lee
    • 4
  • Young-Hwa Kang
    • 1
  • Kyung-Sik Song
    • 1
  1. 1.School of Applied Biosciences, College of Agriculture and Life SciencesKyungpook National UniversityDaeguKorea
  2. 2.College of Veterinary MedicineChungbuk National UniversityChungbukKorea
  3. 3.College of PharmacyChungnam National UniversityDaejonKorea
  4. 4.Department of Biochemistry, School of MedicineKonyang UniversityNonsanKorea
  5. 5.Department of Natural Fiber Science, College of Agriculture and Life SciencesKyungpook National UniversityDaeguKorea

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