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The Pharmaceutical Society of Korea (대한약학회)
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[ $\beta$ ]-Secretase (BACE1) Inhibitors from Sanguisorbae Radix

  • Lee, Hee-Ju (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University) ;
  • Seong, Yeon-Hee (College of Veterinary Medicine, Chungbuk National University) ;
  • Bae, Ki-Hwan (College of Pharmacy, Chungnam National University) ;
  • Kwon, Soon-Ho (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University) ;
  • Kwak, Hye-Min (School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University) ;
  • Nho, Si-Kab (Department of Natural Fiber Science, College of Agriculture and Life Sciences, Kyungpook National University) ;
  • Kim, Kyung-A (Department of Natural Fiber Science, 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) ;
  • Lee, Kyung-Bok (Department of Biochemistry, School of Medicine, Konyang 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 : 2005.07.01
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Abstract

In the course of screening anti-dementia agents from natural products, two $\beta$-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-$\beta$-D-glucopyranoside (Tellimagrandin II, 1) and 1,2,3,4,6-pentagalloyl-$\beta$-D-glucopyranoside (2) and were shown to non-competitively inhibit $\beta$-secretase (BACE1) with the $IC_{50}$ values of $3.10{\times}10^{-6}M\;and\;3.76{\times}10^{-6}M$, respectively. The Ki values of 1 and 2 were $6.84{\times}10^{-6}M\;and\;5.13{\times}10^{-6}M$. They were less inhibitory to asecretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1.

Keywords

References

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