Proceedings of the PSK Conference (대한약학회:학술대회논문집)

The Pharmaceutical Society of Korea (대한약학회)
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Green Tea Catechins as a BACE1 ($\beta$-Secretase) Inhibitor

  • Jeon, So-Young (Division of Applied Biology & Chemistry, College of Agriculture & Life sciences, Kyungpook National University) ;
  • Lee, Hee-Ju (College of Pharmacy, Chungnam National University) ;
  • Kim, Ji-Eun (College of Veterinary, Chungbuk National University) ;
  • Bae, Ki-Hwan (College of Veterinary, Chungbuk National University) ;
  • Seong, Yeon-Hee (College of Veterinary, Chungbuk National University) ;
  • Song, Kyung-Sik (College of Veterinary, Chungbuk National University)
  • Published : 2003.10.01
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Abstract

In the course of searching for BACE1 (${\beta}$-secretase) inhibitors from natural products, the ethyl acetate soluble fraction of green tea, which was suspected to be rich in catechin content, showed potent inhibitory activity. (-)-Epigallocatechin gallate, (-)-epicatechin gallate, and (-)-gallocatechin gallate ware isolated with IC$\_$50/ values of 1.6${\times}$10$\^$-6/ M, 4.5${\times}$10$\^$-6/ M, and 1.8${\times}$10$\^$-6/ M, respectively. Seven additional authentic catechins were tested for a fundamental structure-activity relationship. (-)-Catechin gallate, (-)-gallocatechin, and (-)-epigallocatechin significantly inhibited BACE1 activity with IC$\_$50/ values of 6.0${\times}$10$\^$-6/ M, 2.5${\times}$10$\^$-6/ M, and 2.4${\times}$10$\^$-6/ M, respectively. (omitted)

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