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Food science and biotechnology v.15 no.4 = no.70, 2006년, pp.617 - 624   피인용횟수: 3

Plant Phenolics as ${\beta}$-Secretase (BACE1) Inhibitors

Jun, Mi-Ra   (Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National UniversityUU0000096  ); Lee, Seung-Ho   (College of Pharmacy, Yeungnam UniversityUU0000951  ); Choi, Sun-Ha   (Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National UniversityUU0000096  ); Bae, Ki-Hwan   (College of Pharmacy, Chungnam National UniversityUU0001302  ); Seong, Yeon-Hee   (College of Veterinary, Chungbuk National UniversityUU0001309  ); Lee, Kyung-Bok   (Department of Biochemistry, College of Medicine, Konyang UniversityUU0000053  ); Song, Kyung-Sik   (Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National UniversityUU0000096  );
  • 초록

    Various plant phenolics were assessed for ( ${\beta}$ -secretase (BACE1) inhibitory activity in order to screen for anti-dementia agents. Among 39 phenolics, eight compounds, 1,2,3-trigalloyl glucopyranoside, acetonyl geraniin, euphorscopin, furosine, helioscopinin A, helioscopinin B, jolkinin, and rugosin E exhibited strong inhibition of BACE1 with $IC_{50}$ values of $5.87{\times}10^{-8}-54.93{\times}10^{-6}\;M$ . Among them, rugosin E was the most potent ( $IC_{50}$ $5.87{\times}10^{-8}\;M$ ). The active compounds were shown to be non-competitive inhibitors by Dixon plot. All the phenolic BACE1 inhibitors except furosin also suppressed prolyl endopeptidase (PEP) activity. However, these phenolic compounds caused less inhibition of ${\alpha}$ -secretase (tumor necrosis factor a converting enzyme; TACE) and no significant inhibition of other serine proteases such as trypsin, chymotrypsin, and elastase was seen, demonstrating that they are relatively specific to both BACE1 and PEP. No significant structure-activity relationships were found.


  • 주제어

    ${\beta}$-secretase .   inhibitor .   plant phenolics .   Alzheimer's disease.  

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