Earticle

초록

영어

Various plant phenolics were assessed for (B-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 IC50 values of 5.87x10-8-54.93x10-6 M. Among them, rugosin E was the most potent (IC50 5.87x10-8 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 a-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.

목차

Abstract
 Introduction
 Materials and Methods
 Results and Discussion
 Acknowledgments
 References

키워드

저자

• Jun, Mi-Ra [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University ]
• Lee, Seung-Ho [ College of Pharmacy, Yeungnam University ]
• Choi, Sun-Ha [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University ]
• Bae, Ki-Hwan [ College of Pharmacy, Chungnam National University ]
• Seong, Yeon-Hee [ College of Veterinary, Chungbuk National University ]
• Lee, Kyung-Bok [ Department of Biochemistry, College of Medicine, Konyang University ]
• Song, Kyung-Sik [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University ] Corresponding author

참고문헌

발행기관

간행물

표지보기 관심저널 등록

• 간행물명

  Food Science and Biotechnology

• 간기

  격월간

• pISSN

  1226-7708

• 수록기간

  1992~2009

• 십진분류

  KDC 574 DDC 664