Earticle

초록

영어

The deposition of the amyloid β (Aβ)-peptide following proteolytic processing of amyloid precursor protein (APP)by β-secretase (BACE1) and γ-secretase is critical feature in the progress of Alzheimer’s disease (AD). Consequently,BACE1, a key enzyme in the production of Aβ, is a prime target for therapeutic intervention in AD. In the course of searchingfor BACE1 inhibitors from natural sources, the ethyl acetate fraction of Petasites japonicus showed potent inhibitory activity.Two BACE1 inhibitors quercetin (QC) and kaempferol 3-O-(6''-acetyl)-β-glucopyranoside (KAG) were isolated from P.japonicus by activity-guided purification. QC, in particular, non-competitively attenuated BACE1 activity with IC50 value of2.1×10−6 M and Ki value of 3.7×10−6 M. Both compounds exhibited less inhibition of α-secreatase (TACE) and other serineproteases including chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific and selective inhibitors toBACE1. Furthermore, both compounds significantly reduced the extracellular Aβ secretion in APP695-transfected B103 cells.

목차

Abstract
 Introduction
 Materials and Methods
 Results and Discussion
 Acknowledgments
 References

키워드

저자

• Kyung-Sik Song [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 702-701, Korea ]
• Sun-Ha Choi [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 702-701, Korea ]
• Jong-Moon Hur [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 702-701, Korea ]
• Hyo-Jun Park [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 702-701, Korea ]
• Eun-Ju Yang [ Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 702-701, Korea ]
• Inhee Mook-Jung [ Department of Biochemistry, College of Medicine, Seoul National University, Seoul 110-799, Korea ]
• Jung-Hyun Yi [ Division of Food Science, Dong-A University, Busan 604-714, Korea ]
• Mira Jun [ Division of Food Science, Dong-A University, Busan 604-714, Korea ] 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