Planta Med 2009; 75(5): 537-540
DOI: 10.1055/s-0029-1185311
Natural Product Chemistry
Letter
© Georg Thieme Verlag KG Stuttgart · New York

A New Specific BACE-1 Inhibitor from the Stembark Extract of Vitis vinifera

Yeon Hee Choi1 , 2 , Mi Young Yoo1 , Chun Whan Choi1 , Mi-Ran Cha1 , Gyu Hwan Yon1 , Dae Young Kwon3 , Young Sup Kim1 , Woo-Kyu Park1 , Shi Yong Ryu1
  • 1Korea Research Institute of Chemical Technology, Daejeon, Korea
  • 2College of Pharmacy, Sungkyunkwan University, Suwon, Korea
  • 3Korea Food Research Institute, Gyeonggi-do, Korea
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Publikationsverlauf

received October 8, 2008 revised November 27, 2008

accepted December 3, 2008

Publikationsdatum:
30. Januar 2009 (online)

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Abstract

A new resveratrol dimer, (+)-vitisinol E (1) which demonstrated inhibitory activity on BACE-1 (beta-site APP-cleaving enzyme 1) in vitro, was isolated from the stembark extract of Vitis vinifera (Vitaceae) together with four known resveratrol oligomers, (+)-ε-viniferin (2), (+)-ampelopsin A (3), (+)-vitisin A (4) and (−)-vitisin B (5). The chemical structure of 1 was established by MR spectroscopic analyses, including HMBC. All isolated resveratrol derivatives (1–5) demonstrated significant inhibition on baculovirus-expressed BACE-1 in a dose-dependent manner, which was assessed with the FRET assay using Rh-EVNLDAEFK as a substrate in vitro.

References

Dr. Shi Yong Ryu

Korea Reseach Institute of Chemical Technology
Yusung

P. O. Box 107

Daejeon

Korea 305-343

Telefon: + 82 4 28 60 71 63

Fax: + 82 4 28 61 03 07

eMail: syryu@krict.re.kr