IJPPP Copyright © 2009-All rights reserved. Published by e-Century Publishing Corporation, Madison, WI 53711
Int J Physiol Pathophysiol Pharmacol 2009;1(1):76-82.

Original Article
Effects of acetylate hyperforin on the processing of amyloid precursor protein

Xiang Chen, Wenshang Feng, Qing Chen, Xiangling Yang, Depo Yang, Dongmei Wang, Ling Zhong

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China

Received February 9, 2009; accepted February 18, 2009; available online February 20, 2009

Abstract: Hyperforin (HF) is a phloroglucinol compound obtained from St. John’s Wort (Hypericum perforatum). Recent studies have
shown that Hyperforin can be used to improve psychopathologic symptoms of Alzheimer’s disease but the mechanism is not clear.
This may be partly due to the difficult in studying Hyperforin, since this chemical is unstable and is sensitive to light, oxygen, and heat. In
this study, we explored the effects of acetylate hyperforin (ace-HF), a stable derivative of hyperforin, on the processing of amyloid
precursor protein (APP). HEK293 cells transfected with pcDNA3.1APP695sw and SH-SY5Y cells were treated with ace-HF, followed by
measuring the levels of APP and sAPPα. Twelve hours of treatment led to an increase in extracellular sAPPα, but APP mRNA and
protein levels were unchanged. Further studies with α-secretase and a pan PKC inhibitor, Calphostin C, indicated that ace-HF’s effect
on extracellular sAPPα was closely related to PKC activities and α-secretase activities. Our findings suggest that ace-HF can modulate
α-secretase-mediated APP processing via a PKC signaling pathway. (IJPPP902005).

Key words: Soluble amyloid precursor protein α (sAPPα); protein kinase C (PKC); Alzheimer’s disease (AD); hyperforin

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Address all correspondence to:
Ling Zhong, PhD
School of Pharmaceutical Sciences
Sun Yat-sen University
132 Wai Huan East Road
Guangzhou, 510006, China
Tel: +86-20-3994-302