NDLI: Apple procyanidins affect several members of the ErbB receptor tyrosine kinase family <i>in vitro</i>

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Food & Function Vol - 4 Issue - 4

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Apple procyanidins affect several members of the ErbB receptor tyrosine kinase family in vitro

Content Provider	Royal Society of Chemistry (RSC)
Author	Raul, Francis Esselen, Melanie Roth, Matthias Richling, Elke Blust, Volker Schreier, Peter Teller, Nicole Fridrich, Diana Dietrich, Helmut Hümmer, Wolfgang Boettler, Ute Marko, Doris Will, Frank
Copyright Year	2013
Abstract	Complex polyphenol-rich extracts from apples are known to inhibit the activity of the epidermal growth factor receptor (EGFR) in vitro. The aim of the present study was to identify the bioactive constituents of the apple juice extract which contribute substantially to this potentially chemopreventive effect and to address the question whether the effect is specific to the EGFR or whether other members of the ErbB-receptor family might also be affected. Apple-derived dihydrochalcones and their respective glycosides were found to decrease EGFR activity under cell-free conditions with IC50-values ranging from 0.4 ± 0.1 to 267.0 ± 50.0 μM but showed no activity on human cancer cells. The concentration of quercetin or its glycosides in the extract was too low to contribute substantially to the EGFR-inhibitory properties. In contrast, fractions derived from the apple juice extract comprising ≥86% oligomeric procyanidins (OPCs) suppressed the activity of the EGFR in cell culture with an IC50 ∼ 100 μg mL−1. In addition, the activity of further members of the ErbB-receptor family was potently inhibited, with ErbB3 receptor activity being most potently decreased (IC50 ∼ 10 μg mL−1). From the apple polyphenols identified so far OPCs were found to add the highest contribution to the inhibitory effects towards members of the ErbB-receptor family. Considering the crucial role of the ErbB-receptors in carcinogenesis, these results support the hypothesis that apple-derived OPCs as well as OPC-rich apple preparations might be of interest with respect to chemoprevention.
Starting Page	689
Ending Page	697
Page Count	9
File Format	HTM / HTML PDF
ISSN	20426496
Volume Number	4
Issue Number	5
Journal	Food & Function
DOI	10.1039/c3fo30166d
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	EGFR receptor Growth factor Estrogen receptor Epidermal growth factor receptor Apple juice IC50 Cancer Quercetin Cell culture Carcinogenesis Chemoprophylaxis
Content Type	Text
Resource Type	Article
Subject	Medicine Food Science

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Apple procyanidins affect several members of the ErbB receptor tyrosine kinase family in vitro

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Apple procyanidins affect several members of the ErbB receptor tyrosine kinase family in vitro