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Structure-activity relationship of flavonoids for inhibition of epidermal growth factor-induced transformation of JB6 Cl 41 cells

✍ Scribed by Daisuke Ichimatsu; Masaaki Nomura; Seiji Nakamura; Shuzo Moritani; Koichi Yokogawa; Shinjiro Kobayashi; Tatsuo Nishioka; Ken-ichi Miyamoto

Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
391 KB
Volume
46
Category
Article
ISSN
0899-1987

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✦ Synopsis

Abstract

We found that quercetin, myricetin, quercetagetin, fisetin, (−)‐epigallocatechin gallate (EGCG), and theaflavins, among 24 flavonoids examined, markedly inhibited epidermal growth factor (EGF)‐induced cell transformation of mouse epidermal JB6 Cl 41 cells. The six flavonoids suppressed the EGF‐induced activation of activator protein 1 (AP‐1). In addition, myricetin, quercetagetin, EGCG, and theaflavins directly inhibited EGF‐induced phosphatidylinositol 3‐kinase (PI3K) activation. The important structural features of flavonoids for cell transformation‐inhibitory activity are 3′‐ and 4′‐OH on the B‐ring, 3‐OH on the C‐ring, C2C3 double bond in the C‐ring, and the phenylchromone (C6C5C6) skeleton in the flavonols, and the galloyl group in EGCG and theaflavins. Our results provide new insight into possible mechanisms of the anti‐carcinogenic effects of flavonoids, and could help to provide a basis for the design of novel cancer chemopreventive agents. © 2007 Wiley‐Liss, Inc.

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