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

• Ichimatsu, Daisuke

• Nomura, Masaaki

• Nakamura, Seiji

• Moritani, Syuzo

• Yokogawa, Koichi

• Kobayashi, Shinjiro

• Nishioka, Tatsuo

• Miyamoto, Kenichi

抄録

金沢大学医学部附属病院薬剤部

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.

収録刊行物

• Molecular Carcinogenesis

  Molecular Carcinogenesis 46 (6), 436-445, 2007-06-01

  John Wiley & Sons

キーワード

• AP-1
• Cell transformation
• Flavonoids
• PI3K
• Signal transduction

詳細情報

• CRID: 1050282810960520192
• NII論文ID: 120001133169
• ISSN: 08991987
• Web Site: http://hdl.handle.net/2297/6749
• 本文言語コード: en
• 資料種別: journal article
• データソース種別:
  • IRDB
  • CiNii Articles