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  • 标题:Effects of Hydroxy Groups in the A-Ring on the Anti-proteasome Activity of Flavone
  • 本地全文:下载
  • 作者:Kasumi Nakamura ; Jia-Hua Yang ; Eiji Sato
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2015
  • 卷号:38
  • 期号:6
  • 页码:935-940
  • DOI:10.1248/bpb.b15-00018
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    The ubiquitin–proteasome pathway plays an important role in regulating apoptosis and the cell cycle. Recently, proteasome inhibitors have been shown to have antitumor effects and have been used in anticancer therapy for several cancers such as multiple myeloma. Although some flavones, such as apigenin, chrysin and luteolin, have a specific role in the inhibition of proteasome activity and induced apoptosis in some reports, these findings did not address all flavone types. To further investigate the proteasome-inhibitory mechanism of flavonoids, we examined the inhibitory activity of 5,6,7-trihydroxyflavone, baicalein and 5,6,7,4′-tetrahydroxyflavone, scutellarein on extracted proteasomes from mice and cancer cells. Unlike the other flavones, baicalein and scutellarein did not inhibit proteasome activity or accumulate levels of ubiquitinated proteins. These results indicate that flavones with hydroxy groups at positions 5, 6 and 7 of the A-ring lack the anti-proteasome function.

  • 关键词:ubiquitin; flavonoid; proteasome; inhibitor
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