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  • 标题:Homoisoflavonoids from Caesalpinia sappan Displaying Viral Neuraminidases Inhibition
  • 本地全文:下载
  • 作者:Hyung Jae Jeong ; Young Min Kim ; Jang Hoon Kim
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2012
  • 卷号:35
  • 期号:5
  • 页码:786-790
  • DOI:10.1248/bpb.35.786
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:In this study, twelve neuraminidase (NA) inhibitory compounds 1 – 12 were isolated from heartwood of Caesalpinia sappan on the basis of their biological activities against three types of viral NAs. Of isolated homoisoflavonoids, sappanone A ( 2 ) showed the most potent NAs inhibitory activities with IC50 values of 0.7 µ M [H1N1], 1.1 µ M [H3N2], and 1.0 µ M [H9N2], respectively, whereas saturated homoisoflavonoid ( 3 ) did not show significantly inhibition. This result revealed that α,β-unsaturated carbonyl group in A-ring was the key requirements for viral NAs inhibitory activity. In our enzyme kinetic study, all NA inhibitors screened were found to be reversible noncompetitive types.
  • 关键词:Caesalpinia sappan;homoisoflavonoid;α,β-unsaturated carbonyl;neuraminidase
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