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  • 标题:Biological Activity of Tropolone
  • 本地全文:下载
  • 作者:Yasuhiro Morita ; Eiko Matsumura ; Toshihiro Okabe
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2003
  • 卷号:26
  • 期号:10
  • 页码:1487-1490
  • DOI:10.1248/bpb.26.1487
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Tropolone (1) showed strong insecticidal activity on Tyrophagus putrescentiae and Dermatophagoides farinae . The insecticidal effect of 1 on both insects was stronger than that of hinokitiol (2, 4-isopropyltropolone: major component of Thujopsis dolabrata S IEB . et Z UCC . hondai M AKINO ). The insecticidal activity of both compounds was higher than that of N , N -diethyl- m -toluamide (DEET), used as a positive control. Compound 1 had potent insecticidal activity against Coptotermes formosanus , although its activity was much lower than that of commercial chloropyrifos. Like 2, 1 showed the inhibitory activity toward metalloproteases such as carboxypeptidase A, collagenase and thermolysin and their inhibitory activities were much higher than that of 1,10-phenanthroline, used as a positive control. The inhibitory activity of 1 on carboxypeptidase A was especially high, its 50% inhibitory concentrations (IC50) being 2.73×10−6 M . This inhibitory activity was as high as that of 2 (IC50: 2.76×10−6 M ). Compound 1 inhibited the growth of seven kinds of plant-pathogenic fungi and their minimum inhibitory concentration (MIC) values were in the range of 6.0—50.0 μg/ml. In particular, 1 showed strong antifungal activity on Pythium aphanidermatum IFO-32440 (MIC: 6.0 μg/ml).
  • 关键词:tropolone;hinokitiol;antifungal activity;plant-pathogenic fungus;metalloprotease inhibition;insecticidal activity
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