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标题：Biological Activity of Tropolone
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作者：Yasuhiro Morita ; Eiko Matsumura ; Toshihiro Okabe 等
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