Biological Activity of Tropolone

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 SIEB. et ZUCC. hondai MAKINO). The insecticid...

Full description

Saved in:
Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2003, Vol.26(10), pp.1487-1490
Main Authors: Morita, Yasuhiro, Matsumura, Eiko, Okabe, Toshihiro, Shibata, Mitsunobu, Sugiura, Masaaki, Ohe, Tatsuhiko, Tsujibo, Hiroshi, Ishida, Nakao, Inamori, Yoshihiko
Format: Article
Language:eng ; jpn
Subjects:
Analysis
Analytical, structural and metabolic biochemistry
Animals
antifungal activity
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Biological and medical sciences
Fundamental and applied biological sciences. Psychology
General pharmacology
hinokitiol
Insecta - drug effects
Insecta - physiology
insecticidal activity
Insecticides - chemistry
Insecticides - pharmacology
Medical sciences
metalloprotease inhibition
Pharmacology. Drug treatments
plant-pathogenic fungus
Pythium - drug effects
Pythium - physiology
tropolone
Tropolone - chemistry
Tropolone - pharmacology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 SIEB. et ZUCC. hondai MAKINO). 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).
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.26.1487