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标题：Antimicrobial Activity and Metalloprotease Inhibition of Hinokitiol-Related Compounds, the Constituents of Thujopsis dolabrata S. and Z. hondai MAK.
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作者：Yoshihiko INAMORI ; Sayo SHINOHARA ; Hiroshi TSUJIBO 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：1999
卷号：22
期号：9
页码：990-993
DOI：10.1248/bpb.22.990
出版社：The Pharmaceutical Society of Japan
摘要：γ-Thujaplicin, β-dolabrin and hinokitiol(β-thujaplicin), hinokitiol-related compounds isolated from the wood of Thujopsis dolabrata S. and Z. hondai MAK have antimicrobial activity. In particular, strong antibacterial activity of hinokitiol and β-dolabrin on Staphylococcus epidermidis IFO-12993 was found, with a minimum inhibitory concentration (MIC) of 0.2 μg/ml. This activity was higher than that of gentamicin, used as a positive control, and so the strong antibacterial activity of both compounds on this bacterium is of considerable interest. Of the three compounds, γ-thujaplicin showed the strongest antifungal activity and its MIC was found to be around 1.5 μg/ml. The three compounds also inhibited metalloproteases. The inhibitory activity of hinokitiol on carboxypeptidase A was especially strong, its 50%-inhibitory concentration (IC₅₀) being 2.76×10^-6 M. Considering that metaloproteases are involved in inflammation, the strong inhibitory activity of hinokitiol could be important. On the other hand, hinokitiol-acetate did not show any antimicrobial activity and metalloprotease inhibition, suggesting that at least part of the activity is due to metal chelation between the carbonyl group at C-1 and the hydroxyl group at C-2 in the tropolone skeleton.
关键词：γ-thujaplicin;β-dolabrin;hinokitiol;hinokitiol-related compound;antimicrobial activity;metalloprotease inhibition