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标题：Cytotoxicity of the Hinokitiol-Related Compounds, γ-Thujaplicin and β-Dolabrin
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作者：Eiko MATSUMURA ; Yasuhiro MORITA ; Tomomi DATE 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：2001
卷号：24
期号：3
页码：299-302
DOI：10.1248/bpb.24.299
出版社：The Pharmaceutical Society of Japan
摘要：γ-Thujaplicin and β-dolabrin, the constituents of the wood of Thujopsis dolabrata SIEB. Et ZUCC. Var. hondai showed strong in vitro cytotoxic effects against the human stomach cancer cell lines KATO-III and Ehrlich’s ascites carcinoma. The cytotoxic effects of the two compounds against both tumor cell lines were clear when cell growth was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. γ-Thujaplicin and β-dolabrin at 0.32 μg/ml inhibited cell growth of human stomach cancer KATO-III by 85 and 67%, and Ehrlich’s ascites carcinoma by 91 and 75%, respectively. There is no large difference in cytotoxicity between these compounds, but the activity of γ-thujaplicin was slightly more potent than that of β-dolabrin. On the other hand, hinokitiol acetate did not show a cytotoxic effect, suggesting that at least a part of the mechanism of the cytotoxic effect of hinokitiol-related compounds is due to metal chelation between the carbonyl group at C-1 and the hydroxyl group at C-2 in the tropolone skeleton of these molecules. The acute toxicities [50% lethal dose (LD₅₀) value: intraperitoneal injection, Van der Waedem] of γ-thujaplicin and β-dolabrin in mice were 277 mg/kg and 232 mg/kg, respectively.
关键词：hinokitiol;γ-thujaplicin;β-dolabrin;cytotoxic effect;human stomach cancer KATO-III;Ehrlich’s ascites carcinoma