Morita Yasuhiro, Matsumura Eiko, Okabe Toshihiro, Fukui Toru, Ohe Tatsuhiko, Ishida Nakao, Inamori Yoshihiko
Osaka Organic Chemical Industry, Ltd, Katayama-cho, Kashiwara, Japan.
Biol Pharm Bull. 2004 Oct;27(10):1666-9. doi: 10.1248/bpb.27.1666.
Beta-dolabrin, gamma-thujaplicin, and 4-acetyltropolone, the components of Aomori Hiba (Thujopsis dolabrata SIEB. et ZUCC. var. hondai MAKINO), showed antifungal activity on seven kinds of plant-pathogenic fungi, antibacterial activity against two kinds of Legionella sp., and in vitro cytotoxic effect on murine P388 lymphocytic leukemia cell line. Firstly, beta-dolabrin, gamma-thujaplicin and 4-acetyltropolone had clear antifungal activity against seven kinds of plant-pathogenic fungi tested. In particular, beta-dolabrin and 4-acetyltropolone showed strong antifungal activity against Pythium aphanidermatum IFO 32440, with minimum inhibitory concentration (MIC) values of 6.0 microg/ml. Secondly, beta-dolabrin, gamma-thujaplicin and 4-acetyltropolone had obvious growth-inhibitory effect on two kinds of Legionella sp. 4-Acetyltropolone especially had strong antibacterial activity toward Legionella pneumophila SG 1, and its MIC value was 3.1 microg/ml. These three compounds showed cytotoxic effects against murine P388 lymphocytic leukemia cell line in vitro. The cytotoxic effect of three compounds in the murine P388 lymphocytic leukemia cell line were clear when cell growth was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. At 48 h after treatment, gamma-thujaplicin and 4-acetyltropolone at 0.63 microg/ml inhibited cell growth of murine P388 lymphocytic leukemia by 85% and 65%, respectively. At the same time after treatment, the growth of the murine P388 lymphocytic leukemia cell line was completely suppressed by the three compounds at concentrations higher than 5.0 microg/ml. Among these three compounds, gamma-thujaplicin had the strongest cytotoxic activity on the growth of this tumor cell line in vitro.
青森桧（扁叶扁柏变种钝叶扁柏）的成分β-桧脑、γ-崖柏素和4-乙酰基托酚酮对7种植物病原真菌具有抗真菌活性，对两种嗜肺军团菌具有抗菌活性，并且对小鼠P388淋巴细胞白血病细胞系具有体外细胞毒性作用。首先，β-桧脑、γ-崖柏素和4-乙酰基托酚酮对所测试的7种植物病原真菌具有明显的抗真菌活性。特别是，β-桧脑和4-乙酰基托酚酮对瓜果腐霉IFO 32440表现出较强的抗真菌活性，最低抑菌浓度（MIC）值为6.0微克/毫升。其次，β-桧脑、γ-崖柏素和4-乙酰基托酚酮对两种嗜肺军团菌有明显的生长抑制作用。4-乙酰基托酚酮尤其对嗜肺军团菌SG 1具有较强的抗菌活性，其MIC值为3.1微克/毫升。这三种化合物在体外对小鼠P388淋巴细胞白血病细胞系表现出细胞毒性作用。当使用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）法测量细胞生长时，这三种化合物在小鼠P388淋巴细胞白血病细胞系中的细胞毒性作用明显。处理48小时后，0.63微克/毫升的γ-崖柏素和4-乙酰基托酚酮分别抑制小鼠P388淋巴细胞白血病细胞生长85%和65%。同时在处理后，浓度高于5.0微克/毫升的这三种化合物完全抑制了小鼠P388淋巴细胞白血病细胞系的生长。在这三种化合物中，γ-崖柏素在体外对该肿瘤细胞系的生长具有最强的细胞毒性活性。
