Morita Y, Matsumura E, Tsujibo H, Yasuda M, Sakagami Y, Okabe T, Ishida N, Inamori Y
Osaka Organic Chemical Industry, Ltd., Kashiwara, Japan.
Biol Pharm Bull. 2001 Jun;24(6):607-11. doi: 10.1248/bpb.24.607.
Alpha-thujaplicin, a minor component of Thujopsis dolabrata SIEB. et ZUCC. var. hondai MAKINO, which was synthesized, showed the antibacterial activity, phytogrowth-inhibitory effect, inhibition of carboxypeptidase A and cytotoxic effect. Antibacterial activity of alpha-thujaplicin on Enterococcus faecalis IFO-12965 [minimum inhibitory concentration (MIC): 1.56 microg/ml] was higher than that of gentamicin (MIC: 6.25 microg/ml) used as a positive control. Inhibitory activity of alpha-thujaplicin on carboxypeptidase A [50% inhibitory concentration (IC50): 3.24 x 10(-5) M] was higher than that of 1,10-phenanthroline used as a positive control. Alpha-thujaplicin showed germination inhibition toward the seed of Echinochloa utilis Ohwi et Yabuno even at the low concentration of 10 ppm and its growth inhibitory effect was stronger than that of sodium 2,4-dichlorophenoxyacetate used as a standard. Alpha-thujaplicin at 1.25 microg/ml inhibited cell growth of human stomach cancer KATO-IIl by 86%, and Ehrlich's ascites carcinoma by 87%, respectively. This compound even at the low concentration of 0.32 microg/ml also inhibited cell growth of the former by 66%, and the latter by 75%, respectively. The acute toxicity of alpha-thujaplicin [50% lethal dose (LD50) value: 256 mg/kg] in mice was as strong as those of beta-dolabrin (LD50 value: 232 mg/kg) and gamma-thujaplicin (LD50 value: 277 mg/kg).
α-崖柏素是日本扁柏（Thujopsis dolabrata SIEB. et ZUCC. var. hondai MAKINO）的一种次要成分，其合成产物具有抗菌活性、植物生长抑制作用、对羧肽酶A的抑制作用以及细胞毒性作用。α-崖柏素对粪肠球菌IFO-12965的抗菌活性[最低抑菌浓度（MIC）：1.56微克/毫升]高于用作阳性对照的庆大霉素（MIC：6.25微克/毫升）。α-崖柏素对羧肽酶A的抑制活性[50%抑制浓度（IC50）：3.24×10⁻⁵ M]高于用作阳性对照的1,10-菲啰啉。α-崖柏素即使在10 ppm的低浓度下也对稗草（Echinochloa utilis Ohwi et Yabuno）种子表现出萌发抑制作用，其生长抑制作用强于用作标准的2,4-二氯苯氧乙酸钠。1.25微克/毫升的α-崖柏素分别抑制人胃癌KATO-IIl细胞生长86%，抑制艾氏腹水癌细胞生长87%。该化合物即使在0.32微克/毫升的低浓度下也分别抑制前者细胞生长66%，抑制后者细胞生长75%。α-崖柏素在小鼠中的急性毒性[50%致死剂量（LD50）值：256毫克/千克]与β-崖柏素（LD50值：232毫克/千克）和γ-崖柏素（LD50值：277毫克/千克）相当。
