Biological activity of alpha-thujaplicin, the isomer of hinokitiol.

alpha-Thujaplicin, a minor component of Aomori Hiba (Thujopsis dolabrata SIEB. et ZUCC. var. hondai MAKINO), showed rather strong antifungal activity against seven kinds of plant-pathogenic fungi, their minimum inhibitory concentrations (MICs) being in the range of 12.0-50.0 microg/ml. alpha-Thujaplicin and hinokitiol (the major component of Aomori Hiba) also showed clear antibacterial activity against Legionella pneumophila SG 1 and L. pneumophila SG 3, and their MICs are in the range of 6.25-50 microg/ml. This compound showed strong insecticidal activity against Reticulitermes speratus [50%-lethal concentration (LC(50)): 0.02 g/m(2)], and it also had clear acaricidal activity against Dermatophagoides farinae (LC(50): 0.66 g/m(2)). At 24 h after treatment, alpha-thujaplicin at 0.63 microg/ml inhibited the cell growth of murine P388 lymphocytic leukemia by 78%, and its cytotoxic activity at a concentration higher than 0.63 microg/ml was as high as that of vincristine, used as a positive control. On the other hand, the cytotoxic effect of alpha-thujaplicin at 0.63 microg/ml was weaker than that of vinblastine. In this respect, the strong cytotoxic effect of alpha-thujaplicin on murine P388 lymphocytic leukemia cell line should be emphasized, considering that it has recently been found to be low in toxicity to mice.