Biological activity of alpha-thujaplicin, the minor component of Thujopsisdolabrata Sieb. et Zucc. var. hondai Makino

Citation
Y. Morita et al., Biological activity of alpha-thujaplicin, the minor component of Thujopsisdolabrata Sieb. et Zucc. var. hondai Makino, BIOL PHAR B, 24(6), 2001, pp. 607-611
Citations number
25
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Pharmacology & Toxicology
Journal title
BIOLOGICAL & PHARMACEUTICAL BULLETIN
ISSN journal
0918-6158 → ACNP
Volume
24
Issue
6
Year of publication
2001
Pages
607 - 611
Database
ISI
SICI code
0918-6158(200106)24:6<607:BAOATM>2.0.ZU;2-P
Abstract
alpha -Thujaplicin, a minor component of Thujopsis dolabrata SIEB. et Zucc. var. hondai MAKINO, which was synthesized, showed the antibacterial activi ty, phytogrowth-inhibitory effect, inhibition of carboxypeptidase A and cyt otoxic effect. Antibacterial activity of alpha -thujaplicin on Enterococcus faecalis IFO-12965 [minimum inhibitory concentration (MIC): 1.56 mug/ml] w as higher than that of gentamicin (MIC: 6.25 mug/ml) used as a positive con trol. 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 ge rmination inhibition toward the seed of Echinochloa utilis Ohwi et Yabuno e ven 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 mug/ml inhibited cell growth of human stomach cancer KATO-III by 86%, and Ehrlich's ascites carcinoma by 87%, respectivel y: This compound even at the low concentration of 0.32 mug/ml also inhibite d cell growth of the former by 66%, and the latter by 75%, respectively. Th e acute toxicity of alpha -thujaplicin [50% lethal dose (LD50) value: 256 m g/kg] in mice was as strong as those of beta -dolabrin (LD50 value: 232 mg/ kg) and gamma -thujaplicin (LD50 value: 277 mg/kg).