Fujita T, Sakuma S, Sumiya T, Nishida H, Fujimoto Y, Baba K, Kozawa M
Department of Hygienic Chemistry, Osaka University of Pharmaceutical Sciences, Japan.
Res Commun Chem Pathol Pharmacol. 1992 Aug;77(2):227-40.
The effects of a new chalcone derivative, xanthoangelol E, isolated from Angelica keiskei Koidzumi, on arachidonic acid metabolism in the gastric antral mucosa and platelet of the rabbit were examined. When gastric antral mucosal slices were incubated with xanthoangelol E (0.05-1.0 mM), there was no significant effect on the production of prostaglandin (PG) E2, PGF2 alpha and their metabolites. On the other hand, this compound inhibited effectively the production of thromboxane B2 and 12-hydroxy-5,8,10-heptadecatrienoic acid from exogenous arachidonic acid in platelets, and the concentration required for 50% inhibition (IC50) was approximately 5 microM. The formation of 12-hydroxy-5,8,10,14-eicosatetraenoic acid was also reduced by this drug (IC50, 50 microM). These results suggest that xanthoangelol E has the potential to modulate arachidonic acid metabolism in platelets and that this action may participate in some pharmacological effect of the plant.
研究了从明日叶中分离出的一种新的查尔酮衍生物黄当归醇E对兔胃窦黏膜和血小板中花生四烯酸代谢的影响。当胃窦黏膜切片与黄当归醇E(0.05 - 1.0 mM)一起孵育时,对前列腺素(PG)E2、PGF2α及其代谢产物的产生没有显著影响。另一方面,该化合物有效抑制了血小板中血栓素B2和12 - 羟基 - 5,8,10 - 十七碳三烯酸从外源性花生四烯酸的产生,50%抑制所需浓度(IC50)约为5 microM。该药物也降低了12 - 羟基 - 5,8,10,14 - 二十碳四烯酸的形成(IC50,50 microM)。这些结果表明,黄当归醇E有调节血小板中花生四烯酸代谢的潜力,并且这种作用可能参与了该植物的某些药理作用。