Antithrombin Effect of Jidabokuippo and Identification of Active Compounds

Abstract

Static blood (Oketsu) is a blood disorder of Kampo medicine. Many natural medicines have been used to cure static blood, and these drugs are called blood stasis-resolving formula. Some of these were reported to inhibit blood coagulation. Jidabokuippo (JDI), one of the blood stasis-resolving formulas, has been used to treat bruises and sprains. In this study, we evaluated the antithrombin activity of JDI and its active compounds using thrombin and an artificial substrate. Bioassay-guided isolation was performed for JDI, and the active compounds were identified using spectral data (NMR spectroscopy and mass spectrometry) by comparison with reported data. JDI depressed thrombin activity in a dose-dependent manner, ranging from 0.125 to 1 mg/mL. Chrysophanol-1- O-β-D-glucoside (1) and chrysophanol-8- O-β-D-glucoside (2) were obtained from JDI and showed thrombin inhibitory activity. This study provided the first report of the antithrombin effect of JDI and the isolation from it of two active compounds (1 and 2). These findings might contribute to the understanding of the mechanism of static blood and blood stasis-resolving formula.