Rhubarb is one of the most well-known herbal medicines that constitute daiokanzoto (DKT), which is clinically effective for constipation. Sennoside A is transformed into an active metabolite, rheinanthrone, by intestinal bacteria. Sennoside A in rhubarb showed significantly accelerated metabolic activity in intestinal bacteria in comparison with sennoside A alone. In this study, we investigated the influence of rhubarb constituents on the metabolism and purgative activity of sennoside A. The 20% MeOH-eluted fraction separated by MCI-gel CHP-20P column chromatography from the water extract of rhubarb showed sennoside A metabolic activity similar to that of rhubarb extract. The 20% MeOH elute was further purified and rhein 8-O-β-D-glucopyranoside (RG) was isolated. The metabolic activity of sennoside A was significantly accelerated by increasing the level of RG. Moreover, rhein, emodin and aloe-emodin also accelerated sennoside A metabolism. The purgative activity of sennoside A was significantly accelerated when RG or rhein was concomitantly given with sennoside A in a dose-dependent manner. These results suggest that anthraquinones contribute to the purgative action of sennoside A in rhubarb. Therefore, it is assumed that the influence of anthraquinones on the fate of rheinanthrone transformed from sennoside A may promote the purgative action of sennoside A.
2012 The Pharmaceutical Society of Japan