目的 蒽醌多酣為中醫常用中藥大黃之活性成分,主以配糖體形式存在於大黃中。大多數多酚配糖體• 通常於體內經由腸內菌進行酵素水解形成其苷元後方能吸收。本研究利用大鼠便探討大黃水煎劑中四種蒽醌多酚包括蘆蒼大黃素、大黃酸、大黃素、大黃酚及彼等之配糖體之循環前代謝。 方法 利用所開發之HPLC方怯,定量大黃水煎劑及大鼠便懸浮液中之藍蒼大黃素、大黃酸、大黃素、大黃酚。將大鼠便懸浮液與大黃水煎劑或蒽醌苷元於無氧下進行培養,以探討此等蒽醌多酚遭受腸內菌作用之循環前代謝。 結果 大黃水煎劑與大鼠便懸浮液經由混合後,四種蒽醌苷元之含量立即顯著增加,顯示彼等之配糖體受到腸內菌迅速水解,隨後之培養使所有蒽醌苷元顯著降低,顯示苷元受到腸內菌之進一步降解。 結論 大黃之蒽醌多酚於腸道吸收前遭受之代謝,包括配糖體先受到腸內菌之水解形成苷元,普並遭其進一步降解。(中台灣醫誌2004 ; 9 : 87 一95 )
Objectives. Anthraquinone polyphenols are bioactive constituents which mainly present as glycosides in rhubarb, an herb widely used in clinical Chinese medicine. Most polyphenol glycosides are absorbed only after being hydrolyzed to their aglycones by enteral microflora. In the present study, we investigated the presystemic metabolism of four anthraquinone polyphenols including aloe-emodin, rhein, emodin, and chrysophanol as well as their glycosides in rhubarb decoction and in rat feces. Methods. Aloe-emodin, rhein, emodin and chrysophanol in rhubarb decoction and feces suspension were determined by HPLC methods developed in this study. The presystemic metabolism of these anthraquinones by enteral microflora was investigated by separately incubating rhubarb decoction and anthraquinone aglycones with rat feces suspension under anaerobic conditions. Results. The contents of four anthraquinone aglycones in rhubarb decoction significantly increased instantaneously upon mixing with feces suspension. Moreover, there was a rapid decrease in all anthraquinone aglycones during incubation. Conclusions. The anthraquinone polyphenols in rhubarb were presystemically metabolized before absorption, including hydrolysis of glycosides and degradation of aglycones by enterobacteria. ( Mid Taiwan J Med 2004;9:87-95 )