Zhou Siyuan, Yang Runtao, Teng Zenghui, Zhang Bangle, Hu Yuzhen, Yang Zhifu, Huan Menglei, Zhang Xiang, Mei Qibing
Department of Pharmaceutics, Xijing Hospital, Fourth Military Medical University, Xi'an, China.
J Agric Food Chem. 2009 Jun 10;57(11):4572-9. doi: 10.1021/jf803948g.
There is considerable evidence that stilbenes provide health benefits. trans-Polydatin is one of the major stilbenoid compounds in red wine. The purpose of this study is to investigate the dose-dependent absorption and metabolism of trans-polydatin in rats. trans-Polydatin was administered to rats by gavage at three different doses (50, 100, and 300 mg x kg(-1)). Blood samples were then collected at different time points. In situ perfusion of rat small intestine and liver was used to investigate the first-pass metabolism of trans-polydatin. trans-Polydatin and its metabolites were detected by LC-MS/MS. trans-Polydatin and its metabolites resveratrol, glucuronidated resveratrol, and glucuronidated trans-polydatin were detected in plasma within 10 min following oral administration of trans-polydatin; in situ perfusion of the rat small intestine and liver with trans-polydatin yielded the same result. The AUC(0-infinity) of trans-polydatin and its metabolites increased in a dose dependent manner following oral administration of trans-polydatin. This indicates that in the rats, trans-polydatin is absorbed in a dose-dependent manner and undergoes extensive first-pass deglycosylation and glucuronidation. Orally administered trans-polydatin, therefore, is metabolized primarily to resveratrol in the small intestine and liver, where it is further metabolized to the glucuronidated resveratrol.
有大量证据表明芪类化合物对健康有益。反式白藜芦醇苷是红酒中的主要芪类化合物之一。本研究的目的是调查反式白藜芦醇苷在大鼠体内的剂量依赖性吸收和代谢情况。以三种不同剂量（50、100和300 mg·kg⁻¹）通过灌胃法给大鼠施用反式白藜芦醇苷。然后在不同时间点采集血样。采用大鼠小肠和肝脏原位灌注法研究反式白藜芦醇苷的首过代谢。通过液相色谱-串联质谱法检测反式白藜芦醇苷及其代谢产物。口服反式白藜芦醇苷后10分钟内，在血浆中检测到反式白藜芦醇苷及其代谢产物白藜芦醇、白藜芦醇葡萄糖醛酸苷和反式白藜芦醇苷葡萄糖醛酸苷；用反式白藜芦醇苷对大鼠小肠和肝脏进行原位灌注也得到了相同结果。口服反式白藜芦醇苷后，反式白藜芦醇苷及其代谢产物的AUC(0-∞)呈剂量依赖性增加。这表明在大鼠体内，反式白藜芦醇苷以剂量依赖性方式吸收，并经历广泛的首过去糖基化和葡萄糖醛酸化。因此，口服的反式白藜芦醇苷主要在小肠和肝脏中代谢为白藜芦醇，在那里它进一步代谢为白藜芦醇葡萄糖醛酸苷。
