单 位：
石河子大学医学院第一附属医院;石河子大学药学院
关键词：
香叶木素;微粒体;UGT代谢;单向肠灌流;肠吸收
摘 要：
为研究香叶木素在大鼠不同肠段肠灌流模型中的吸收及UGT代谢特征。采用体外肠微粒体孵育及在体单向肠灌流模型分别研究不同浓度在大鼠不同肠段香叶木素的UGT代谢和吸收情况。结果显示:香叶木素在微粒体中和肠灌流模型中会发生UGT代谢,并产生2个单葡萄糖醛酸苷代谢产物,结肠代谢生成香叶木素葡萄糖醛酸苷的速率较慢。不同浓度的香叶木素在各肠段肠的Papp无显著性差异,表明香叶木素在大鼠小肠内吸收无明显变化,并且无自身浓度抑制作用,主要以被动转运方式吸收。由此可知,香叶木素在大鼠小肠吸收方式以被动转运为主,且在肠道中易吸收的不同四段肠的吸收无显著性差异;但由于香叶木素在细胞内发生葡萄糖醛酸苷代谢,并且由于代谢产物的外排,使得香叶木素的生物利用度下降。
译 名：
The absorption and UGT metabolism of diosmetin in rat intestine
作 者：
ZENG Xuejun;YUAN Yong;GUO Xinhong;MA Tieye;WANG Xinchun;School of Pharmacy, Shihezi University;the First Affiliated Hospital, School of Medicine, Shihezi University;
关键词：
diosmetin;;microsomes;;UGT;;one-way intestinal perfusion model;;intestinal absorption
摘 要：
To investigate the absorption and UGT metabolism of diosmetin in rat intestine. The intestine microsomes and the one-way intestinal perfusion model were used. Diosmetin was much stable in HBSS and KPI solution, the concentration of diosmetin and its glucuronides were determined by UHPLC. Diosmetin can be metabolized into two monoglucuronides, and the rate of the glucuronidation of diosmetin in colon was lower than other intestinal segments, and the rate of formation of diosmetin-3'-O-glucuronide was faster than that of diosmetin-7-O-glucuronide. No significant difference of Papp value was found in different concentrations of diosmetin at different intestine segments, which showed that there was no obvious change in absorption of diosmetin in rat small intestine and no inhibition due to different concentrations and the absorption of diosmetin mainly was complied with the passive diffusion. Because of the UGT metabolism and the excretion of the glucuronides, the bioavailability of the diosmetin decreased.
