Fan Li, Tong Qing, Dong Weiwei, Yang Guangjie, Hou Xiaolong, Xiong Wei, Shi Chunyang, Fang Jianguo, Wang Wenqing
Department of Pharmacy, Tongji Hospital Affiliated with Tongji Medical College, Huazhong University of Science and Technology , Wuhan 430030, China.
Wuhan Institute for Drug and Medical Device Control , Wuhan 430075, China.
J Agric Food Chem. 2017 Jun 14;65(23):4597-4604. doi: 10.1021/acs.jafc.7b01155. Epub 2017 May 31.
Dihydromyricetin (DMY), a flavanonol compound found as the most abundant and bioactive constituent in vine tea (Ampelopsis grossedentata), possesses numerous biological activities. In the present study, an HPLC-MS/MS method for the determination of DMY in tissues, urine, and feces was developed and applied to the tissue distribution and excretion study after oral administration in rats, and the metabolic profile of DMY was further investigated using UPLC-QTOF-MS. The results indicated that DMY could be distributed rapidly in various tissues and highly in the gastrointestinal tract. The elimination of DMY occurred rapidly as well, and most unconverted forms were excreted in feces. A total of eight metabolites were identified in urine and feces, while metabolites were barely found in plasma. The predicted metabolic pathways including reduction, dehydroxylation, methylation, glucuronidation, and sulfation were proposed. The present findings may provide the theoretical basis for evaluating the biological activities of DMY and will be helpful for its future development and application.
二氢杨梅素（DMY）是藤茶（显齿蛇葡萄）中含量最丰富且具有生物活性的黄酮醇类化合物，具有多种生物活性。在本研究中，建立了一种用于测定组织、尿液和粪便中DMY的HPLC-MS/MS方法，并将其应用于大鼠口服给药后的组织分布和排泄研究，同时使用UPLC-QTOF-MS进一步研究了DMY的代谢谱。结果表明，DMY能够迅速分布于各种组织中，在胃肠道中的分布尤为显著。DMY的消除也很快，大部分未转化的形式通过粪便排出。在尿液和粪便中总共鉴定出了8种代谢产物，而在血浆中几乎未发现代谢产物。提出了包括还原、脱羟基、甲基化、葡萄糖醛酸化和硫酸化在内的预测代谢途径。本研究结果可为评估DMY的生物活性提供理论依据，并有助于其未来的开发和应用。
