Dept. of Pharmacy, Tongji Hospital Affiliated with Tongji Medical College, Huazhong Univ. of Science and Technology, Wuhan, 430030, China.
J Food Sci. 2018 Jul;83(7):1941-1947. doi: 10.1111/1750-3841.14112. Epub 2018 Jul 3.
A variety of beneficial pharmacological activities have been reported for dihydromyricetin (DMY), however, its oral bioavailability is poor and the intestinal absorption profiles of DMY remains unknown. The aim of this study was to investigate the uptake and transport mechanism of DMY in human intestinal Caco-2 cells. DMY was detected using a liquid chromatography-tandem mass spectrometry method. Several factors including time, concentration, pH, temperature and efflux transporters were systematically evaluated. DMY was poorly absorbed by a passive diffusion mechanism. The uptake and transport of DMY were time and concentration dependent. Interestingly, decreasing the pH from 8.0 to 6.0 markedly enhanced the DMY uptake, but didn't significantly affect its bidirectional transport. Efflux transporters, multidrug resistance protein 2 and breast cancer resistance protein also influenced the DMY uptake and transport processes. This work details the uptake and transport characteristics of DMY and provides basis for future study.
This study elucidated the uptake and transport characteristics of dihydromyricetin (DMY). DMY was poorly absorbed by a passive diffusion mechanism. The uptake and transport of DMY were time and concentration dependent. Interestingly, pH affected DMY uptake but not its bidirectional transport. MRP2 and BCRP were involved in the uptake and transport of DMY, which hindered the absorption of DMY in the intestinal. Thus, the present study may provide useful information for designing DMY delivery systems and avoiding DMY-drug interactions.
二氢杨梅素（DMY）具有多种有益的药理活性，但口服生物利用度差，其肠内吸收情况尚不清楚。本研究旨在探讨 DMY 在人肠 Caco-2 细胞中的摄取和转运机制。采用液相色谱-串联质谱法检测 DMY。系统评价了时间、浓度、pH 值、温度和外排转运体等多种因素。DMY 主要通过被动扩散机制被吸收。DMY 的摄取和转运均依赖于时间和浓度。有趣的是，将 pH 值从 8.0 降低至 6.0 显著增强了 DMY 的摄取，但对其双向转运没有显著影响。多药耐药蛋白 2（MRP2）和乳腺癌耐药蛋白（BCRP）也影响 DMY 的摄取和转运过程。本研究详细阐述了 DMY 的摄取和转运特征，为今后的研究提供了依据。
本研究阐明了二氢杨梅素（DMY）的摄取和转运特征。DMY 主要通过被动扩散机制被吸收。DMY 的摄取和转运均依赖于时间和浓度。有趣的是，pH 值影响 DMY 的摄取，但不影响其双向转运。MRP2 和 BCRP 参与了 DMY 的摄取和转运，这阻碍了 DMY 在肠道中的吸收。因此，本研究可为设计 DMY 传递系统和避免 DMY-药物相互作用提供有用信息。
