Dept. of Pharmacy, Tongji Hospital Affiliated with Tongji Medical College, Huazhong Univ. of Science and Technology, Wuhan, 430030, China.
J Food Sci. 2018 May;83(5):1444-1453. doi: 10.1111/1750-3841.14128. Epub 2018 Apr 16.
Dihydromyricetin (DMY) is the main bioactive constituent in vine tea (Ampelopsis grossedentata), which was predominantly distributed in the gastrointestinal tract and showed poor oral bioavailability. Our aim was to systematically investigate the interactions of DMY with gut microbiota. Through the metabolism study of DMY by fecal microflora in vitro, it was found that DMY could be metabolized into three metabolites by fecal microflora via reduction and dehydroxylation pathways, and the dehydroxylation metabolite was the dominant one. Meanwhile, in order to consider the influence of gut microbiota metabolism on the pharmacokinetics of DMY, the pharmacokinetics of DMY in control and pseudo-germ-free rats were compared. It was shown that area under the curve (AUC) could only slightly increase, however, peak concentration (C ) could significantly increase in the pseudo-germ-free rats compared with the control rats, which indicated the gut microbiota metabolism played an important role in the pharmacokinetics of DMY. In addition, the long-term influence of DMY on gut microbiota composition by using 16S rRNA pyrosequencing was further investigated. And it was found that DMY could markedly alter the richness and diversity of the gut microbiota and modulate the gut microbiota composition. The present findings will be helpful for the future development and clinical application of DMY.
The gut microbiota plays an important role in the pharmacokinetics of flavonoids. As well, the long-term supplements of flavonoids could alter the gut microbiota composition in turn. The study aims to clarify the mutual interaction of DMY with gut microbiota, which may lead to new information with respect to the mechanism study and clinical application of DMY.
二氢杨梅素(DMY)是藤茶(显齿蛇葡萄)中的主要生物活性成分,主要分布在胃肠道中,口服生物利用度较差。我们的目的是系统研究 DMY 与肠道微生物群的相互作用。通过体外粪便微生物对 DMY 的代谢研究,发现 DMY 可通过粪便微生物的还原和去羟化途径代谢为三种代谢物,其中去羟化代谢物为主要产物。同时,为了考虑肠道微生物代谢对 DMY 药代动力学的影响,比较了 DMY 在对照和假无菌大鼠中的药代动力学。结果表明,与对照组相比,AUC 仅略有增加,而 C 显著增加,这表明肠道微生物代谢对 DMY 的药代动力学起重要作用。此外,还进一步采用 16S rRNA 焦磷酸测序研究了 DMY 对肠道微生物组成的长期影响。结果发现,DMY 可明显改变肠道微生物的丰富度和多样性,并调节肠道微生物组成。本研究结果有助于 DMY 的未来开发和临床应用。
肠道微生物在类黄酮的药代动力学中起重要作用。此外,类黄酮的长期补充会反过来改变肠道微生物组成。本研究旨在阐明 DMY 与肠道微生物群的相互作用,这可能为 DMY 的机制研究和临床应用提供新的信息。