Vesely Ondrej, Marsik Petr, Jarosova Veronika, Doskocil Ivo, Smejkal Karel, Kloucek Pavel, Havlik Jaroslav
Department of Food Science, Faculty of Agrobiology, Food and Natural Resources, Czech University of Life Sciences Prague, 16500 Prague, Czech Republic.
Department of Microbiology, Nutrition and Dietetics, Faculty of Agrobiology, Food and Natural Resources, Czech University of Life Sciences Prague, 16500 Prague, Czech Republic.
Foods. 2021 Nov 10;10(11):2754. doi: 10.3390/foods10112754.
2-arylbenzofurans represent a small group of bioactive compounds found in the plant family Moraceae. As it has not been investigated whether these substances are stable during passage through the gastrointestinal tract, their biological effects may be altered by the metabolism of intestinal microbiota or cells. The aim of the present study was to investigate and compare mulberrofuran Y (), moracin C (), and mulberrofuran G () in an in vitro model of human intestinal bacterial fermentation and in an epithelial model using the Caco-2 cell line. The analysis of compounds by LC-MS-Q-TOF showed sufficient stability in the fermentation model, with no bacterial metabolites detected. However, great differences in the quantity of permeation were observed in the permeability assay. Moreover, mulberrofuran Y () and moracin C () were observed to be transformed into polar metabolites by conjugation. Among the test compounds, mulberrofuran Y () was mostly stable and accumulated in endothelial cells (85.3%) compared with mulberrofuran G () and moracin C () (14% and 8.2%, respectively). Thus, only a small amount of mulberrofuran Y () was conjugated. Moracin C () and mulberrofuran G () were metabolized almost completely, with only traces of the unchanged molecule being found on the apical and cellular sides of the system. Only conjugates of mulberrofuran Y () and moracin C () were able to reach the basolateral side. Our results provide the basic description of bioavailability of these three compounds, which is a necessary characteristic for final evaluation of bio-efficacy.
2-芳基苯并呋喃是桑科植物中发现的一小类生物活性化合物。由于尚未研究这些物质在通过胃肠道时是否稳定，它们的生物学效应可能会因肠道微生物群或细胞的代谢而改变。本研究的目的是在人肠道细菌发酵的体外模型和使用Caco-2细胞系的上皮模型中研究和比较桑呋喃Y（）、桑色素C（）和桑呋喃G（）。通过LC-MS-Q-TOF对化合物进行分析，结果表明其在发酵模型中具有足够的稳定性，未检测到细菌代谢产物。然而，在渗透性试验中观察到渗透量存在很大差异。此外，观察到桑呋喃Y（）和桑色素C（）通过结合转化为极性代谢产物。在测试化合物中，与桑呋喃G（）和桑色素C（）（分别为14%和8.2%）相比，桑呋喃Y（）大多稳定并在内皮细胞中积累（85.3%）。因此，只有少量的桑呋喃Y（）发生结合。桑色素C（）和桑呋喃G（）几乎完全代谢，在系统的顶端和细胞侧仅发现微量未变化的分子。只有桑呋喃Y（）和桑色素C（）的结合物能够到达基底外侧。我们的结果提供了这三种化合物生物利用度的基本描述，这是最终评估生物功效的必要特征。
