Laboratory of Metabolic Biophysics and Applied Pharmacology (LR12ES02), Department of Biophysics, Faculty of Medicine Ibn El Jazzar of Sousse, University of Sousse, Sousse, Tunisia.
Department of Metabolism and Nutrition, Institute of Food Science, Technology and Nutrition (ICTAN), Spanish National Research Council (CSIC), Madrid, Spain.
J Sci Food Agric. 2018 Aug;98(10):3741-3751. doi: 10.1002/jsfa.8886. Epub 2018 Mar 12.
Rosmarinus officinalis is an aromatic plant used in folk medicine as a result of the therapeutic properties associated with its phenolic composition, being rich in rosmarinic acid (RA) and caffeic acid (CA). To better understand the bioactivity of these compounds, their absorption and metabolism were assessed in human Caco-2 and HepG2 cells, as small intestine and liver models, respectively, using RA and CA standards, as well as a rosemary infusion and ferulic acid (FA).
Test compounds were partially up-taken and metabolized by Caco-2 and HepG2 cells, although a higher metabolization rate was observed after hepatic incubation compared to intestinal incubation. CA was the compound best absorbed followed by RA and FA, showing metabolites percentages of 30.4%, 11.8% and 4.4% in Caco-2 and 34.3%, 10.3% and 3.2% in HepG2 cells, respectively. RA in the rosemary infusion showed improved bioavailability compared to pure RA. Methyl derivatives were the main metabolites detected for CA and RA after intestinal and hepatic metabolism, followed by methyl-glucuronidates and glucuronidates. RA was also minimally hydrolyzed into CA, whereas FA only was glucuronidated. Rosemary polyphenols followed the same biotransformation pathways as the standards. In addition, phase II derivatives of luteolin were observed.
Rosemary polyphenols are partially metabolized in both the intestine and liver. © 2018 Society of Chemical Industry.
迷迭香是一种芳香植物，由于其酚类成分所具有的治疗特性，在民间医学中被用作药物，其富含迷迭香酸（RA）和咖啡酸（CA）。为了更好地了解这些化合物的生物活性，在人 Caco-2 和 HepG2 细胞中（分别作为小肠和肝脏模型）用 RA 和 CA 标准品以及迷迭香浸液和阿魏酸（FA）评估了它们的吸收和代谢情况。
测试化合物部分被 Caco-2 和 HepG2 细胞摄取和代谢，但与肠孵育相比，肝孵育后观察到更高的代谢率。CA 是吸收最好的化合物，其次是 RA 和 FA，在 Caco-2 细胞中分别显示出 30.4%、11.8%和 4.4%的代谢产物百分比，在 HepG2 细胞中分别显示出 34.3%、10.3%和 3.2%的代谢产物百分比。迷迭香浸液中的 RA 与纯 RA 相比具有更好的生物利用度。在肠和肝代谢后，CA 和 RA 的主要代谢物是甲基衍生物，其次是甲基-葡糖苷酸和葡糖苷酸。RA 也被轻微水解成 CA，而 FA 仅被葡糖醛酸化。迷迭香多酚遵循与标准品相同的生物转化途径。此外，还观察到木犀草素的 II 期衍生物。
迷迭香多酚在肠和肝中部分被代谢。 © 2018 化学工业协会。
