Metabolites of Dietary Acteoside: Profiles, Isolation, Identification, and Hepatoprotective Capacities

In recent years, cistanche tea has been increasingly used as a major herbal supplement in functional drinks, and it has attracted a growing number of consumers because of its excellent tonic effects and medicinal properties. Acteoside (ACT), which is the principal bioactive component of Chinese cistanche tea, possesses various pharmacological effects. This study profiled, isolated, identified, and investigated the hepatoprotective capacities of metabolites in rat urine after the administration of ACT. Eleven metabolites, including one new compound (M8), were obtained and identified by nuclear magnetic resonance (NMR) spectroscopy for the first time. Compared with native ACT, ACT metabolites such as hydroxytyrosol (HT), 3-hydroxyphenylpropionic acid (3-HPP), and caffeic acid (CA) exhibited higher hepatoprotective activities by regulating oxidative stress, lipid peroxidation, and inflammatory responses in a GalN/LPS-induced-acute-hepatic-injury mouse model. The HT treatment markedly reduced the levels of TNF-α to 280 ± 14.3 ng/L compared with the model group (429 ± 9.20 ng/L, p < 0.01). The results obtained indicated that cistanche tea could be developed as a functional drink for the prevention of hepatic injuries and that ACT metabolites could be responsible for the potent hepatoprotective activity as well as the other therapeutic effects.