Degradation Kinetics of 6 '''-p-Coumaroylspinosin and Identification of Its Metabolites by Rat Intestinal Flora

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Journal of Agricultural and Food Chemistry


6 '''-p-Coumaroylspinosin (P-CS), a bioactive flavonoid, is typically extracted from Semen Ziziphi Spinosae (SZS). In this study, a high-performance liquid chromatographytandem mass spectrometry (HPLCMS/MS) method was developed to determine P-CS for investigating the degradation characteristics of P-CS incubated with rat feces. The results showed that P-CS degraded rapidly and the degradation speeds varied depending upon the P-CS concentrations (3, 15, and 30 mu g/mL). The degradation of P-CS processes follow first-order kinetics. On the basis of the mass spectrometry (MS) spectrum mode of the product ions, two main metabolites of P-CS were identified. Swertisin was the main metabolite at 3 and 15 mu g/mL, while spinosin was produced when the P-CS concentration was 30 mu g/mL. Spinosin and swertisin could improve mRNA transcription levels of glutamate receptor K1, K2, and K3 (GluK1, GluK2, and GluK3) subunits in rat hippocampal neurons. In addition, they showed an obvious synergistic effect in this respect. Collectively, the results can be used to explain the metabolic and pharmacological mechanisms of P-CS.


This work was supported by the National Natural Science Foundation of China (Grants 31101235 and 31000749), the "131" Innovative Talents Training Project in Tianjin, and the Tianjin Thousand Talents Program (to Aimin Zhou in 2013).