Jiao Lijuan, Li Yaxin, Zhang Yanqing, Liu Junjun, Xie Junbo, Zhang Kunsheng, Zhou Aimin
Department of Chemistry, Cleveland State University , Cleveland, Ohio 44115, United States.
J Agric Food Chem. 2017 Jun 7;65(22):4449-4455. doi: 10.1021/acs.jafc.7b01486. Epub 2017 May 25.
6‴-p-Coumaroylspinosin (P-CS), a bioactive flavonoid, is typically extracted from Semen Ziziphi Spinosae (SZS). In this study, a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/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 μg/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 μg/mL, while spinosin was produced when the P-CS concentration was 30 μg/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.
6″-对香豆酰斯皮诺素（P-CS）是一种生物活性黄酮类化合物，通常从酸枣仁中提取。在本研究中，建立了一种高效液相色谱-串联质谱（HPLC-MS/MS）方法来测定P-CS，以研究其与大鼠粪便孵育时的降解特性。结果表明，P-CS降解迅速，降解速度因P-CS浓度（3、15和30μg/mL）而异。P-CS的降解过程符合一级动力学。根据产物离子的质谱（MS）谱图模式，鉴定出P-CS的两种主要代谢产物。当P-CS浓度为3和15μg/mL时，獐牙菜苷是主要代谢产物，而当P-CS浓度为30μg/mL时，会产生斯皮诺素。斯皮诺素和獐牙菜苷可提高大鼠海马神经元中谷氨酸受体K1、K2和K3（GluK1、GluK2和GluK3）亚基的mRNA转录水平。此外，它们在这方面表现出明显的协同作用。总体而言，这些结果可用于解释P-CS的代谢和药理机制。
