Division of Pharmacognosy, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China.
Molecules. 2018 Oct 19;23(10):2702. doi: 10.3390/molecules23102702.
Sibirioside A and angoroside C are two important phenylpropanoid glycosides of the traditional Chinese medicine Scrophulariae Radix. High performance liquid chromatography, coupled with an ion trap time-of-flight multistage mass spectrometry equipped with electrospray ionization source (HPLC-ESI-IT-TOF-MS), was applied to the profile and we identified the metabolites of sibirioside A and angoroside C in vivo in rats. A total of four metabolites of sibirioside A were identified: SM1, SM2 and SM3 which were known as new compounds. A total of 25 metabolites were detected for angoroside C: AM4, AM5, AM6, AM7, AM16, AM17, AM20, AM21, AM22, AM23 and AM25 which were identified to be new compounds. The main metabolic reactions were hydrolysis, reduction, hydroxylation, methylation, sulfation, and gluconylation. The prototype of sibirioside A was widely distributed in tissues found in the heart, liver, spleen, lung, kidney, stomach and small intestine of rats, and mainly distributed in the stomach, small intestine, kidney and liver. But for angoroside C, nothing was found in the viscera except the stomach and small intestine. The metabolites of sibirioside A were mainly eliminated from feces, while it was urine for the metabolites of angoroside C. Furthermore, 19 metabolites were likely to have bioactivities based on the 'PharmMapper' analysis, which roughly matched the known pharmacological activities of Scrophulariae Radix (SR) and the prototypes. One of the main pharmacological activities of SR in traditional Chinese medicine is anti-diabetes, and the predicted results showed that SM1, SM2, SM3, AM2, AM4, AM5, AM6, AM9, AM10, AM11, AM12, AM13, AM15, AM18, AM19, AM24, and AM25 might be used to cure diabetes. These findings provide a reference for studying the metabolism, distribution and pharmacological actions of phenylpropanoid glycosides in vivo.
西伯利亚苷 A 和玄参苷 C 是传统中药玄参的两种重要苯丙素糖苷。采用高效液相色谱-电喷雾离子阱飞行时间多级质谱联用（HPLC-ESI-IT-TOF-MS）对其体内代谢产物进行了分析。共鉴定出西伯利亚苷 A 的 4 种代谢产物：SM1、SM2 和 SM3，均为新化合物。共检测到玄参苷 C 的 25 种代谢产物：AM4、AM5、AM6、AM7、AM16、AM17、AM20、AM21、AM22、AM23 和 AM25，均为新化合物。主要代谢反应为水解、还原、羟化、甲基化、硫酸化和葡萄糖醛酸化。西伯利亚苷 A 的原型广泛分布于大鼠心、肝、脾、肺、肾、胃和小肠组织中，主要分布于胃、小肠、肾和肝中。而对于玄参苷 C，除胃和小肠外，其他内脏器官均未发现。西伯利亚苷 A 的代谢产物主要从粪便中排出，而玄参苷 C 的代谢产物则从尿液中排出。此外，根据“PharmMapper”分析，有 19 种代谢产物可能具有生物活性，这大致与玄参的已知药理活性和原型相匹配。玄参在传统中药中的主要药理作用之一是抗糖尿病，预测结果表明，SM1、SM2、SM3、AM2、AM4、AM5、AM6、AM9、AM10、AM11、AM12、AM13、AM15、AM18、AM19、AM24 和 AM25 可能用于治疗糖尿病。这些发现为研究苯丙素糖苷在体内的代谢、分布和药理作用提供了参考。
