Department of Natural Product Chemistry, College of Pharmacy, Jilin University, Changchun, China.
Department of Pharmaceutics, Changzhi Medical College, Changzhi, China.
Rapid Commun Mass Spectrom. 2020 Jul 15;34(13):e8788. doi: 10.1002/rcm.8788.
Panax ginseng C.A. Meyer (PG), which contains polysaccharides and ginsenosides as the major bioactive components, has been used to promote health and treat diseases for thousands of years in China. Total ginsenosides were extracted from a decoction of Panax ginseng (GD), which included both ginsenosides and polysaccharides, and dissolved in water to obtain a total ginsenosides aqueous solution (TGAS). To study their absorption and metabolism, the pharmacokinetics (PK) and metabolites of ginsenosides in vivo were investigated after the administration of GD and TGAS.
Rat and mice plasma samples were collected after the administration of GD and TGAS. Ultra-performance liquid chromatography coupled with time-of-flight mass spectrometry was used with the UNIFI platform to identify metabolites in the plasma sample. The pharmacokinetic parameters were calculated using a noncompartmental method in the Drug and Statistics software package.
Thirty ginsenoside metabolites were identified in mice plasma, of which only seven were found in the rat plasma after the administration of GD. The PK of ginsenosides Rb , Rc, and Rd were also determined after the oral administration of GD and TGAS and showed significant differences in the pharmacokinetic parameters.
There was no difference in the biotransformation pathways after the oral administration of GD and TGAS, indicating that there was no influence of polysaccharides on the biotransformation of ginsenosides in vivo. However, the pharmacokinetic parameters were different after the administration of GD and TGAS, possibly because of the polysaccharides in GD. This study should be of significance in exploring the basis of PG bioactivities and lays the foundation for the further development of new drugs using PG.
人参（PG），含有多糖和人参皂苷作为主要生物活性成分，在中国已经使用了几千年来促进健康和治疗疾病。总人参皂苷从人参煎剂（GD）中提取，其中包括人参皂苷和多糖，并溶解在水中以获得总人参皂苷水溶液（TGAS）。为了研究它们的吸收和代谢，在给予 GD 和 TGAS 后，研究了体内人参皂苷的药代动力学（PK）和代谢物。
在给予 GD 和 TGAS 后，收集大鼠和小鼠的血浆样品。使用超高效液相色谱-飞行时间质谱联用技术（UNIFI 平台），结合药物和统计学软件包中的非房室模型方法，在血浆样品中鉴定代谢物。
在小鼠血浆中鉴定出 30 个人参皂苷代谢物，其中仅在给予 GD 后在大鼠血浆中发现了 7 种。口服 GD 和 TGAS 后还确定了人参皂苷 Rb、Rc 和 Rd 的 PK，并且在药代动力学参数方面显示出显著差异。
口服 GD 和 TGAS 后的生物转化途径没有差异，表明多糖对体内人参皂苷的生物转化没有影响。然而，给予 GD 和 TGAS 后的药代动力学参数不同，可能是因为 GD 中的多糖。这项研究对于探索 PG 生物活性的基础具有重要意义，并为进一步开发使用 PG 的新药奠定了基础。
