人参水提取物中的人参三萜在人肠内菌体外温孵体系的转化研究

目的:研究人参水提取物中的人参三萜在人源肠内细菌作用下的生物转化。方法:将人参水提取物中人参三萜样品与人源肠内细菌进行温孵培养,采用超快速液相色谱-质谱/质谱法(UFLC-MS/MS)进行定性定量分析,确定人肠内细菌转化前后人参皂苷的动态变化。通过人参三萜种类和含量的变化,总结原人参二醇(PPD)型、原人参三醇(PPT)型和齐墩果烷(OLE)型人参三萜在人肠内细菌作用下的转化途径。结果:与对照品比对,共鉴定了49个化合物。人参皂苷在肠内细菌的作用下以脱糖基转化为主,其中人肠内细菌对PPD型人参皂苷的转化能力要明显强于对PPT型人参皂苷的转化能力,尤其是人参皂苷化合物K和20(S)-PPD的含量上升明显,甚至能达到初始值的数十倍;随着温孵时间的延长,含有乙酰基的人参皂苷含量迅速下降。结论:人参皂苷经人肠内细菌生物转化后更利于其吸收进入系统循环,为人参皂苷在体的吸收代谢和生物学活性发挥提供了参考。

Biotransformation of Triterpenes in Ginseng Radix et Rhizoma Water Extract with Human Intestinal Flora Incubation System in Vitro

Objective To study the biotransformation of triterpenes in Ginseng Radix et Rhizoma water extract with human intestinal flora incubation system in vitro.Methods The triterpene samples from Ginseng Radix et Rhizoma water extract were incubated with human intestinal flora and the resulting biotransformation products were qualitatively and quantitatively analyzed by ultra-fast liquid chromatography with tandem mass spectrometry (UFLC-MS/MS), thereby clarifying the dynamic changes of ginsenosides before and after biotransformation. According to the variation of the types and content of triterpenes, the transformation pathways of protopanaxatriol (PPT)-type, protopanaxadiol (PPD)-type, and oleanane (OLE)-type triterpenes under the action of human intestinal flora were summarized, respectively.Results A total of 49 compounds were identified through comparison with reference substances. Ginsenosides were mainly deglycosylated by human intestinal flora. The biotransformation of PPD-type ginsenosides was significantly stronger than that of PPT type, particularly the ginsenoside compound K (G-CK) and 20(S)-PPD. Content of ginsenosides with acetyl group decreased rapidly with the incubation.Conclusion Ginsenosides were more easily absorbed into systemic circulation after being transformed by human intestinal flora. This paper lays a basis for further study of the absorption, metabolism, and bioactivities of ginsenosides in vivo.