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

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

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。

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.