稀有原人参二醇型皂苷的人肠道菌群生物转化

利用高分离度液相色谱-四极杆飞行时间质谱(RRLC-Q-TOF MS)和超高效液相色谱-三重四极杆质谱(UPLC-QQQ MS)定性定量分析了稀有原人参二醇型皂苷Rd, F₂, Rg₃, CK和Rh₂在离体人肠道菌群中的生物转化过程. 并将上述二醇型皂苷与人肠道菌群在体外厌氧, 37 ℃下共温孵育, 采用电喷雾质谱在负离子模式进行检测, 鉴定代谢产物, 监测其含量变化, 拟合代谢路径. 结果表明, 人参皂苷Rd主要被代谢为F₂, Rg₃, CK, Rh₂和PPD; 人参皂苷F₂主要被代谢为CK和PPD; 人参皂苷Rg₃主要被代谢为Rh₂和PPD; 人参皂苷CK和Rh₂主要被代谢为PPD. 在离体条件下, 人参皂苷Rd, F₂和Rg₃会被肠道菌群完全转化为其代谢产物, 而人参皂苷CK和Rh₂则不能被肠道菌群完全转化为其代谢产物. 原人参二醇型皂苷在人肠道菌群中的主要转化为脱糖基反应, 单糖苷和苷元是稀有原人参二醇型皂苷在人体内发挥药效的物质基础.

Biotransformation of Rare Protopanaxadiol Saponin by Human Intestinal Microflora†

The rapid resolution liquid chromatography-quadrupole time-of-flight mass spectrometry(RRLC-Q-TOF MS) method and ultra high performance liquid chromatography-triple quadruple mass spectrometry(UPLC-QQQ MS) method were applied for qualitative and quantitative analyzing the biotransformation process of rare protopanaxadiol saponin Rd, Rg₃, F₂, CK and Rh₂ under intestinal micro flora in vitro. The rare protopanaxadiol saponin Rd, F₂, Rg₃, CK, Rh₂ and intestinal micro flora were cultured in vitro at 37 ℃ under anaerobic condition. The mass spectrometrics detection with electrospray ionization under negative ion mode was applied for identifying the metabolites, monitoring content variation, and matching metabolic pathways. The results show ginsenoside Rd is mainly metabolized into five products of F₂, Rg₃, CK, Rh₂ and PPD. Ginsenoside F₂ is mainly metabolized into two products of CK and PPD. Ginsenoside Rg₃ is mainly metabolized into two products CK and PPD. Ginsenosides CK and Rh₂ are both mainly metabolized into one product PPD. Ginsenosides Rd, F₂ and Rg₃ are metabolized completely into metabolic products, but ginsenosides CK and Rh₂ are not, under human intestinal micro flora condition in vitro. The results also indicated that deglycosylation reaction was the major metabolic pathway of rare protopanaxadiol saponin under the human intestinal microflora condition. And that monoglycosides and aglycone may be the material basis for rare protopanaxadiol saponin to exert its efficacy in human body.