三七皂苷的人肠道菌群体外代谢研究  

Metabolism of Saponins of Panaxnotoginseng by Human Intestinal Microflora in vitro

作　　者：李雪晴[1] 李丽[1] 刘秀峰[1] 刘吉华[1] 

机构地区：[1]中国药科大学江苏省中药评价与转化重点实验室,江苏南京211198

出　　处：《药物生物技术》2017年第3期218-223,共6页Pharmaceutical Biotechnology

基　　金：国家自然科学基金资助项目(No.81173471);江苏高校优势学科建设工程资助项目(PAPD)

摘　　要：研究三七中皂苷类成分(原人参二醇PPD型和原人参三醇PPT型)的人离体肠道菌群的厌氧代谢,为三七皂苷类成分代谢特征的研究提供参考。采集健康成人的新鲜粪便制备肠道菌群混悬液,分别与每种三七皂苷进行体外厌氧培养,HPLC-ESI-Q-TOF-MS/MS方法对代谢产物进行定性和定量分析。结果:(1)三七中皂苷类成分的代谢途径包括PPD和PPT型,PPD型代谢途径为人参皂苷Rb1→人参皂苷Rd→人参皂苷Rg3→人参皂苷Rh2→PPD和人参皂苷Rb1→七叶胆苷XVII→人参皂苷F2→人参皂苷Compound K→PPD,PPT型代谢途径为人参皂苷Re→人参皂苷Rg2→人参皂苷F1→PPT和三七皂苷R1→三七皂苷R2→人参皂苷Rh1→PPT以及人参皂苷Rg1→人参皂苷Rh1→PPT。(2)三七皂苷的人肠道菌群代谢反应主要是脱糖反应,即在相同母核结构下,四糖苷、三糖苷、二糖苷、单糖苷逐步转化为苷元,其中单糖苷和苷元在肠道菌群环境中的含量较多且相对稳定。(3)由于三七皂苷上的糖基位置的差异,PPD的代谢程度要高于PPT。结论:三七中的皂苷类成分可被人肠道菌群代谢,皂苷成分的代谢造成比例发生变化,单糖苷和苷元的含量较多且相对稳定,揭示了单糖苷和苷元可能是三七在体内发挥药效的物质基础。To investigate metabolism of saponins of Panax notoginseng, Protopanoxadiol （PPD） and Protopanaxatriol （PPT） were incubated with human intestinal mieroflora in vitro, which could provide scientific basis for metabolism characteristic of Panax notog- inseng saponins by human intestinal microflora. Healthy human intestinal microflora were obtained from human feces, and were incu- bated with each kind of Panax notoginseng saponins respectively. HPLC-ESI-Q-TOF-MS/MS was applied for the qualitative and quantitative analysis of the metabolites. Results ： （ 1 ） PPD-types and PPT-types were two metabolic pathways of Panax notoginseng saponins ,PPD-types were metabolized in the pathway：ginsenoside Rbl→ginsenoside Rd→ginsenoside Rg3→ginsenoside Rh2→PPD and ginsenoside Rb1→Gypenoside XVII→ginsenoside F2 →ginsenoside Compound K→PPD, PPT-types were metabolized in the pathway： ginsenoside Re→ginsenoside Rg2→ginsenoside F1→PFF, Notoginsenoside R1 →Notoginsenoside R2→ginsenoside Rh1 PPT and ginsenoside Rgl→ginsenoside Rh1→PPT. （2） Major metabolic reaction of Panax notoginseng saponins was deglycosylation gradually by human intestinal microflora. Tetrasaccharide saponins/trisaccharidesaponins/disaccharide saponins and monosaccharide saponins were metabolized to PPD or PPT finally, monosaccharide saponins and sapogenin were the major metabolites of saponins and remained relatively stable. （3）The metabolism of PPD was higher than PPT, because of the different location of glycosyl. The metabo- lism of Panax notoginsengs aponins have changed the composition ratio of saponins, and monosaccharide saponins and sapogenin were the majority of saponins after metabolized with human intestinal microflora, implying that monosaccharide saponins and sapogenin were the possible material basis of drug efficacy of Panax notoginseng in vitro.

关 键 词：原人参二醇 原人参三醇 人肠道菌群 脱糖反应 液相质谱 药效物质基础 

分 类 号：R282.710.2[医药卫生—中药学]