通过RRLC-Q-TOF MS和UPLC-QQQ MS分析原人参三醇型皂苷在人肠道菌群中的代谢产物

Analysis of Metabolites of Protopanaxatriol Saponins in Human Intestinal Flora by RRLC-Q-TOF MS and UPLC-QQQ MS

通过高分离度快速液相色谱-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)法对原人参三醇型皂苷Re、Rg 1、Rg 2、Rh 1、Rf、F 1、R 1在人肠道菌群中的转化产物进行定性、定量分析,确定原人参三醇型皂苷的代谢产物、转化途径和60 h时的转化率。结果表明,人参皂苷Re的转化产物为人参皂苷Rg 1、Rg 2、Rh 1、F 1和PPT,转化率为91%;人参皂苷Rg 1的转化产物为人参皂苷Rh 1、F 1和PPT,转化率为80%;人参皂苷Rg 2的转化产物为人参皂苷Rh 1和PPT,转化率为73%;人参皂苷Rh 1和F 1主要通过PPT代谢,转化率分别为82%和81%;人参皂苷Rf的转化产物为人参皂苷Rh 1和PPT,转化率为89%;三七皂苷R 1的转化产物为人参皂苷Rg 1、R 2、Rh 1和PPT,转化率为79%。原人参三醇型皂苷类成分可被人肠道菌群代谢,主要通过丢失糖残基形成转化产物,而次级皂苷和苷元是人参在体内发挥药理作用的物质基础。

Ginseng is popular among scholars at home and abroad,it is an important and widely used herbal medicine in Asia and western countries.Ginseng mainly contains ginsenosides,polysaccharides and amino acids.Ginsenoside is the main active ingredient of ginseng and has many pharmacological activities,it is mainly divided into two types according to its structure:protopanaxadiol(PPD)and protopanaxatriol(PPT).Ginseng products are usually administered orally,studies have shown that ginsenosides have low oral bioavailability and metabolized into secondary glycosides in the gastrointestinal tract to play its pharmacological role.In order to discover the metabolites of protopanaxatriol saponins in human intestinal flora,ginsenoside Re,Rg 1,Rg 2,Rh 1,Rf,F 1,R 1 were incubated in bacterial solution,the identification and quantification of metabolites of protopanaxatriol ginsenosides were determined by using rapid resolution liquid chromatography-quadrupole time-of-flight mass spectrometry(RRLC-Q-TOF MS)and ultra-high performance liquid chromatography-triple quadrupole mass spectrometry(UPLC-QQQ MS).As a result,ginsenoside Rg 1,Rg 2,Rh 1,F 1 and PPT are transformation products of ginsenoside Re,with the conversion rate of 91%.Ginsenoside Rh 1,F 1 and PPT are transformation products of ginsenoside Rg 1,and the conversion rate is 80%.Ginsenoside Rh 1 and PPT are transformation products of ginsenoside Rg 2,and the conversion rate is 73%.Ginsenoside Rh 1 and F 1 are mainly metabolized by PPT,the conversion rate is 82%and 81%,respectively.Ginsenoside Rh 1 and PPT are products of ginsenoside Rf,and the conversion rate is 89%.Ginsenoside Rg 1,R 2,Rh 1 and PPT are conversion products of notoginsenoside R 1,the conversion rate is 79%.The study suggested that protopanaxatriol ginsenosides can be metabolized by human intestinal flora,the transformation products are mainly formed by the loss of glucose residues,it is revealed that secondary ginsenoside is the material basis of pharmacological action in vivo.