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

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, Rg₁, Rg₂, Rh₁, Rf, F₁, R₁ 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 Rg₁, Rg₂, Rh₁, F₁ and PPT are transformation products of ginsenoside Re, with the conversion rate of 91%. Ginsenoside Rh₁, F₁ and PPT are transformation products of ginsenoside Rg₁, and the conversion rate is 80%. Ginsenoside Rh₁ and PPT are transformation products of ginsenoside Rg₂, and the conversion rate is 73%. Ginsenoside Rh₁ and F₁ are mainly metabolized by PPT, the conversion rate is 82% and 81%, respectively. Ginsenoside Rh₁ and PPT are products of ginsenoside Rf, and the conversion rate is 89%. Ginsenoside Rg₁, R₂, Rh₁ and PPT are conversion products of notoginsenoside R₁, 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.