| Gynostemma pentaphyllum is a climbing plant of the Cucurbitaceae family.It is mostly used for the prevention and treatment of hypertension,high cholesterol,diabetes.It has the properties of liver-protective and antiinflammatory,and clinically used for various cancers.Preliminary research by our research group showed that the chemical components and the efficacy of G.pentaphyllum varies significantly under different origins and different processing methods.The purpose of this research is to qualitatively and quantitatively analyze the chemical components of G.pentaphyllum from Guangxi and Fujian provinces before and after heat processing,exploring and analyzing the effects of different origins and heat processing on the components of G.pentaphyllum,and to explore the metabolic pathways and pharmacokinetics of drug-derived components in blood,providing a reference for further basic research on pharmacodynamicsA qualitative analysis method for the chemical components of G.pentaphyllum was established based on the UPLC-Q-TOF-MS.A total of 102 saponins and 66 flavonoids were found in G.pentaphyllum in Guangxi province,and 120 saponins and 46 flavonoids were found in G.pentaphyllum from Fujian province.This project is the first time to discover the saponins linking butenoyl and pentenoyl groups in G.pentaphyllum.Combined with semi-quantitative and absolute quantitative analysis,it is speculated that the hydrolysis of glycosidic bonds and the hydrolysis of malonyl and acetyl groups mainly occurred during the heat processing.The extraction,separation and structure identification of G.pentaphyllum from Guangxi province were carried out.A total of 10 monomeric compounds were separated,among which Astragalin was a flavonoid separated from G.pentaphyllum for the first time.38 components in plasma of G.pentaphyllum extract were identified based on UPLC-Q-TOF-MS,22 of them were entered into the blood in the form of prototype,and 16 of them were metabolites of phase Ⅰ and phase Ⅱ.In addition to the form of prototype,the reactions of oxidation,sulfonation and glucuronidation are the main metabolic pathways of components in G.pentaphyllum.A method for pharmacokinetics of nine saponins was established based on the UPLC-Q-Trap-MS,and the PK character-istics of gypenoside L,damulin B and other saponins were elucidated for the first time,meanwhile,the results indicated that the metabolic processes of saponins in G.pentaphyllum may involve enterohepatic circulation.In conclusion,this paper established rapid and accurate qualitative and quantitative methods for the in vivo and in vitro components of G.pentaphyllum by LC-MS,revealed the differences of origins and the mechanism of heat processing,and clarifies the metabolic pathways and pharmacokinetic characteristics of components entering the blood.This paper provided an effective reference for the analysis of chemical components in G.pentaphyllum,the research on the metabolic mechanism of components entering the blood,and clinical rational drug use. |