ABSTRACT
A sensitive UPLC-HRMS method was developed and validated for simultaneous quantification of four active flavonoids from Chimonanthus nitens Leaf Granules (CNLG) in biological matrix. The method was utilized in pharmacokinetic study of the four flavonoids in rats as well as other evaluation assays in vitro. It was revealed that rutin, nicotiflorin, and astragalin had poor oral bioavailability in rats possibly due to low intestinal permeability and metabolism in intestinal flora. Kaempferol underwent rapid glucuronidation and sulphation in rat plasma with medium permeability coefficient. The results provided valuable data for future research and development of CNLG flavonoids.
Subject(s)
Flavonoids , Kaempferols , Plant Leaves , Animals , Flavonoids/pharmacokinetics , Flavonoids/chemistry , Plant Leaves/chemistry , Rats , Kaempferols/pharmacokinetics , Kaempferols/chemistry , Molecular Structure , Male , Rutin/pharmacokinetics , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacokinetics , Rats, Sprague-Dawley , Calycanthaceae/chemistry , Chromatography, Liquid/methods , Biological Availability , Mass Spectrometry/methods , Chromatography, High Pressure Liquid/methods , Liquid Chromatography-Mass SpectrometryABSTRACT
Objective To study and compare the metabolism of Hedyotis diffusa flavonoid extract in intestinal flora from human, normal rats and pseudo germ-free rats in vitro. Methods Intestinal flora of human, normal rats and pseudo germ-free rats were incubated with Hedyotis diffusa extract, rutosid, isoquercitrin and quercitrin under anaerobic conditions at 37℃.High-performance liquid chromatography with diode-array detection ( HPLC-DAD ) was used for the analysis of components and metabolic products.The trends of metabolic transformation of the various components were analyzed according to the changes in chromatographic peak areas at different incubation time points. Results The components of Hedyotis diffusa extract and its monomer were quickly metabolized by human and normal rat intestinal flora and the main metabolite was quercetin.However, they were hardly metabolized by intestinal flora from pseudo germ-free rats. The metabolism effect of intestinal flora was weaker on components than on the corresponding monomers. Conclusion By comparing flavonoids metabolism in intestinal flora from human, normal rats and pseudo germ-free rats, the important role of intestinal microflora in the metabolism of flavonoids is further confirmed.
ABSTRACT
Objective To investigate dynamic metabolism in vivo of Ginkgo Folium Tablet under the guidance of sequential metabolism thoughts. Methods In situ closed-loop in rats was carried out to study sequential metabolism of Ginkgo Folium Tablet through oral digestive system, namely to investigate and compare the intestinal flora metabolism, the gut wall metabolism and hepatic metabolism, combined with chromatographic fingerprint of blood samples. Results The analysis showed that 12 peaks in Ginkgo Folium Tablet were metabolized by intestinal flora, and 7 peaks generated through the gut wall. Most components of Ginkgo Folium Tablet were metabolized in liver, and 3 original medicine components were directly into the blood. Conclusion This study conducts a qualitative description of metabolism of Ginkgo Folium Tablet in different parts of the oral route, and provides references for the quality control, mechanism explanation and secondary development for Ginkgo Folium Tablet.
ABSTRACT
Objective To study and compare the metabolism of Chrysanthemum morifolium extracts(CME) in vitro intestinal flora from human,rat,Beagle dog,and rabbit.Methods Intestinal flora of human,rat,Beagle dog,and rabbit and CME were anaerobically cultured at 37 ℃ in vitro. After being extracted by acetic ether,the main metabolites of CME were separated and quantified by HPLC.Results In vitro,CME was easily metabolized by the intestinal flora and the main metabolites in incubation medium were determined in high concentration after 0.5 h.By LC-MS,luteolin and apigenin were identified,respectively;both metabolites were degraded with prolongation of incubation time and the concentrations of luteolin and apigenin were low after 24 h;moreover,CME was quickly metabolized by human,rat,Beagle dog intestinal flora,and gently by rabbit intesinal flora.Conclusion In vitro,CME is easily metabolized by intestinal flora human,rat,Beagle dog,and rabbit and the main metabolites are luteolin and apigenin.
