Content determination of seven active components of Eucommiae Cortex in aortic vascular endothelial cells of spontaneously hypertensive rats by UPLC-MS/MS / 中国中药杂志

In the present study, the contents of seven active components [genipinic acid(GA), protocatechuic acid(PCA), neochlorogenic acid(NCA), chlorogenic acid(CA), cryptochlorogenic acid(CCA),(+)-pinoresinol di-O-β-D-glucopyranosid(PDG), and(+)-pinoresinol 4'-O-β-D-glucopyranoside(PG)] of Eucommiae Cortex in aortic vascular endothelial cells of spontaneously hypertensive rats(SHR) were simultaneously determined by ultra-high liquid chromatography-triple quadrupole mass spectrometry(UPLC-MS/MS). The qualified SHR models were selected. The primary aortic endothelial cells(VECs) of rats were separated and cultured by ligation and adherence, followed by subculture. After successful identification, an UPLC-MS/MS method for simultaneously determining the contents of GA, PCA, NCA, CA, CCA, PDG, PG in seven components of Eucommiae Cortex in VECs was established, including specificity, linearity, matrix effect, recovery, accuracy, precision and stability. The established method had the lo-west limit of quantification of 0.97-4.95 μg·L~(-1), accuracy of 87.26%-109.6%, extraction recovery of 89.23%-105.3%, matrix effect of 85.86%-106.2%, and stability of 86.00%-112.5%. Therefore, the established accurate UPLC-MS/MS method could rapidly and simultaneously determine the contents of the seven active components of Eucommiae Cortex in VECs of SHRs, which provided a refe-rence for the study of cellular pharmacokinetics of active components of Eucommiae Cortex extract.

Simultaneous determination of eleven volatile components in Cinnamomi Oleum by GC-MS / 中国中药杂志

A gas chromatography-triple quadrupole mass spectrometry(GC-MS) method was established for the simultaneous determination of eleven volatile components in Cinnamomi Oleum and the chemical pattern recognition was utilized to evaluate the quality of essential oil obtained from Cinnamomi Fructus medicinal materials in various habitats. The Cinnamomi Fructus medicinal materials were treated by water distillation, analyzed using GC-MS, and detected by selective ion monitoring(SIM), and the internal standards were used for quantification. The content results of Cinnamomi Oleum from various batches were analyzed by hierarchical clustering analysis(HCA), principal component analysis(PCA), and orthogonal partial least squares-discriminant analysis(OPLS-DA) for the statistic analysis. Eleven components showed good linear relationships within their respective concentration ranges(R~2>0.999 7), with average recoveries of 92.41%-102.1% and RSD of 1.2%-3.2%(n=6). The samples were classified into three categories by HCA and PCA, and 2-nonanone was screened as a marker of variability between batches in combination with OPLS-DA. This method is specific, sensitive, simple, and accurate, and the screened components can be utilized as a basis for the quality control of Cinnamomi Oleum.

Determination of plasma protein binding rate of Shuganning Injection using equilibrium dialysis and UPLC-MS/MS / 中国中药杂志

Traditional Chinese medicine(TCM) compound preparations have complex compositions. As a widely used TCM injection, Shuganning Injection, its in vivo processes are not yet fully understood. Determining the plasma protein binding rate is of great significance for pharmacokinetic and pharmacodynamic studies. In this experiment, the equilibrium dialysis method combined with UPLC-MS/MS technology was used to determine the plasma protein binding rates of 10 components, including p-hydroxyacetophenone, caffeic acid, baicalein, oroxylin A, geniposide, baicalin, cynaroside, oroxylin A-7-O-β-D-glucuronide, scutellarin, and hyperoside, in Shuganning Injection in rat and human plasma to provide a theoretical basis for further elucidating the in vivo processes of Shuganning Injection and guiding clinical medication. The results showed that, except for baicalein and geniposide, the plasma protein binding rates of the other eight components were higher in human plasma than in rat plasma, and there were interspecies differences. In human plasma, except for geniposide, caffeic acid, and baicalin, the plasma protein binding rates of the remaining seven components were above 80%, with baicalein and oroxylin A exceeding 90%. All components exhibit a high level of binding to plasma proteins, with the exception of geniposide.

Simultaneous determination of content of eight components in Caesalpinia decapetala by UPLC-MS/MS / 中国中药杂志

The present study established the ultra-high performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method for simultaneous determination of the content of eight major active components in Caesalpinia decapetala and performed the quality evaluation of C. decapetala from different habitats with the chemical pattern recognition. The analysis was carried out on a Waters BEH C_(18) column(2.1 mm×100 mm, 1.7 μm) at 40 ℃, with the mobile phase of water containing 0.1% formic acid(A) and acetonitrile containing 0.1% formic acid under gradient elution, the flow rate of 0.3 mL·min~(-1), and the injection volume of 1 μL. The electrospray ionization(ESI) source in the negative mode and multiple reaction monitoring(MRM) were used for MS quantitative analysis. The content results were analyzed by the hierarchical cluster analysis(HCA) and principal component analysis(PCA) for the evaluation of the quality difference. Eight components showed good linear relationships within their respective concentration ranges(r>0.999), with the average recoveries of 96.85%-103.4% and RSD of 0.52%-2.8%. The analysis results showed that the quality of samples from different batches was different. The samples were classified into three clusters by HCA and PCA. The method is simple, sensitive, accurate, and efficient, and can be used for the quality evaluation of C. decapetala.

Difference Analysis of Pharmacokinetic Behavior of Active Ingredients in Wujiwan Between Normal Rats and Rats with Irritable Bowel Syndrome / 中国实验方剂学杂志

Objective:To establish an ultra-performance liquid chromatography-mass spectrometry （UPLC-MS/MS） for determining the plasma concentrations of 10 active ingredients in Wujiwan at different time points after oral administration， and to compare the pharmacokinetic characteristics between normal rats and rats with chronic visceral hypersensitive irritable bowel syndrome （CVH-IBS）. Method:CVH-IBS rat model was prepared by the neonatal rat colon percutaneous transluminal coronary angioplasty （PTCA） balloon stimulation method. After intragastric administration of Wujiwan （0.245 g·kg^-1）， blood was collected from the jugular vein at different time points， and the plasma concentrations of 10 active ingredients （berberine hydrochloride， palmatine hydrochloride， coptisine hydrochloride， jatrorrhizine hydrochloride， epiberberine， dihydroberberine， evodiamine， evodine， paeoniflorin， albiflorin） in Wujiwan was detected simultaneously by UPLC-MS/MS， the pharmacokinetic parameters of each component in normal rats and CVH-IBS rats were calculated. Result:The established UPLC-MS/MS could sensitively and accurately detect the plasma concentrations of 10 active ingredients of Wujiwan in rats. Compared with the normal group， the absorption rates of these 10 active ingredients of Wujiwan in the blood of CVH-IBS rats all decreased to a certain extent， and the peak time （<italic>t</italic>_max） was prolonged. Among them， the <italic>t</italic>_max of berberine hydrochloride and jatrorrhizine hydrochloride were significantly prolonged from 54 minute and 39 minute to 90 minute， respectively （<italic>P</italic><0.05， <italic>P</italic><0.01）. Area under the plasma concentration-time curve （AUC_0-<italic>_t</italic>） of each component increased， and evodiamine and paeoniflorin were significantly different （<italic>P</italic><0.05，<italic> P</italic><0.01）. The clearance rates （CL/<italic>F</italic>） of these 10 active ingredients were all decreased， among which berberine hydrochloride， palmatine hydrochloride and evodiamine had significant differences （<italic>P</italic><0.05， <italic>P</italic><0.01）. Conclusion:There are significant differences in the pharmacokinetic behavior of the active ingredients in Wujiwan between normal rats and CVH-IBS rats， which may be related to the destruction of microstructure of intestinal epithelial cells and the change of activity of liver enzymes under the pathological state of IBS.

Analysis of research status based on projects in pharmacokinetics of traditional Chinese medicine funded by National Natural Science Foundation of China / 中国中药杂志

The pharmacokinetics of traditional Chinese medicine is a subject that studies the dynamic changes of the absorption, distribution, metabolism and excretion of complex components of traditional Chinese medicine, which is an important method for elucidating the pharmacodynamic material basis, action characteristics, and compatibility mechanisms of traditional Chinese medicine. However, given on the fact that traditional Chinese medicine is a multi-dimensional and complex system with multiple components, multiple pathways, multiple targets, and an unclear pharmacodynamic material basis, the research on the pharmacokinetics of traditio-nal Chinese medicine has become a scientific and technological problem. Although the pharmacokinetics of traditional Chinese medicine has achieved remarkable development with the emergence of new theories, methods and technologies, there are still some problems in the application of the research direction of the pharmacokinetics of traditional Chinese medicine judging from the current application of the National Natural Science Foundation of China. Therefore, this article discussed the current research status on pharmacokinetics of traditional Chinese medicines by analyzing the projects funded by the National Natural Science Foundation of China in the past 5 years from 2016 to 2020, mainly including the application and funding analysis, main research contents of the projects in pharmacokinetics of traditional Chinese medicines. And the research hotspots, difficulties and deficiencies were focused in order to provide certain reference for researchers engaged in pharmacokinetics of traditional Chinese medicine.

Intestinal absorption properties of Gastrodiae Rhizoma powder with different particle size by circulation pass perfusion model in rats / 中国中药杂志

This study is to study the absorption properties of different particle size of Gastrodiae Rhizoma powder in rats. In vivo circulation pass perfusion model combined with ultra high performance liquid chromatography-mass spectrometry(UPLC-MS/MS) method was used to determine the cumulative absorption of each component in different particle size of Gastrodiae Rhizoma powder, and the effect of different particle size, different concentrations, different intestine segments and bile on the intestine absorption of gastrodin and other compositions in Gastrodiae Rhizoma powder was investigated to illuminate the absorption properties and compare the absorption difference of gastrodin and other compositions in Gastrodiae Rhizoma powder in different particle size. The results showed that the absorption of gastrodin in each intestinal segment has no significant difference, pointing out that gastrodin may be passive absorption and the absorption of barrison glycosides may be active absorption; the absorption of gastrodin in ultrafine powder was better than that of common powder and superfine powder of Gastrodiae Rhizoma; the absorption of these barrison glycosides was good in ultrafine powder of Gastrodiae Rhizoma under the high concentration. However, an appropriate degree of superfine grinding can promote the absorption of active ingredients of Gastrodiae Rhizoma. This test can provide information for the deep development of Gastrodiae Rhizoma.

Differences in intestinal absorption characteristics of Laportea bulbifera extract in normal and rheumatoid arthritis model rats by isolated everted intestine model / 中国中药杂志

This work aimed to investigate the intestinal absorption characteristics of Laportea bulbifera extract in normal and rheumatoid arthritis model rats. The contents of neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, rutin, kaempferol-3-O-rutinoside, galuteolin, quercetin and isoquercetin in intestinal absorption solution samples were detected by UPLC-MS/MS with 5.0 g·L~(-1) as the absorption concentration. The cumulative absorption(Q) and absorption rate constant(K_a) were calculated, and the absorption characteristics of different components of L. bulbifera in intestinal absorption solution of normal rats and rheumatoid arthritis rats were compared. The results showed that all the eight index components in the extract of L. bulbifera could be absorbed into the intestinal capsule, the cumulative absorption-time curve of each component showed an upward trend without saturation, and the correlation regression coefficient(R~2) was greater than 0.92, which is consistent with the zero-order absorption rate process. It was speculated that the possible absorption mode of each component was passive diffusion. In normal condition, the absorption of ileum was the best(except chlorogenic acid), and in pathological condition, duodenum was the best. The total absorption of 8 components in each intestinal segment of RA rats was better than that of normal rats, which speculated that rheumatoid arthritis may change the specific site of drug absorption. The experimental results showed that rheumatoid arthritis could change the intestinal absorption of the extract of L. bulbifera, and its mechanism needs further study.

Simultaneous determination of four components of Shuganning Injection in rat plasma by UPLC-MS/MS and its application to a pharmacokinetic study / 中国中药杂志

This study aims to reveal the pharmacokinetics of Shuganning Injection in normal rats. In this experiment,ultra-high performance liquid chromatography-electrospray-tandem mass spectrometry( UPLC-ESI-MS/MS) was used to establish an analytical method for simultaneous determination of chlorogenic acid,gardenioside,oroxylin A and baicalin in rat plasma. Then,the non-compartmental model( NCA) in Phoenix WinN onL in 6. 4 software was used to fit pharmacokinetic parameters. The methodological validation showed that the linear relationship of the components in rat plasma samples were good( r>0. 995). The recovery rate and matrix effect of plasma samples with low,middle and high concentration were 79. 14%-101. 4%. The intra-day and inter-day precision,accuracy and stability meet the requirements of biological sample analysis. The half-life( t1/2) of chlorogenic acid,gardenioside,oroxylin A did not change significantly and the area under blood concentration-time curve( AUC0-t) is proportional to the dose,which suggested that three components showed a linear kinetic characteristics,but baicalin showed nonlinear kinetic characteristics. Moreover,the retention time of each component in rats was short. The established UPLC-MS/MS quantitative analysis method is rapid,sensitive and accurate,which can be used for the determination of chlorogenic acid,gardenioside,oroxylin A and baicalin in rat plasma and pharmacokinetic study of Shuganning Injection.

Study on metabolites of Laportea bulbifera extract in rat feces based on UHPLC-Q-TOF-MS~E technique / 中国中药杂志

This project is to study the metabolites of Laportea bulbifera extract in rat feces. After the SD rats were gavaged with the extract(136 g·kg~(-1), according to the crude drug dose), the metabolites in their feces were detected by UHPLC-Q-TOF-MS~E technique, and the obtained mass spectrometry data was combined with UNIFI software for prediction. The prototype components and metabolites in rat feces were identified with reference materials and related literature. A total of 43 metabolites were identified(including 8 prototype components and 35 metabolites). The metabolic pathways mainly include monocaffeoylquinic acid(hydrogenation reduction, ring-opening cracking, sulfation, hydroxylation, glucuronidation), quercetin(O-C2 bond ring-opening cleavage, C2-C3 double bond reduction, rutin carbonylation) and so on. The metabolites and metabolic process of L. bulbifera extract in rat feces were clarified, which provided a basis for the study of the active substances and its mechanism of action.

UPLC-Q-TOF-MS/MS analysis on prototypes components and metabolites of effective fractions of Polygonum orientale flower in rat serum and urine / 中国中药杂志

Ultra performance liquid chromatography coupled with time-of-flight mass spectrometry( UPLC-Q-TOF-MS/MS) method was applied to analyze the prototypes and metabolites of the effective components of Polygonum orientale in SD rat serum and urine. The separation was performed on Agilent Eclipse Plus C_(18) column( 2. 1 mm×100 mm,1. 8 μm),with 0. 1% formic acid solution( A)-acetonitrile( B) as the mobile phase for gradient elution. Mass spectrometry data of biological samples were obtained under positive and negative electrospray ion mode. By comparing chromatogram differences between blank samples and drug treatment samples,prototype components and metabolites of the effective components of P. orientale extract were identified. The results showed that 12 metabolites were detected in serum and 26 metabolites in urine( including cross-components) of rats. The main metabolic pathways included hydrogenation,hydroxylation,glucuronidation,sulfation reaction,and methylation-glucuronidation,etc. The method established in this study was reliable and effective for studying the metabolic characteristics of the effective components of P. orientale in rats,and it can provide a reference for further studies on therapeutic material basis of this herb.

Determination of plasma protein binding rates of nine compounds of Inula cappa extraction based on method of equilibrium dialysis / 中国中药杂志

To determine the plasma protein binding rate of the nine compounds in Inula cappa extraction by the method of equilibrium dialysis. The proteins in plasma samples were precipitated by methanol, and the ultra-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) was developed for determination of the concentrations of the nine active compounds, namely chlorogenic acid, scopolin, neochlorogenic acid, cryptochlorogenic acid, 1,3-O-dicaffeoylquinic acid, galuteolin, 3,4-O-dicaffeoylquinic acid, 3,5-O-dicaffeoylquinic acid, 4,5-O-dicaffeoylquinic acid, with the internal standard of puerarin. We found that all components have a good linearity(r≥0.999), and accuracy, precision, extraction recovery and stability conformed to the requirements of determination, without endogenous compounds disturbing within the range of optimum concentration. This suggested that the method was stable and reliable, and could be used for the determination of the plasma protein binding rates of the nine active compounds in rat and human plasma of I. cappa. The plasma protein binding rates of the nine active compounds in rat and human plasma respectively were(41.07±0.046)%-(94.95±0.008)%, and(37.66±0.043)%-(97.46±0.013)%. According to the results, there were differences in the plasma protein binding rates of the nine compounds in I. cappa extraction between rat and human.

Comparison of in Vitro Dissolution of Active Ingredients in Gastrodiae Rhizoma Powder with Different Particle Size / 中国实验方剂学杂志

Objective: To compare in vitro dissolution behaviors of active ingredients (gastrodin,parishin A,p-hydroxybenzyl alcohol,parishin B and parishin C) in Gastrodiae Rhizoma powder with different particle size.Method: In vitro dissolution of Gastrodiae Rhizoma powder in different dissolution media (water,artificial gastric juice and artificial intestinal juice) were detected by stirring paddle method.Dissolution of these five components in Gastrodiae Rhizoma powder with different particle size was determined by HPLC,mobile phase was acetonitrile-0.1% phosphoric acid solution for gradient elution,column temperature was set at 40℃ and detection wavelength was 220 nm.Result: In water and artificial intestinal juice,the dissolution rates of five active components in three kinds of Gastrodiae Rhizoma ultrafine powders were higher than that of the fine powder and the finest powder;in artificial gastric juice,the dissolution rates of gastrodin and p-hydroxybenzyl alcohol in Gastrodiae Rhizoma ultrafine powders were higher than that of the other powders,and the dissolution rate of parishin A in Gastrodiae Rhizoma ultrafine powders was lower than that of the other powders.Conclusion: An appropriate degree of superfine grinding can promote the dissolution of active ingredients in Gastrodiae Rhizoma,but not as fine as possible.The dissolution medium has an obvious influence on the dissolution behaviors of active components,which provides a reference for screening optical particle size of Gastrodiae Rhizoma powder in clinical application.

Protective Effect of Gastrodiae Rhizoma Powder with Different Particle Sizes on Cerebral Ischemia Reperfusion Injury in Rats / 中国实验方剂学杂志

Objective: To study the protective effect of Gastrodiae Rhizoma ultrafine powder with different particle sizes on focal cerebral ischemia-reperfusion injury in rats, in order to provide theoretical basis for the application of ultrafine powder technology in related products. Method: The SD rats were randomly divided into six groups, namely sham-operated group, ischemia-reperfusion group, Gastrodiae Rhizoma ultramicro-powder Ⅰ group(1.2 g·kg-1), Gastrodiae Rhizoma ultramicro-powder Ⅱ group(1.2 g·kg-1), Gastrodiae Rhizoma ultramicro-powder Ⅲ group(1.2 g·kg-1), and nimodipine positive drug group(12.6 g·kg-1). The cerebral ischemia-reperfusion model was established after 7 days of drug administration. The focal ischemia reperfusion injury model was prepared by middle cerebral artery occlusion (MCAO) for 1 h followed by reperfusion for 24 h. The infarct size of brain tissue was measured by triphenyltetrazolium Chloride(TTC) staining. The activities of superoxide dismutase (SOD), malondialdehyde (MDA) and nitricoxide synthase (NOS) in brain homogenate and serum were measured by colorimetry. The contents of glutamate(Glu), aspartic acid(Asp) and glycine(Gly) in hippocampus were determined by liquid chromatography-tandem mass spectrometry (LC/MSMS). Result:The model group showed obvious signs of neurobehavioral deficit (PPPPPConclusion:Gastrodiae Rhizoma ultramicro-powder with different particle sizes has a protective effect on cerebral ischemia-reperfusion injury, and the Gastrodiae Rhizoma ultramicro-powder Ⅲ group has a more obvious protective effect than the the Gastrodiae Rhizoma ultramicro-powder Ⅰ group. The results showed that the protective effect of Gastrodiae Rhizoma ultramicro-powder on middle cerebral artery ischemia-reperfusion in rats was related to its particle size.

Serum Pharmacochemical Analysis of Periploca forrestii Rhizomes Based on UPLC-Q-TOF-MS / 中国实验方剂学杂志

Objective:To study the serum pharmacochemistry of Periploca forrestii rhizomes,and to investigate the pharmacological material basis of extract of P. forrestii rhizomes in rats. Method:Rapid identification of constituents absorbed into blood was carried out by UPLC-Q-TOF-MS,according to retention time,accurate relative molecular mass and standard substance comparison,these constituents were identified and speculated by Data Analysis,Metabolite Detect and other softwares,then preliminary determination of constituents absorbed into blood of rats after oral administration of extract of P. forrestii rhizomes was investigated. Result:Totally 17 constituents absorbed into blood were detected in serum,ten of them were prototype constituents and the other were metabolites.Seven of the prototypes were identified as 5-O-caffeoylquinic acid,4-O-caffeoylquinic acid,3-O-caffeoylquinic acid,3,4-di-O-caffeoylquinic acid,3,5-di-O-caffeoylquinic acid,4,5-di-O-caffeoylquinic acid and periplocin. Conclusion:These constituents absorbed into blood may be substances that act directly in vivo of P. forrestii rhizomes,and it is helpful to clarify pharmacological material basis and mechanism of this herb.

Kinetic Analysis of Enzymatic Reaction of Active Components from Xinshao Formula in Liver Microsomes of Sham-Operated and Cerebral Ischemia-reperfusion Injury Rats / 中国实验方剂学杂志

Objective: To investigate and compare enzymatic kinetics of scutellarin,apigenin-7-O-glucronide and paeoniflorin from Xinshao fomula in liver microsomes of sham-operated rats and middle cerebral artery occlusion(MCAO) rats with focal cerebral ischemia-reperfusion injury. Method: Xinshao fomula were incubated respectively with liver microsomes of sham-operated rats and MCAO rats,UPLC-MS and substrate elimination method was employed,Michaelis constant(Km),maximum velocity of enzymatic reaction(Vmax) and intrinsic clearance(CLint) of these three components from Xinshao fomula in liver microsomes of sham-operated rats and MCAO rats were calculated,these parameters between different groups were evaluated by statistical analysis. Result: The Km values of scutellarin,apigenin-7-O-glucronide and paeoniflorin in liver microsomes of MCAO rats were (0.798±0.031),(0.213±0.017),(0.499±0.029) μmol·L-1,which were quite different to these in liver microsomes of sham-operated rats.Compared with the sham-operated group,Vmax and CLint values of scutellarin and paeoniflorin in liver microsomes of MCAO rats were significantly reduced(PPVmax of apigenin-7-O-glucronide in liver microsomes of MCAO rat was also significantly reduced(PConclusion: Metabolic rates of these three active components from Xinshao fomula in liver microsomes of MCAO rats with focal cerebral ischemia-reperfusion injury decrease with low elimination rate.

Absorption of Inula cappa extract based on everted intestinal sac method / 中国中药杂志

To investigate the absorptive characteristics of Inula cappa extract based on the rat everted intestinal sac method . Nine representative ingredients in I. cappa extract were selected as the study objects. An UPLC-MS/MS method was established to determine and detect their cumulative absorption amount for expounding the absorptive characteristics of ingredients in different intestinal sections. According to the results， the transport mechanism of 8 compounds showed passive diffusion by the reverted gut sac method. And scopolin was actively transported in the intestine. The best absorption site of chlorogenic acid was duodenum. The best absorption site of cryptochlorogenic acid， 1，3--dicaffeoylquinic acid， luteolin-7-glucoside and 3，4--dicaffeoylquinic acid were jejunum. The best absorption site of neochlorogenic acid， scopolin， 4，5--dicaffeoylquinic acid and 3，5--dicaffeoylquinic acid was ileum. The absorption of all the compounds was affected by pH and bile. All of the nine ingredients in I. cappa extract could be absorbed in intestines， but with differences in the absorption rate， the best absorptive site and mechanism， indicating that the intestinal absorption of I. cappa extract was selective.

Study on absorption activity of five components of Polygonum orientale L. Flower in Caco-2 cell monolayer / 中国药理学通报

Aim To observe the absorption activity of five components of Polygonum orientale L. Flower ex-tract in Caco-2 cell monolayer. Methods The effects of different concentrations, time, temperature, pH and P-glycoprotein inhibitors on Caco-2 cells were investi-gated by UPLC-MS/MS. Results The absorption of five components of Polygonum orientale L. Flower ex-tract presented a concentration-and time-dependent manner, and the uptake of quercetin was reduced in Caco-2 cells after 90 min. There was a highest intake at 37℃,and the uptake of four components was best in acid environment except for the quercetin at pH 6 , which was best at pH5 . The uptake of quercetin and kaempferol was significantly improved after the addition of P-glycoprotein inhibitors of verapamil. Conclusions The cellular uptake mechanisms of the five compo-nents of Polygonum orientale L. Flower extract is man-inly through passive diffusion. P-glycoprotein is in-volved in the uptake of quercetin and kaempferol.

Metabolism of Inula cappa extract by rat intestinal bacteria in vitro / 中国中药杂志

To investigate the metabolism of major components in Inula cappa by rat intestinal bacteria in vitro. I. cappa extract was incubated for 24 h with rat intestinal bacteria under anaerobic environment. After the samples were precipitated by n-butanol, UPLC-Q-TOF-MS/MS was applied for the qualitative analysis of the metabolites, combined with data software such as Metabolite Tools, Data Analysis and so on. The potential metabolites in rat intestinal bacteria were analyzed by comparing the total ion current of the test samples and blank samples and analyzing the quasi-molecular ion and fragment ion of all chromatograms. The results injected that fourteen metabolites were detected in rat intestinal flora. Various types of metabolic reactions happen to caffeoylquinic acid in intestinal flora, including isomerization, hydrolyzation, there were also methylation, hydrogenation and acetylation of caffeic acid. At the same time, a methylate of dicaffeoylquinic acid was also detected. Presumably, caffeoylquinic acids were gradually transformed into more hydrophobic metabolites with smaller molecular mass, which were better absorbed by the intestinal tract.

Advances on pharmacokinetics of traditional Chinese medicine under disease states / 中国中药杂志

In recent years, more and more research shows that the pharmacokinetic parameter of traditional Chinese medicine can be affected by the disease states. It's possible that drug metabolic enzymes, transporters, cell membrane permeability and the change of microbes group could be interfered with physiological and pathological changes, which enables the pharmacokinetics of traditional Chinese medicine in the body to be altered, including the process of absorption, distribution, metabolism and excretion, and then the pharmacokinetic parameters of traditional chinese medicine are altered. It's found that investigating the pharmacokinetic of traditional Chinese medicine in the pathological state is more useful than that of in normal state because the great part of traditional Chinese medicine is mainly used to treat disease. This article reflects the latest research on the pharmacokinetic of traditional Chinese medicine in the disease state such as diabete, cerebral ischemia, liver injury, inflammatory disease, nervous system disorders and fever in order to provide certain reference for clinicians designing reasonable administration dose.