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.

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.

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.

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.

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.

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.

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.

Research on bioactive ingredients in rat liver after oral administration of different combinations of Wuji pill / 中国中药杂志

A L9 (3(4)) orthogonal design table to be used to get nine combinations of extraction of three herbs of Wuji pill: Coptis chinensis, Tetradium ruticarpum and Paeonia lactiflora Pall., and nine extraction of single herbs correspondingly, altogether eighteen combinations. Quantification of five representative bioactive ingredients: berberine, palmatine, evodiamine, rutaecarpine, paeoniflorin in rat liver by ultra high liquid chromatography-tandem mass spectrometry after oral administration at 2 h time point of eighteen combinations. The result shows the bioactive ingredients have different concentrations betweem different combinations and the single herb with the same dosage significantly as well as the same dose combinations. C. chinensis with evodiamine concentration of low and high dose T. ruticarpum was positively correlated. T. ruticarpum with berberine concentration of low dose C. chinensis was negatively correlated and of meddle dose C. chinensis was correlated positively. T. ruticarpum with paeoniflorin concentration of middle dose P. lactiflora was correlated positively. P. lactiflora with palmatine concentration of middle dose C. chinensis was negatively correlated and with evodiamine and rutaecarpine concentration of middle dose T. ruticarpum was negatively correlated. These shows the three single herbs interactions resulted in the differences of each ingredients concentration in rat liver. The orthogonal analysis indicates the combination 12: 6: 6 make the maximum concentration in rat liver.

Antitumor effect of alcohol extracts from Stellera chamaejasme / 中国中药杂志

<p><b>OBJECTIVE</b>To screen the best antitumor components of Stellera chamaejasme and their sensitive cell lines.</p><p><b>METHOD</b>Sixteen different components of alcohol extracts from S. chamaejasme, including HH, H1-H8, JH and J1-J8, were got by gradient column chromatography eluted with alcohol in different concentrations. In the first screening, the solvent control group, the drug group, the positive group and the blank group were set up. Then the human cancer cell lines such as hepatocarcinoma BEL-7402, SK-HEP-1, and lung cancer A549, NCI-H157 were processed with the components, and the concentration for each drug group was 100 mg x L(-1). Thus, the 48 hour suppression ratio to the four kinds of cancer cells for each component were compared by the SRB method, to select the most inhibitive components and the most sensitive cell lines, which were used as the subjects of the second screening. In the second screening, each component including the concentration of 6.25, 12.5, 25, 50, 100 mg x L(-1) was used to treat the sensitive cell lines and the inhibition rates to each cell line of 24, 48, 72 h by the SRB assay were detected. Also, the IC50 of each component was calculated and their main chemical composition was analyzed by UPLC-MS.</p><p><b>RESULT</b>The inhibition effect to the proliferation of the different cancer cells has great difference among 16 components, and the lung cancer cells are more sensitive to them than the hepatocarcinoma cells. Besides, the inhibition rates of JS, J6 and H8 are higher than the other components and their effect has a certain time and concentration dependence. At 72 h, the inhibition rate of each component ranges from (60.57 +/- 3.83)% to (96.66 +/- 0.51)% for lung cancer cells, and IC50 from (9.61 +/- 0.79) mg x L(-1) to (55.76 +/- 2.31) mg x L(-1). J5, J6 and H8 are the biflavonoids.</p><p><b>CONCLUSION</b>The biflavonoids in alcohol extracts from S. chamaejasme have exerted a satisfactory inhibitory effect on the lung cancer cell proliferation.</p>

Study on metabolism of Coptis chinensis alkaloids from different compatibility of Wuji Wan in human intestinal flora / 中国中药杂志

<p><b>OBJECTIVE</b>To study the metabolism of berberine and palmatine in prescription compatibility of Wuji Wan in human intestinal flora.</p><p><b>METHOD</b>The L9 (3(4)) orthogonal design was adopted to compare prescription compatibility of nine groups of Wuji Wan composed of Coptis chinensis, Evodiae and fried Radix paeoniae alba into and single ingredient of C. chinensis. They were cultivated with fresh human excrements under anaerobic conditions for 24 h. A HPLC-UV method was adopted for determining berberine and palmatine in bacteria culture medium, in order to compare the metabolism of the two components in different prescription compatibility.</p><p><b>RESULT</b>Metabolism of berberine was positively correlated with doses, whereas metabolism of palmatine was negatively correlated with doses in extracts from C. chinensis. Compound compatibility speeded up the metabolism of berberine in low dose, which was positively related to the doses of Evodiae and fried Paeoniae Alba Radix; meanwhile Compound compatibility slowed down the metabolism of berberine in high dose, which was negatively related to the dose of Evodiae. Compound compatibility speeded up the metabolism of palmatine in high dose, which was negatively related to the doses of Evodiae and fried Paeoniae Alba Radix.</p><p><b>CONCLUSION</b>The metabolism of the compatibility of Wuji Wan speeds up, when Coptis chinensis components metabolite rapidly in intestinal flora; while the metabolism of the compatibility of Wuji Wan slows down, when C. chinensis components metabolite slowly in intestinal flora. Therefore, they show a balanced effect. Additionally, different proportion of C. chinensis, Evodiae and fried Paeoniae Alba Radix cause difference in metabolism speed of berberine and palmatine to some extent.</p>

Effect of Shenlian extracts on blood flow and vessel pathological changes in rabbits carotid atherosclerosis model induced by low shear stress / 中国中药杂志

Lipid accumulation in the vessel wall and tunica intima vasorum pathological changes are important factors in the development of atherosclerosis, which are closely related with hemodynamics. In this paper, we established a model of local low shear stress in rabbits using carotid artery cannula and a high cholesterol diet for 2 weeks, 4 weeks and 8 weeks. The effects of Shenlian extract on blood flow, vascular pathology formation and lipid metabolism were assessed by electromagnetic blood flow meter and hematoxylin-eosin staining of the proximal end in carotid artery at different times. The results demonstrate that the relationship between blood flow and shear stress for control, atorvastatin, Shenlian extract high-dose, Shenlian extract middle-dose, and Shenlian extract low-dose were linearly related. The blood flow and the shear stress of proximal end in carotid artery of Shenlian extract (1.12, 2.24, 4.48 g x kg(-1)), and atorvastatin (4.7 x 10(-4) g x kg(-1)) were significantly (P < 0.05)increased compared with the control. Plasma total cholesterol (TC), low density lipoprotein cholesterol (LDL-C) ,and high density lipoprotein cholesterol (HDL-C) were markedly decreased with the increasing of dose and time. This study is the first to prove that the inhibition of Shenlian extract on low shear stress (LSS) induces rabbits carotid atherosclerosis with increasing blood flow and decreasing lipids and vessel pathological changes.