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1.
Article in Chinese | WPRIM | ID: wpr-943095

ABSTRACT

ObjectiveTo analyze changes of the chemical composition in Euodiae Fructus before and after processing with Coptidis Rhizoma decoction, so as to provide scientific basis for elucidating the processing mechanism of this decoction pieces. MethodUltra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was performed on a Titank C18 column (2.1 mm×100 mm, 1.8 μm), the mobile phase was 0.1% formic acid aqueous solution-acetonitrile for gradient elution, the column temperature was set at 40 ℃, the flow rate was 0.25 mL·min-1. Electrospray ionization (ESI) was used to scan in positive and negative ion modes, and the scanning range was m/z 50-1 250. The chemical constituents in Euodiae Fructus were identified before and after processing by reference substance comparison, database matching and literature reference, and MarkerView™ 1.2.1 software was used to normalize the obtained data, SIMCA-P 14.1 software was employed to perform principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA) on MS data of raw and processed products to screen the differential components before and after processing. ResultA total of 50 compounds were identified, including 48 kinds of stir-fried products with Coptidis Rhizoma decoction and 44 kinds of raw products. After processing, six compounds were added, including danshensu, noroxyhydrastinine, oxyberberine, 13-methylberberrubine, protopine and canadine. However, two kinds of compounds, including (S)-7-hydroxysecorutaecarpine and wuchuyuamide Ⅱ, were not detected after processing. In general, after processing, the overall contents of phenolic acids and flavonoids decreased significantly, the overall content of limonoids increased, and the overall content of alkaloids did not decrease insignificantly. The results of PCA and OPLS-DA showed that there were significant differences in the composition and content of the chemical components of Euodiae Fructus before and after processing, and a total of 12 variables such as quercetin, dihydrorutaecarpine and dehydroevodiamine were obtained by screening. ConclusionEuodiae Fructus stir-fried with Coptidis Rhizoma decoction mainly contains phenolic acids, flavonoids, limonoids and alkaloids. The composition and content of the chemical components have some changes before and after processing. The addition of processing excipients and hot water immersion are the main reasons for the difference, which can provide experimental basis for interpretation of the processing mechanism of this characteristic processed products of Euodiae Fructus.

2.
Article in Chinese | WPRIM | ID: wpr-940842

ABSTRACT

ObjectiveTo explore the application law of compound prescriptions containing Coptidis Rhizoma to diabetes and its complications based on data mining. MethodA total of 288 records on formulas containing Coptidis Rhizoma in the treatment of diabetes and its complications and the corresponding syndromes and symptoms were retrieved from the medical records of modern physicians, with 218 on the treatment of diabetes and 70 on the treatment of diabetes complications. The Traditional Chinese Medicine Inheritance Computing Platform (V3.0) was used or data mining on the compositions of the formulas. Moreover, it was employed for the frequency statistics, formula analysis, symptom analysis, association rules analysis, network visualization, and cluster analysis. ResultThe 218 formulas containing Coptidis Rhizoma for the treatment of diabetes involved 190 Chinese medicinals. A total of 12 syndromes showed the occurrence frequency ≥ 6, and the one with the highest frequency was deficiency of both qi and yin, followed by the syndrome of excessive heat in lung and stomach, syndrome of Yin deficiency and effulgent fire, and syndrome of excessive heat and fluid consumption. The dose of Coptidis Rhizoma for the treatment of diabetes ranged from 1.5-30 g, and the most frequently used doses were 10, 6, and 5 g. The medicinal was frequently applied for the traditional Chinese medicine symptoms of dry stool, dry mouth and tongue, and swift digestion with rapid hungering. Moreover, 26 core medicinal pairs, 17 association rules, 3 diagrams on medicinal relationship, and 3 core combinations were yielded. The 70 formulas containing Coptidis Rhizoma for the treatment of diabetes complications involved 184 Chinese medicinals, and the top 3 complications were diabetic nephropathy, diabetic peripheral neuropathy, and diabetic gastroenteropathy. The dose of Coptidis Rhizoma in the treatment of diabetes complications fell in the range of 2-15 g, and 10, 6, and 5 g were most frequently used. ConclusionFormulas containing Coptidis Rhizoma for the treatment of diabetes and its complications mainly target the syndrome of dampness-heat transforming into fire and the syndrome of excessive heat damaging yin. This study can serve as a reference for standard use of Coptidis Rhizoma in the prevention and treatment of diabetes and its complications.

3.
Article in Chinese | WPRIM | ID: wpr-940691

ABSTRACT

Zuojinwan originated from Danxi′s Experiential Therapy (《丹溪心法》) in the Yuan dynasty. It is a representative prescription for the treatment of liver fire invading stomach syndrome, and is also one of the typical prescriptions of the anti-adjuvant method of traditional Chinese medicine (TCM). In this paper, the method of bibliometrics was used to systematically sort out the ancient books of Zuojinwan, and 729 relevant literature data were obtained. After certain retrieval and screening, 57 ancient books of TCM were finally obtained. The statistics and analysis were carried out from the aspects of prescription source, historical evolution, composition, functions, evolution of prescription meaning, prescription dose, and preparation and usage of Zuojinwan. It was found that Zuojinwan was composed of Coptis chinensis rhizoma and Euodia rutaecarpa fructus in a ratio of 6∶1. It was mainly used for the treatment of liver fire invading stomach syndrome. The symptoms included pain in chest and hypochondrium, vomiting and bitter mouth, noisy acid-swallowing, red tongue coating yellow, and pulse string number. Later medical records recorded that Zuojinwan was mostly consistent with the original prescription. It mainly treated various diseases caused by liver fire, including left by liver fire, including left hypochondriac pain, swallowing acid and vomiting acid, tendon hernia and lump, epigastric pain, bitter mouth pulse string, head pain, diarrhea, gonorrhea, cold and hot, abdominal pain, alcohol wet yellowing, silence of oral dysentery and so on. There was little controversy in the analysis of relevant prescriptions. In the past dynasties, pills was mainly used, which was consistent with the original prescription. In modern times, it is mainly water flooding for pills or steamed cakes for pills, warm boiling water to serve 6 g, taking 2-3 g per time, the history is basically the same. In this paper, through the excavation, collation and systematic analysis of the ancient literature of TCM that recorded Zuojinwan, we hope to provide the literature basis for the development, inheritance and utilization of this famous classical formulas.

4.
Article in Chinese | WPRIM | ID: wpr-940661

ABSTRACT

ObjectiveTo investigate the synergistic effect of Coptidis Rhizoma crude polysaccharide (CCP) and berberine (BBR) in treating ulcerative colitis (UC) model mice. MethodThirty male BALB/c mice were randomized into five groups. Except the 6 mice in the normal group, the rest were given 5% dextran sodium sulfate in their daily drinking water to establish the UC model. After modeling, the mice were administrated with corresponding agents by gavage once daily for 4 days: BBR (100 mg·kg-1) group, BBR (100 mg·kg-1) + low-dose (22.8 mg·kg-1) CCP group, BBR (100 mg·kg-1) + high-dose (45.6 mg·kg-1) CCP group. The mice in the model group and normal group were administrated with the same volume of normal saline. At the end of the experiment, the mice were sacrificed for the collection of colon, and the expression of tight junction proteins zonula occluden-1 (ZO-1), Claudin-1, and Occludin in colon tissue was detected by Western blot. With the normal group as the control, the disease activity index (DAI) score, colon length, colon histomorphology, and expression levels of tight junction proteins in other groups were evaluated. ResultCompared with the normal group, the modeling down-regulated the protein levels of ZO-1, Claudin-1, and Occludin (P<0.01). Compared with the model group, BBR did not significantly change the protein level of Claudin-1 and up-regulated those of ZO-1 and occludin (P<0.01). The expression levels of Claudin-1, ZO-1, and Occludin were up-regulated in BBR + CCP groups (P<0.01). The expression levels of tight junction proteins in BBR + CCP groups were significantly higher than those in the BBR group (P<0.05). ConclusionThe administration of CCP combined with BBR can effectively ameliorate intestinal mucosal barrier damage in the mice with UC.

5.
Article in Chinese | WPRIM | ID: wpr-940578

ABSTRACT

Herb pair, a common form of compounding in Chinese medicinal prescriptions, reflects the experience of pharmacists in clinical medication in the past. It is characterized by simple composition while has the basic characteristics of Chinese medicine compounding. The combination of two medicinal herbs can enhance effect or reduce toxicity. Coptidis Rhizoma (CR) has the effects of clearing heat, drying dampness, purging fire, and removing toxin. Euodiae Fructus (EF) is acrid, bitter, and hot-natured, which can not only warm the Yang Qi in spleen and stomach to dissipate cold and relieve pain, but also descend stomach Qi and prevent vomiting. Furthermore, it can warm the liver and kidney. CR and EF form a typical cold-heat herb pair, which oppose and yet also complement each other. Specifically, their cold and heat natures interact with each other to clear liver fire, harmonize stomach for descending adverse Qi, relieve depression, and dissipate mass. CR clears the intestine and stops dysentery, while EF warms the middle and promotes the circulation of Qi. The combination of them can thus clear heat, dry dampness, and relieve pain. Modern pharmacological studies have demonstrated that CR-EF has not only significant efficacy against digestive system diseases but also good anti-cancer, anti-inflammatory, anti-ulcer, and lipid-lowering activities. Therefore, the article summarized the effect enhancement and toxicity reduction of the herb pair at the levels of cellular molecule, isolated organ, and whole animal, and clarified the mechanism of its pharmacological action. It will provide a theoretical basis for further development and clinical use of the herb pair.

6.
Article in Chinese | WPRIM | ID: wpr-940337

ABSTRACT

Through the combing of ancient books of Chinese herbal medicine in the past dynasties, a textual research of Coptidis Rhizoma involved the name, origin, medicinal parts, producing area, quality evaluation, harvesting and processing methods in famous classical formulas was conducted in this paper. After textual research, the mainstream varieties of Coptidis Rhizoma in the Ranunculaceae family before Tang and Song dynasties were Coptis chinensis and C. chinensis var. brevisepala, after the Ming and Qing dynasties, C. deltoidea, C. teeta and C. omeiensis were gradually praised. In ancient times, the authentic producing area of Coptidis Rhizoma has the characteristics of gradually moving to the west. The eastern Coptidis Rhizoma was highly praised in the early stage, while in the later stage, western Coptidis Rhizoma like chicken feet was highly praised. In the early stage, western Coptidis Rhizoma probably originated from C. chinensis and its genus, while Coptidis Rhizoma like chicken feet was cultivated, and no wild species has been found so far. As Coptidis Rhizoma has mixed use of multiple origins in ancient books of past dynasties, based on the current shortage of market resources in C. teeta and C. deltoidea, there are also endangered and protected plants of C. chinensis var. brevisepala and C. omeiensis, combined with the mainstream medicines and resources of past generations, it is recommended to choose C. chinensis as the base of the formulas. In ancient times, there were many processing methods for Coptidis Rhizoma, such as frying and wine-, ginger-, honey-processed. In the process of developing famous classical formulas, the appropriate processing specifications of Coptidis Rhizoma should be selected based on the original source records and the requirements of the medicinal material.

7.
Article in Chinese | WPRIM | ID: wpr-887942

ABSTRACT

Coptidis Rhizoma, as a bulk medicinal material, is in great demand in clinical practice. Its quality is uneven in the market due to the mixture of genuine, counterfeit and adulterants. Therefore, it is particularly important to establish a quality control system for Coptidis Rhizoma. Based on the concept of Chinese medicine quality marker(Q-marker), the potential quality markers of Coptidis Rhizoma were analyzed and predicted from the perspective of chemistry and pharmacology. The sources of the Q-markers of Coptidis Rhizoma were identified by literature retrieval. The potential Q-markers were then screened through the visualization of the "components-targets-pathways" network. High performance liquid chromatography(HPLC) was used to establish a multi-indicator qualitative and quantitative control method featuring fingerprints for 10 batches of Coptidis Rhizoma. A supervised mode of orthogonality partial least squares method-discriminant analysis(OPLS-DA) was used to screen the main marker components that caused differences between groups. The literature review results showed that the alkaloids were the main source of Coptidis Rhizoma Q-markers.The fingerprints of 13 common peaks were successfully established, and berberine, palmatine, berberine and epiberberine were selected as Q-markers of Coptidis Rhizoma, and their contents were determined.Based on the concept of the Q-marker of traditional Chinese medicine, the four components can be selected as the Q-marker of Coptidis Rhizoma after comprehensive consideration. The results of this study are not only conducive to the quality evaluation of Coptidis Rhizoma on the market, but also provide a reference for the overall quality control of Coptidis Rhizoma and lay foundation for the future exploration of the mechanism of Coptidis Rhizoma.


Subject(s)
Alkaloids , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Multivariate Analysis , Rhizome
8.
Article in Chinese | WPRIM | ID: wpr-873203

ABSTRACT

Objective:Based on UPLC-Q-Orbitrap HRMS and network pharmacology, the material basis, processing principle and molecular mechanism of bile processed Coptidis Rhizoma (BPRC) for reducing excess fire of liver and gallbladder were elucidated.Method:The chemical ingredients of BPRC were analyzed by UPLC-Q-Orbitrap HRMS. Chromatographic separation was achieved with 0.1% formic acid solution (A)-acetonitrile (B) as the mobile phase in gradient elution (0-20 min, 5%-80%B; 20-30 min, 80%-95%B; 30-30.1 min, 95%-5%B; 30.1-35 min, 95%-5%B). The flow rate was 0.2 mL·min-1, electrospray ionization (ESI) was applied and operated in positive and negative ion modes, the acquisition range was m/z 100-1 500. Based on the clinical manifestations and pathogenic factors of excess fire of liver and gallbladder, the potential effective ingredients, targets and functional characteristics of BPRC were predicted and analyzed by online database. Based on the characteristics of the new active ingredients after processing, the processing principle of BPRC was investigated by network pharmacology.Result:A total of 19 ingredients in BPRC were identified, six of which were newly added cholic acids after processing. It was determined that the alkaloids, including worenine, epiberberine, jatrorrhizine, coptisine, berberrubine, berberine, palmatine and cholic acids, including glycohyodeoxycholic acid, taurohyodeoxycholic acid, glycochenodeoxycholic acid, hyodeoxycholic acid and taurochenodeoxycholic acid, were identified as material basis of BPRC. A total of 66 targets of reducing excess fire of liver and gallbladder of BPRC were screened. There were 16 common targets and multiple same signaling pathways between cholic acids and alkaloids of BPRC, and many lesions of excess fire of liver and gallbladder were target organs of cholic acids. By acting on some targets, including albumin (ALB), Caspase-3 (CASP3), mitogen-activated protein kinase 14 (MAPK14), glucocorticoid receptor (NR3C1) and other targets and some signaling pathways, including interleukin (IL)-17, phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt), MAPK and other pathways, BPRC could reduce excess fire of liver and gallbladder.Conclusion:BPRC has the characteristics of multi-component, multi-target and multi-pathway on reducing excess fire of liver and gallbladder. Bile and Coptidis Rhizoma have synergistic effect and bile can enhance the intensity of BPRC in lesions, which confirms the processing theory that the effect of BPRC on excess fire of liver and gallbladder enhance after being processed by bile.

9.
Article in Chinese | WPRIM | ID: wpr-873117

ABSTRACT

Coptidis Rhizoma-Evodia Fructus is a classic herb pair in traditional Chinese medicine prescriptions, the famous prescription is called Zuojinwan, which comes from Danxi Xinfa, is composed of Coptidis Rhizoma-Evodia Fructus (6∶1). In this formula, Coptidis Rhizoma has the effect of clearing heat and drying diuresis, purging fire to remove toxin and clearing heart. Evodia Fructus has the effects of expelling cold and alleviating pain, checking upward adverse flow of Qi tostop vomiting, and assisting yang to stop diarrhea. Coptidis Rhizoma has the properties of bitter and cold, and Evodia Fructus has the properties of pungent and calidus. Pungent drugs have divergent effects, and bitter drugs have sedimentation effect, when used in combination, they can clear the liver and purge fire, calm the adverse-rising energy and stop vomiting. On the basis of Zuojinwan, Coptidis Rhizoma-Evodia Fructus medicine has derived different compatibility ratios. Different ratios are different in terms of efficacy, usage, clinical application. Although with the application of modern analytical instruments and the development of molecular pharmacology theory, the chemical constituents and Pharmacological effects of Coptidis Rhizoma and Evodia Fructus have been fully studied, as to the principle of compatibility, and the study of pharmacological effects and chemical constituents after the compatibility of the two drugs in different proportions, there is still no comprehensive system summary. This article makes a systematic and comprehensive explanation of Coptidis Rhizoma-Evodia Fructus from the aspects of famous literature, chemical composition, pharmacological effects and clinical applicationthrough querying literature and ancient books. In order to make this herb pair more standardized, and provide reference materials for further research and development for this herb pair.

10.
Article in Chinese | WPRIM | ID: wpr-873088

ABSTRACT

Objective::To observe the effect of berberine and 6-shogaol, main components of Coptiae Rhizoma and Zingiberis Rhizoma, on the inflammatory signaling pathway of Toll-like receptors 4 (TLR4)/nuclear factor kappa B (NF-κB) in colonic epithelial cells of mice with ulcerative colitis. Method::Fifty Kunming mice were randomly divided into normal group, model group, berberine group (100 mg·kg-1), 6-shogaol group (100 mg·kg-1), and 6-shogaol combined with berberine group (200 mg·kg-1), with 10 mice in each group. A mouse model of ulcerative colitis was established through oral administration with 2% dextroan sulfate for two weeks. Each group was given corresponding drugs by gavage, while normal group and model group were given equal amount of normal saline. Serum and colon tissue samples were taken 20 days after administration. Enzyme-linked immunosorbent method was used to detect serum interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α) expressions, and real-time fluorescence quantitative polymerase chain reaction(Real-time PCR) and Western blot method were used to detect TLR4, NF-κB p65 mRNA and protein expressions in colon epithelial tissue. Result::Compared with the normal group, relative expressions of TLR4 and NF-κB p65 mRNA and protein were increased in the model group (P<0.01), and the contents of serum IL-1β and TNF-α were increased (P<0.01). Compared with the model group, relative expressions of TLR4 and NF-κB p65 mRNA and protein were significantly decreased in 6-shogaol group, berberine group and 6-shogaol combined with berberine group (P<0.01), and the contents of serum IL-1β and TNF-α were significantly decreased (P<0.01). Among the three groups, 6-shogaol combined with berberine group had the strongest effect (P<0.01). Conclusion::Both 6-shogaol and berberine can inhibit colonic inflammation, reduce inflammatory damage and treat ulcerative colitis. The combined application of 6-shogaol and berberine has a significant synergism effect. The mechanism is related to the excessive activation of TLR4/NF-κB pathway and the regulation of non-controllable intestinal inflammation.

11.
Article in Chinese | WPRIM | ID: wpr-872702

ABSTRACT

Objective:To study the protective effect of different doses of single-flavored Coptis, Magnoliae Officinalis Cortex, and their compatibility on ulcerative colitis (UC) model rats and the colonic B lymphoblastoma-2 associated X protein (Bax) and cysteine-containing aspartame-3(Caspase-3) protein, inflammatory cytokines, and other expressions. Method:The 120 healthy adult SD rats were randomly divided into blank group, model group, sulfasalazine group, Coptidis Rhizoma 2.00, 1.00, 0.50 g·kg-1 group, Magnoliae Officinalis Cortex 2.00, 1.00, 0.50 g·kg-1 group, Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 4.00, 2.00, 1.00 g·kg-1 group, 12 groups with 10 rats in each group. The UC model was prepared by 2,4, 6-trinitrobenzene sulfonic acid/ethanol (TNBS/ethanol). After 24 h of modeling, the rats were gavaged at 10 mL·kg-1 for one time/d. After modeling, the mental state, activity state, hair luster, stool characteristics, and blood in the stool of each group were observed. After continuous administration for 6 days, colon tissues and spleen were taken after the last administration for 24 h. The ratio of colonic weight to length and spleen index was calculated. The degree of colonic injury was evaluated according to the colonic mucosal injury index (CMDI) score criteria. the histopathological observation was performed using hematoxylin-eosin staining (HE). The expression levels of tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), interleukin-10 (IL-10), and myeloperoxidase (MPO) in the serum of Coptidis Rhizoma 2.00 g·kg-1 group, Magnoliae Officinalis Cortex 2.00 g·kg-1 group, Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 4.00 g·kg-1 were detected by enzyme-linked immunosorbent assay(ELISA) in blank group and model group. Western blot was used to detect the expression of Bax and Caspase-3 proteins in the colon of rats. Result:Compared with blank group, rats in model group were sluggish and less active. The colon weight-length ratio, spleen index, CMDI, and colon tissue pathological damage increased significantly, and the expression of serum TNF-α, IL-6, and MPO increased significantly. Serum IL-10 expression levels were extremely significantly reduced (P<0.01). Compared with model group, the sulfasalazine group, the Coptidis Rhizoma 2.00, 1.00 g·kg-1 group, the Magnoliae Officinalis Cortex 2.00 g·kg-1 group, and the three-dose groups of Coptidis Rhizoma combine with Magnoliae Officinalis Cortex, their colon weight-length ratio and CMDI were significantly reduced (P<0.05,P<0.01). The colon weight length ratio and CMDI index of the Coptidis Rhizoma 0.50 g·kg-1 group, Magnoliae Officinalis Cortex 0.50 and 1.00 g·kg-1 group were not significantly different from the model group but compared with Coptidis Rhizoma and Magnolia 0.50 g·kg-1 group, the ratio of colon weight to length in the group of Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 1.00 g·kg-1 group was significantly reduced (P<0.01). Compared with model group, the spleen index of the sulfasalazine group, the Coptidis Rhizoma 2.00 g·kg-1, and the Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 4.00 g·kg-1 group were significantly lower (P<0.05), compared with model group, the sulfasalazine group, Coptidis Rhizoma 2.00, 1.00 g·kg-1 and Magnoliae Officinalis Cortex 2.00 g·kg-1, thre dose groups of Coptidis Rhizoma combine with Magnoliae Officinalis Cortex can significantly improve the depth and scope of histopathological damage and tissue necrosis. Compared with the model group, the preferred Coptidis Rhizoma 2.00 g·kg-1 group, Magnoliae Officinalis Cortex 2.00 g·kg-1 group, Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 4.00 g·kg-1 group serum TNF-α, IL-6, MPO expression levels are extremely significantly reduced, the level of IL-10 increased significantly (P<0.01).Compared with blank group, the expression of  Bax and Caspase-3 protein in the colon of model group was significantly increased (P<0.01). Compared with model group, the expression of Bax and Caspase-3 protein in preferred Coptidis Rhizoma 2.00 g·kg-1 group and Magnoliae Officinalis Cortex 2.00 g·kg-1 group, Coptidis Rhizoma combine with Magnoliae Officinalis Cortex 4.00 g·kg-1 group were significantly reduced (P<0.01). Conclusion:The compatibility of single-flavored Coptidis Rhizoma, Magnoliae Officinalis Cortex, and Coptidis Rhizoma combine with Magnoliae Officinalis Cortex may improve the pathology of UC model rats induced by TNBS/ethanol by down-regulating the expression of Bax and Caspase-3 protein, inhibiting the release of inflammatory cytokines and promoting the release of anti-inflammatory factors injury, it plays a role in protecting colonic mucosa. The compatibility effect of Coptidis Rhizoma and Magnoliae Officinalis Cortex is better than that of single medicine, and Coptidis Rhizoma has a tendency to be better than Magnoliae Officinalis Cortex.

12.
Article in Chinese | WPRIM | ID: wpr-862679

ABSTRACT

Objective::To identify the main active components of Coptidis Rhizoma and Euodiae Fructus for the treatment of gastric cancer, predict the targets of the common active components in these two herbs, establish the network of active drug components-target genes, and further explore the potential mechanism and effect of Coptidis Rhizoma-Euodiae Fructus for the treatment of gastric cancer. Method::The active components of Coptidis Rhizoma-Euodiae Fructus were screened by Traditional Chinese Medicine Systems Pharmacology Database (TCMSP), gastric cancer targets were predicted and screened by Genecard database platform, " drug-active ingredient-disease-targets" networks were built by Cytoscape (3.7.1) software, and protein interaction networks were built by String database platform. Finally, Gene Ontology (GO) analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis were performed by using Bioconductor platform and R language. Result::The 14 potential active components of Coptidis Rhizoma and 15 potential active components of Euodiae Fructus were obtained, involving 127 targets related to gastric cancer. There were 33 common targets for Coptidis Rhizoma-Euodiae Fructus-gastric cancer, which played a therapeutic role in gastric cancer mainly by regulating target genes such as PTGS2, PTGS1, AR, RXRA and NOS2, as well as cell apoptosis, p53 signaling pathway and interleukin (IL)-17 signaling pathway. Conclusion::The therapeutic mechanism of Coptidis Rhizoma-Euodiae Fructus reflects the multi-component, multi-target and multi-pathway characteristics of traditional Chinese medicines and provides the scientific basis for further study and the material basis of Coptidis Rhizoma-Euodiae Fructus against gastric cancer.

13.
China Pharmacy ; (12): 2853-2857, 2020.
Article in Chinese | WPRIM | ID: wpr-837538

ABSTRACT

OBJECTIVE:To provide refere nce f or the quality control and evaluation of rice-wine processed Coptidis Rhizoma decoction piece. METHODS :Taking 17 batches of rice-wine processed Coptidis Rhizoma decoction piece from different manufacturers as samples ,HPLC method was adopted to determine the contents of 4 kinds of alkaloids as epiberberine ,coptisine, palmatine and berberine. The compound weights of epiberberine ,berberine,palmatine and berberine were calculated by the subjective and objective combination weighting method (AHP combined with variation coefficient ). Then the quality evaluation method was used to evaluate the quality of decoction pieces combined with the appearance of decoction pieces and the contents of 4 alkaloids. The percent mass constant was calculated and the grade of rice-wine processed Coptidis Rhizoma decoction piece was classified. RESULTS :According to the results of content determination of 4 kinds of alkaloids ,among 17 batches of samples ,a total of 13 batches of samples met the requirements of 2015 edition of Chinese Pharmacopoeia (part Ⅳ). Mass constants of 13 batches of qualified samples were 10.03-26.96,and the percent mass constants were 37.20%-100%. If the percent mass constant ≥ 80% of the sample was listed as the first-class product ,the sample with the percent mass constant between 50%-<80% was classified as the second-class product ,and the rest was listed as the third-class product ,therefore the quality constant of first-class product was ≥21.57,that of second-class product was 13.48-<21.57,and that of third-class product was <13.48. According to the grading standard ,3 batches of 13 batches of qualified samples are classified as first-class products ,6 batches are classified as second-class products ,4 batches are classified as third-class products. CONCLUSIONS :The established subjective and objective combination weighting method and quality constant method can more scientifically and reasonably classify rice-wine processed Coptidis Rhizoma decoction piece.

14.
Article in Chinese | WPRIM | ID: wpr-828006

ABSTRACT

Inhibition of bitterness is a significant measure to improve the compliance and clinical efficacy of traditional Chinese medicine(TCM) decoction. According to the characteristics of TCM decoction, such as high dispersion of bitterness components, multi-component bitterness superposition and strong instantaneous stimulation, the research group put forward a new strategy to inhibit bitterness in the early stage based on the self-assembly characteristics of amphiphilic substances in aqueous solution, in order to reduce the distribution of bitterness components in real solution and achieve the purpose of bitter-masking. It was found that the bitter-masking effect of amphiphilic substances was different on the bitter compounds of various structures. Therefore, it was speculated that there might be a certain relationship between the bitter inhibition effect and the substrate structure. In this paper, the interaction between mPEG-PLLA and five bitter alkaloids(bamatine, jatrorrhizine, berberine, epiberberine and coptisine) in Coptidis Rhizoma was studied to explore the effect of substrate structure on the inhibition of bitterness. The sensory test of volunteers was used to determine the bitter-masking effect of mPEG-PLLA on the decoction of Coptidis Rhizoma and its main bitter alkaloids. The molecular docking and molecular force field were applied to locate the bitter groups and the bitter-masking parts. The relationship between the bitter strength and the structure was analyzed by the surface electrostatic potential of the bitter alkaloids, and the correlation between the bitter-masking effect and the structural parameters of the bitter components was explored by factor analysis, so as to clarify the structure-activity relationship of mPEG-PLLA in masking the bitterness of coptis alkaloids. It was found that mPEG-PLLA had significant taste masking effect on the decoction of Coptidis Rhizoma and five alkaloids. The masking effect was obviously related to the structure of different alkaloids: the effect increased with the increase of the number of hydrogen donors, rotatable bonds, molecular weight, and hydrophobicity, and decreased with the increase of surface electrostatic potential, electrophilicity and binding energy with bitter receptors. In this study, the influence of alkaloid structure of Coptidis Rhizoma on the butter-masking effect of mPEG-PLLA was preliminarily elucidated, providing a scientific basis for better exerting the bitter-masking effect of amphiphilic block copolymers.


Subject(s)
Alkaloids , Coptis , Drugs, Chinese Herbal , Humans , Molecular Docking Simulation , Structure-Activity Relationship , Taste
15.
Article in Chinese | WPRIM | ID: wpr-846698

ABSTRACT

Objective: To clarify the characteristics of drug pair of Coptidis Rhizoma-Euodiae Fructus on multi-components, multi-targets and multi-pathways based on the network pharmacology, and provide a theoretical reference for further study on the pharmacodynamic basis and mechanism of Coptidis Rhizoma-Euodiae Fructus against cancer and cardio-cerebrovascular diseases. Methods: Through the Traditional Chinese Medicine Systems Pharmacology (TCMSP) database, the parameters of oral bioavailability (OB ≥ 30%) and drug-likeness (DL ≥ 0.18) combined with the biological function, contents, research hotspot and other factors were used to screen out the active ingredients of the medicine pair of Coptidis Rhizoma - Euodiae Fructus. DrugBank and TCMSP databases were used to predict and analyze the targets, and Uniprot database was used to sort out all relevant genes affecting the targets. Combining the KEGG database for GO analysis and pathway analysis, "ingredients-targets-related diseases" network was constructed using Cytoscape software. Results: A total of 41 compounds and 212 potential target genes, as well as 44 signaling pathways were obtained after screening from Coptidis Rhizoma-Euodiae Fructus, and there were 44 major signaling pathways involved in 30 pathways related to cancer, seven pathways which were related to cardio-cerebrovascular diseases, seven pathways which were related to cancer and cardio-cerebrovascular diseases. Conclusion: The active ingredients of Coptidis Rhizoma-Euodiae Fructus can up-regulate the expression of cancer apoptosis genes through multi-components, multi-targets and multi-pathways, down-regulate the expression of cell cycle and apoptosis-related genes, and produce anti-cancer effect; Protecting vascular cells by inhibiting vascular calcification, and to achieve the effect of treating cardio-cerebrovascular diseases by inhibiting apoptosis and proliferation.

16.
Article in Chinese | WPRIM | ID: wpr-846106

ABSTRACT

Objective: HPLC fingerprints of Banxia Xiexin Decoction (BXD) was established to analyze the quality value transmitting relationship between medical herbs-decoction pieces-whole decoction of Scutellariae Radix (SR) and Coptidis Rhizoma (CR). Methods: BXD was prepared by the decoction method recorded in Treatise on Febrile Diseases. BXD HPLC fingerprints was established, and the characteristic peaks were analyzed; The transfer rate, the dry extract rate and the similarity of fingerprint were used as indicators to analyze the quality value transmitting relationship between medical herbs-decoction pieces-whole decoction of SR and CR. Results: The transfer rate of baicalin from medical herbs to decoction pieces was between 81.08% and 119.82%; The transfer rate of baicalin from decoction pieces to BXD was between 44.55% and 59.05%; The transfer rate of berberine from medical herbs to decoction pieces was between 66.65% and 97.51%; The transfer rate of berberine from decoction pieces to BXD was between 7.83% and 22.93%; And the dry extract rate of the whole decoction was between 12.99% and 17.21%. The similarity of fingerprints of 15 batches of BXD ranged from 0.978 to 0.999. Conclusion: The quality evaluation method established by the fingerprint is applicable to the quality control of medical herbs-decoction pieces-whole decoction of SR and CR, which provides some reference for the establishment of the quality evaluation method of famous classic formula.

17.
Article in Chinese | WPRIM | ID: wpr-801999

ABSTRACT

Objective: To observe the effect of Coptidis Rhizoma on blood sugar, inflammatory factors and protein kinase R-like endoplasmic reticulum kinase (PERK)/activating transcription factor 4(ATF4)/CCAAT/enhace-binding protein homologous protein (CHOP) pathway in type 2 diabetic mellitus rats. Method: The 80 SPF grade male rats were randomly divided into normal group, model group,metformin hydrochloride group, Coptidis Rhizoma group,with 20 rats in each group.The rats in the abnormal group were given "10-week high-sugar and high-fat diet+intraperitoneal injection of low dose streptozotocin (STZ)" regimen. Metformin hydrochloride group was given 0.2 g·kg-1·d-1, while rhizoma coptidis group was given 0.4 g·kg-1·d-1. Both model group and normal group were given the same amount of distilled water once a day.Fasting blood glucose (FBG),C reactive protein (CRP) and tumor necrosis factor-α (TNF-α) at an acute stage after 5-week intervention were determined by enzyme linked immunosorbent assay (ELISA) methods. Immunohistochemistry method was perforined with proteins glucoseregulated protein 78 (GRP78),ATF4,CHOP.Western blot assay was used to detect PERK,phosphorylated PKR like endoplasmic reticulum regulating kinase(p-PERK). Result: Compared with normal group,the FBG,CRP,TNF-α,p-PERK,GRP78,ATF4 and CHOP of model group improved(Pα,p-PERK,GRP78,ATF4,CHOP in contrast with model group(PConclusion: Coptidis Rhizoma can reduce blood sugar and reduce the levels of inflammatory factors,inhibit plasmic reticulum stress PERK/ATF4/CH0P pathway, and reduce CHOP, ATF4, GRP78, p-PERK expression in rats.

18.
Article in Chinese | WPRIM | ID: wpr-801830

ABSTRACT

Objective: To screen the best compatibility proportion of total alkaloids of Coptidis Rhizoma and Notoginseng Radix et Rhizoma total saponins (HS composition)by uniform design and pharmacological model and to observe the effect on diabetic complications. Method: The total alkaloids of Coptidis Rhizoma and Notoginseng Radix et Rhizoma total saponins were used as the research objects, U6(62) table was choosed for grouping design.The content of triglyceride fasting blood-glucose (FBG), prothrombin time (PT) and active partial thromboplastin time (APTT) was chosen as index. The best dose ratio was obtained by multipleregression analysis. Rats with type 2 diabetes mellitus induced by high-fat diet combined streptozotocin were divided into blank group, model group, metformin group (150 mg·kg-1), HS composition group (total alkaloids of Coptidis Rhizoma 360 mg·kg-1+ Notoginseng Radix et Rhizoma total saponins 40 mg·kg-1). Rats were administered orally for 10 weeks.By observing the blood glucose, glucose tolerance,area under the curve (AUC), triglyceride (TG), high-density lipoprotein (HDL-C)and low-density lipoprotein (LDL-C), hemorheological indexes and pathological changes of pancreas, heart, kidney and retina in rats of each group, the effect of this composition on diabetic complications was verified. Result: Combination of 625 mg·kg-1 total alkaloids of Coptidis Rhizoma and 60 mg·kg-1 Notoginseng Radix et Rhizoma total saponins was the optimal dosage ratio of HS composition.The validation test showed that compared with blank group, the fasting blood glucose and lipid levels in the model group were significantly increased (PPPPPPPPPPPConclusion: The optimum compatibility dose of HS composition have a good therapeutic effect on diabetic complication rats induced by high-fat diet and streptozotocin.

19.
Article in Chinese | WPRIM | ID: wpr-801804

ABSTRACT

Objective: To investigate the effect of Coptidis Rhizoma on intestinal microflora of normal and type 2 diabetic rats before and after being steamed with rice wine based on 16S rRNA sequencing technology. Method: The type 2 diabetic rat model was established by high-fat diet and streptozotocin. Normal and model rats were given the decoction of Coptidis Rhizoma or Coptidis Rhizoma steamed with rice wine every day (0.8 g·kg-1, according to raw drug quantity), the positive drug group was given metformin solution every day (0.25 g·kg-1), continuous administration for 30 d. Blood glucose was measured once a week and oral glucose tolerance was measured on the 27th day of administration. On the 30th day, feces were taken and the rats were anesthetized. Blood was taken for enzyme linked immunosorbent assay (ELISA). Colon was dissected for hematoxylin-eosin (HE) staining. Based on 16S rRNA gene sequencing technology, the alpha diversity, beta diversity, abundance and composition, and the correlation with anti-inflammatory and antioxidant activities of intestinal microflora were comprehensively analyzed and evaluated. Result: After giving normal rats Coptidis Rhizoma or Coptidis Rhizoma steamed with rice wine, there were some inflammatory reactions, imbalance of oxidation-antioxidant system, pathological damage of colon and changes of intestinal microflora, which showed some toxic and side effects, but the toxic and side effects of Coptidis Rhizoma steamed with rice wine were lower than those of Coptidis Rhizoma. Coptidis Rhizoma could reduce fasting blood glucose and improve glucose tolerance in type 2 diabetic rats before and after steaming. Although the effect of Coptidis Rhizoma steamed with rice wine had an increasing trend, there was no significant difference between before and after processing. Type 2 diabetic rats appeared mild inflammation and imbalance of oxidation-antioxidant system, characterized by significant increase of contents of interleukin (IL)-6, nuclear transcription factor (NF)-κB and malondialdehyde (MDA) (PPPConclusion: Coptidis Rhizoma can treat type 2 diabetic rats by regulating intestinal microflora before and after steaming with rice wine, and the effect of Coptidis Rhizoma steamed with rice wine is better. The toxic and side effects of Coptidis Rhizoma on intestinal flora are reduced by steamed with rice wine. The processing mechanism of increasing efficacy and decreasing toxicity of Coptidis Rhizoma steamed with rice wine is closely related to intestinal microflora.

20.
Article in Chinese | WPRIM | ID: wpr-851336

ABSTRACT

Objective: To investigate the mechanism of type 2 diabetes mellitus (T2DM) treatment by drug pair containing Scutellariae Radix and Coptidis Rhizoma. Methods: The chemical composition and targets of Scutellariae Radix and Coptidis Rhizoma were searched by the analysis of traditional Chinese medicine system pharmacology platform (TCMSP), and T2DM related genes were searched by OMIM, TDD, Drugbank, and Digsee databases. UniProt database was used to query the target-related genes. Cytoscape 3.2.1 was used to construct compound-targets (genes) networks and protein-protein interaction (PPI) network to screen out the key targets. Finally, the mechanism of its action was studied by DAVID analyzing enrichment of gene ontology (GO) function and pathway enrichment analysis based on Kyoto Encyclopedia of Genes and Genomes (KEGG). Results: The compound-target network contained 42 compounds and 213 corresponding targets, and the key targets involved PTGS2, PTGS1, HSP90AA1, HSP90AB1, NOS2, etc. The PPI core network contained 15 protein, and key protein involved in TNF, IL-6, INSR, etc. The functional enrichment analysis of GO obtained 108 GO items (P < 0.05), of which there were 87 biological processes (BP) items, 9 molecular function (CC) items, and 12 related items of cell composition (MF). There were 24 signal pathways (P < 0.05) in the KEGG pathway enrichment screening, involving insulin resistance, T2DM and insulin signaling pathway and so on. Conclusion: The active components of Scutellariae Radix and Coptidis Rhizoma regulate inflammatory cytokines and act on insulin receptor in the treatment of T2DM mainly through DPP4, PPARG, IL6, PPARD, TNF, and other targets.

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