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Rhizoma coptidis extract has a variety of pharmacological activities, including alleviating cognitive impairment in Alzheimer's disease(AD). The main mechanisms of its anti-AD activity include reducing the production of amyloid β(Aβ), inhibiting the phosphorylation of Tau protein, inhibiting cholinesterase, anti-inflammation, anti-oxidation, improving apoptosis, etc.This paper reviewed the anti-AD effect of Rhizoma coptidis extract and the specific mechanisms, aiming to provide a theoretical basis for relevant research and clinical practice.
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Objective: To identify the active ingredients, potential targets, and mechanism of Rhizoma coptidis by bioinformatics method, and to explore the hypoglycemic effect of Rhizoma coptidis by in vitro experiments. Methods: The chemical components of Rhizoma coptidis were collected through database search, and oral bioavailability and drug-likeness were used for preliminary screening. The targets of Rhizoma coptidis and diabetes-related targets were collected by database retrieval and reverse docking techniques, and the biological process of cross-set proteins was analyzed. The inhibitory effects of Rhizoma coptidis on α-glucosidase, α-amylase activity, and advanced glycation end products (AGEs) were determined via in vitro experiments. In addition, the effects of Rhizoma coptidis on pre-adipocyte differentiation, absorption of glucose by adipocytes, and the level of intracellular triglyceride were investigated using the adipocyte differentiation model. Results: There were 11 potentially active ingredients in Rhizoma coptidis. IL-6, caspase-3, epidermal growth factor receptor (EGFR), MYC, and estrogen receptor 1 were considered as the key genes. The bioinformatics analysis showed that Rhizoma coptidis played an anti-diabetic role mainly via biological processes and signaling pathways including hormone receptor activity, glutathione binding, steroid binding, etc. In vitro experiments showed that the extract of Rhizoma coptidis inhibited the activities of α-glucosidase and α-amylase, and the generation of AGEs; meanwhile, the extract promoted the absorption of glucose by adipocytes. In addition, the extract of Rhizoma coptidis decreased triglyceride level. Conclusions: Our network pharmacology and in vitro experiments demonstrate the anti-diabetic effects and possible underlying mechanisms of Rhizoma coptidis extract.
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Objective: To identify the active ingredients, potential targets, and mechanism of Rhizoma coptidis by bioinformatics method, and to explore the hypoglycemic effect of Rhizoma coptidis by in vitro experiments. Methods: The chemical components of Rhizoma coptidis were collected through database search, and oral bioavailability and drug-likeness were used for preliminary screening. The targets of Rhizoma coptidis and diabetes-related targets were collected by database retrieval and reverse docking techniques, and the biological process of cross-set proteins was analyzed. The inhibitory effects of Rhizoma coptidis on α-glucosidase, α-amylase activity, and advanced glycation end products (AGEs) were determined via in vitro experiments. In addition, the effects of Rhizoma coptidis on pre-adipocyte differentiation, absorption of glucose by adipocytes, and the level of intracellular triglyceride were investigated using the adipocyte differentiation model. Results: There were 11 potentially active ingredients in Rhizoma coptidis. IL-6, caspase-3, epidermal growth factor receptor (EGFR), MYC, and estrogen receptor 1 were considered as the key genes. The bioinformatics analysis showed that Rhizoma coptidis played an anti-diabetic role mainly via biological processes and signaling pathways including hormone receptor activity, glutathione binding, steroid binding, etc. In vitro experiments showed that the extract of Rhizoma coptidis inhibited the activities of α-glucosidase and α-amylase, and the generation of AGEs; meanwhile, the extract promoted the absorption of glucose by adipocytes. In addition, the extract of Rhizoma coptidis decreased triglyceride level. Conclusions: Our network pharmacology and in vitro experiments demonstrate the anti-diabetic effects and possible underlying mechanisms of Rhizoma coptidis extract.
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OBJECTIVE@#To investigate the effects of Composition of Ophiopogon polysaccharide, Notoginseng total saponins and Rhizoma Coptidis alkaloids (CONR) on myocardial apoptosis of diabetic atherosclerosis (DA) rabbits METHODS: Sixty male New Zealand white rabbits were randomly divided into 6 groups [control group, model group, CONR high-dose group (450 mg/kg), CONR medium-dose group (150 mg/kg), CONR low-dose group (50 mg/kg), and simvastatin group] by using a completely random method, 10 in each group. DA model was established by intravenously injected alloxan combined with high-fat diet and abdominal aortic balloon injury. After mediation for 10 weeks, fasting blood glucose (FBG), glycosylated hemoglobin (GHB), glycosylated serum protein (GSP), fructoseamine (FRA), aldose reductase (AR), advanced glycation end products (AGEs) in serum were measured by enzyme linked immunosorbent assay (ELISA) method; the expression of receptor of AGEs (RAGE) in myocardial tissue were observed by immunohistochemical method; and p-Jun N-terminal kinase (p-JNK), caspase-3, B-cell lymphoma-2 (bcl-2) protein expression in myocardial tissue were measured by Western blotting. The myocardial apoptosis was detected by TdT-mediated dUTPnick-end labeling (TUNEL) method, and apoptosis index (AI) was calculated.@*RESULTS@#Compared with the control group, serum FBG, GHB, GSP, FRA, AR, AGEs and the expression of myocardium RAGE, p-JNK, caspase-3 proteins, as well as apoptosis index (AI) were significantly increased and bcl-2 protein was significantly decreased in the model group (P<0.01). Compared with the model group, the levels of serum FBG, GHB, GSP, FRA and AR showed a significant decline in CONR high- and medium-dose groups (P<0.01). FBG and GHB showed a significant decline in CONR low-dose group (P<0.01). Compared with the model group, the expression of serum AGEs and myocardium RAGE, p-JNK and caspase-3 protein as well as AI were significantly decreased and bcl-2 protein was significantly up-regulated in all treatment groups (P<0.01); high-dose CONR had the most significant effect on abovementioned indices compared with other treatment groups (P<0.01). Middle-dose CONR had better effect on serum AGEs compared with the low-dose group (P<0.01); middle-dose CONR and simvastatin groups had better effect on the expression of caspase-3, bcl-2 protein, myocardium apoptosis compared with the CONR low-dose group (P<0.01).@*CONCLUSION@#CONR may effectively inhibit myocardial apoptosis on DA rabbits by intervening AGEs-RAGE and JNK, caspase-3, and bcl-2 protein expressions.
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Animals , Male , Rabbits , Alkaloids , Pharmacology , Apoptosis , Atherosclerosis , Diabetes Mellitus, Experimental , Diabetic Angiopathies , Drug Therapy , Disease Models, Animal , Drugs, Chinese Herbal , Pharmacology , Heart , Ophiopogon , Chemistry , Panax notoginseng , Chemistry , Polysaccharides , Pharmacology , Saponins , PharmacologyABSTRACT
Objective To investigate the potential mechanism of Rhizoma Coptidis extracts (RCE) against sepsis associated with acute kidney injury. Methods C57BL/6 mice were divided into sham group, model group and RCE treatment group. The levels of Scr and BUN were measured by test kits. Gas chromatography-mass spectrometry was used to analyze metabolic changes in kidneys. Results The levels of Scr and BUN were increased in the model group than sham, which were reversed by RCE. 16 metabolites related to the progress of sepsis associated with acute kidney injury were detected, which were involved in amino acid metabolism and carbohydrate metabolism. Among these metabolites, the level of 8 metabolites can be reversed with RCE treatment. Conclusion RCE might exert therapeutic effects in sepsis associated with acute kidney injury by altering multiple metabolic pathways.
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This study was designed to validate the correlation between integrated pharmacokinetic and therapeutic effects of alkaloids using bile processed Rhizoma Coptidis (BRC). Rats were divided into three groups: normal, disease model, model+BRC. Rats were induced to have an excessive heat syndrome. Rectal temperatures were collected at 0, 3, 6 and 9 h after single oral administration of the drugs. The plasma concentrations of three alkaloids were quantified at different times by UPLC-MS/MS after the administration of BRC. An approach of self-defined weighting coefficiency was created to the holistic pharmacokinetic profiles of alkaloids in BRC. The classified and integrated synthetic concentrations were obtained, and then the pharmacokinetic parameters of alkaloids were calculated from non-compartmental model analysis. The potential relationship between the integrated mean concentration of alkaloids and the antifebrile efficacy was investigated. The holistic tmax of alkaloids was 1.11 h, the antifebrile effect of BRC at 3 h was improved over the model group. Double peaking appeared in the integrated blood concentration-time curve, the second tmax of alkaloids was 4.82 h. The antifebrile effects of BRC at 3-6 h were significant, and the antifebrile effects at 6-9 h was decreased significantly. Dynamic variation of alkaloids of BRC in the body exhibited the similarity to the pattern of its antifebrile effect.
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Aim To find the material foundation of treatment for diabetes in Coptidis Rhizoma ( RC ) . Methods The antihyperglycemic effect of RC alka-loids ( berberine, coptisine, palmatine, epiberberine, and jatrorrhizine) was evaluated in spontaneity diabe-tes KK-Ay mice. Results After 40 days′ oral admin-istration ( 225 mg · kg-1 · d-1 , ig ) , berberine and coptisine significantly suppressed the elevated fasting blood glucose level and ameliorated the glucose toler-ance . Body weight gain of KK-Ay mice was significant-ly decreased in the epiberberine-treated group. Berber-ine improved insulin resistance and jatrorrhizine in-creased the SOD activity, decreased the MDA level. Conclusions These results indicate that the main an-tihypoglycemic effect constituents are berberine and coptisine, while they show different mechanisms. Pal-matine, epiberberine and jatrorrhizine display different potential roles in the treatment of diabetes. The meth-ylene-dioxy groups at the C-2 , C-3 , C-9 and C-10 po-sitions are indispensable for antihyperglycemic effect of RC alkaloids.
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Objective To observe the therapeutic effect of iced Rhizoma Coptidis decoction stimulation for post-stroke swallowing disorder. Methods Sixty-two post-stroke swallowing disorder patients admitted from June of 2012 to June of 2014 in Sanya Hospital of Traditional Chinese Medicine were enrolled into the study. The patients were evenly randomized into intervention group and control group. The control group was given conventional intervention and stomatological nursing with ice, and the intervention group was given conventional intervention and stomatological nursing with iced Rhizoma Coptidis decoction, once a day for 4 continuous weeks. After treatment, the therapeutic effect on swallowing disorder was evaluated, and the changes of scores of swallowing disorder before and after treatment were compared in the two groups. Results (1) The total effective rate of intervention group was 87.09%, and that of the control group was 67.74%, the difference being significant (P<0.05) . (2) After treatment, scores of swallowing disorder were increased in both groups (P<0.05 compared with those before treatment) , and the increase in the intervention group was superior to that in the control group ( P<0.05) . Conclusion Iced Rhizoma Coptidis decoction stimulation is effective on improving swallowing function of post-stroke swallowing disorder patients.
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This study was aimed to optimize the extraction conditions of polysaccharides from Rhizoma Coptidis.With the R.Coptidis of extraction yield,polysaccharide yield and uronic acid yield as evaluation indexes,the impact of extraction temperature,extraction times,extraction duration and liquid-to-solid ratio on the process of R.Coptidis polysaccharides reflux extraction were investigated by the Box-Behnken design-response surface methodology.The results showed that the optimal extraction conditions were achieved and listed as follows:extraction temperature at 100℃,extracted 3 times with 3.8 h per each time,liquid-to-solid ratio of 1:15.7.It was concluded that the Box-Behnken design-response surface methodology was accurate,rational and feasible to optimize the extraction method of polysaccharides fromR.Coptidis.
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Objective To investigate the molecular mechanism of the inhibitory effects of rhizoma coptidis on multi-drug resistant uropathogenic Escherichia coli.Methods High-throughput RNA sequencing ( RNA-seq ) was performed to investigate the transcriptome in a multi-drug resistant uropathogenic Escherichia coli strain (NB8) treated with water decoction of rhizoma coptidis .Agar dilution test was used to determine the minimal inhibitory concentration ( MIC) of water decoction of rhizoma coptidis against the NB 8 strain.A growth curve was drawn to evaluate the effects of water decoction of rhizoma coptidis on the growth of NB8 strain.Total RNAs were extracted from the NB 8 strain after treated with the water decoction of rhizo-ma coptidis for 30 minutes and then synthetized to cDNA by reverse transcription after screening out the rRNAs.The HiSeq 2000 sequencing system was used for transcriptome sequencing .The TopHat software was used to map and analyze the RNA-Seq reads, and then Cufflinks was run to assemble transcripts and es-timate their abundances .The differential expression , GO enrichment and KEGG metabolic pathway were fur-ther analyzed .The NB8 strain dealt with normal saline was used as negative control .Results The MIC of water decoction of rhizoma coptidis to NB 8 strain was 12.5 mg/ml.There were 3665 genes expressed in NB8 strain treated with water decoction of rhizoma coptidis and 3430 genes expressed in NB8 strain treated with normal saline .The number of differentially expressed genes was 1428 including 921 up-regulated genes and 507 down-regulated genes .Those differentially expressed genes mainly enriched in the modules of binding and catalysis.The genes concerning cell adhesion , apoptosis and multicellular process were up-regulated, while those concerning the regulation of enzyme activities were down-regulated.Results of the KEGG meta-bolic pathway enrichment analysis showed that the genes concerning synthetic pathway of LPS were signifi -cantly up-regulated as well as those encoding the repair polymerase Ⅲthat was involved in DNA replication . However , the genes concerning fatty acid metabolism , histidine metabolism , thiamine metabolism , folate metabolism and iron carrier in ribosome synthesis showed overall down-regulation.Conclusion The tran-scriptome in uropathogenic Escherichia coli strain treated with rhizoma coptidis was profiled .The main mo-lecular mechanism of the inhibitory effects of rhizoma coptidis on uropathogenic Escherichia coli was to de-stroy the cell wall of Escherichia coli, affect the replication of DNA and regulate the transcription and transla-tion of proteins .This study illustrated that the inhibitory effects of rhizoma coptidis on uropathogenic Esche-richia coli were achieved in multiple levels .
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An HPLC method to determine six alkaloids of the Coptidis for Chinese Pharmacopoeia of 2015 Edition was established through C18 column. The mobile phase was CH3CN-0.25 mol·L-1 NH4Ac (36:64) (containing 8 mmol·L-1 SDS and adjusting pH 9.3 with ammonia) at the flow rate of 1 mL·min-1, the detective wavelength was 270 nm and the column temperature was 35 oC. The linear ranges of jatrorrhizine hydrochloride, columbamine hydrochloride, epiberberine hydrochloride, coptisine hydrochloride, palmatine hydrochloride and berberine hydrochloride were 0.006 96-0.233, 0.004 75-0.152, 0.003 30-0.528, 0.006 31-1.010, 0.004 71-0.753, 0.017 8-2.884 μg·mL-1, respectively. The average recoveries were 99.65%, 98.59%, 98.49%, 98.66%, 98.64%, 98.63% and RSD were 0.03%、0.15%、0.21%、0.12%、0.28%、0.23%, respectively. The method is simple and accurate, and can be used to determine the contents of jatrorrhizine, columbamine, epiberberine, coptisine, palmatine and berberine in the Coptidis.
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PURPOSE: This study aims to investigate the additive effect of the Hedera helix (HH) and Rhizoma coptidis (RC) extracts mixture on antitussive and expectorant activities in animals. MATERIALS AND METHODS: The expectorant assay was performed with phenol red secretion in mice trachea. Mice or guinea pigs were randomly divided into groups of 8 each, including negative and positive control groups. After gastric administration of the test extracts in mice, 2.5% phenol red solution (0.2 mL) was intraperitoneally injected. Trachea was dissected and optical density of tracheal secretion was measured. After gastric administration of the test extracts in guinea pigs, the antitussive activities were assessed using a citric acid-induced cough measurement. RESULTS: The extracts of HH and RC significantly increased tracheal secretion and inhibited cough. The mixture of HH and RC extracts in a 1:1 concentration at a dose of 200 mg/kg showed a more potent effect on phenol red secretion (25.25+/-3.14) and cough inhibition (61.25+/-5.36) than the individual use of each extracts [phenol red secretion; HH 13.39+/-4.22 (p=0.000), RC 20.78+/-2.50 (p=0.010), cough inhibition; HH 9.89+/-4.14 (p=0.010), RC 30.25+/-7.69 (p=0.000)]. A 3:1 ratio mixture of HH to RC demonstrated an optimal expectorant effect (p<0.001), and this mixture showed expectorant and antitussive effects in a dose-dependent manner. CONCLUSION: This study provides evidence for antitussive and expectorant effect of a 3:1 mixture of HH and RC, which may be a useful therapeutic option for respiratory diseases.
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Animals , Male , Mice , Antitussive Agents/administration & dosage , Behavior, Addictive , Cough/drug therapy , Drugs, Chinese Herbal/administration & dosage , Ethanol , Expectorants/administration & dosage , Guinea Pigs , Hedera/chemistry , Phytotherapy , Plant Extracts/pharmacology , Plant Roots/chemistry , Trachea/drug effectsABSTRACT
Aim To study the hypnotic effect of five alkaloids extracted from Rhizoma Coptidis (berberine , coptisine,palmatine,epiberberine,jatrorrhizine )in mice,and preliminarily explore its underlying mecha-nism.Methods The experiments of locomotor activity and hypnosis induced by suprathreshold and subthresh-old doses of pentobarbital sodium were used to evaluate the effect of drugs on sleep behavior in mice.Then, HPLC-FLD was used to detect the contents of NE,DA and 5-HT on PCPA mice model.Results Compared with control group,berberine and coptisine notably in-hibited spontaneous activity in behavioral experiments (P <0.05),and increased the sleeping percentage of mice under subthreshold dose of pentobarbital sodium. Berberine and coptisine shortened the period of sleep latency,and prolonged the sustained period of sleeping at suprathreshold dose in mice (P <0.05 or P <0.01 ).Other alkaloids had no significant differences in sleep latency and period of sleep observed in this current experiment.Compared with PCPA mice model group,berberine and coptisine remarkably increased the contents of NE and 5-HT (P <0.01 ),but they had no effects on DA.Conclusions Berberine and coptisine may play a sedative and hypnotic role in PC-PA mice by increasing contents of 5-HT and NE in hy-pothalamus,and the sedative and hypnotic effects of berberine are stronger than those of coptisine.Other alkaloids have no effects on sleeping in mice.
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Objective: To study the interaction between biomacromolecules (protein and DNA) and different Rhizoma Coptidis alkaloids (palmatine, coptisine, epiberberine, jatrorrhizine and berberine) and the difference among 5 Rhizoma Coptidis alkaloids. Methods: Bovine serum albumin (0.5 mL of 1.10 × 10-5 mol/L) was added to 1.5mL of each alkaloid of different concentrations (concentrations of palmatine, coptisine, epiberberine, jatrorrhizine and berberine being 0, 1.95×10-6, 3.9×10-6, 7.8×10-6, 1.56×10-5 and 3.12×10-5 mol/L, respectively). The reaction system was shaken and incubated at 37°C for 1h, and then the emission spectra of mixed solution were recorded within 300 to 500nm at 280nm excitation. Plasmid DNA (0.5mL of 0.1%) was added to 1.5mL of each alkaloid with different concentrations (concentrations of palmatine, coptisine, epiberberine, jatrorrhizine and berberine being 0, 1.95×10-6, 3.9×10-6, 7.8×10-6 and 1.56×10-5 mol/L, respectively). The reaction mixture was well shaken, and then the fluorescent emission spectrum was recorded from 480 to 650 nm at 368 nm excitation by an F-4500 fluorescence spectrophotometer. Results: All the Rhizoma Coptidis alkaloids in test exhibited similar quenching effect on fluorescence of bovine serum albumin, and they all showed fluorescence enhancing effect on plasmid DNA, and the enhancing effects varied greatly among the five alkaloids, with epiberberine showing the strongest activity, followed by coptisine, palmatine, berberine, and jatrorrhizine in order. The strongest interaction between DNA and five alkaloids were found at the concentration of 7.8×10-6mol/L. Conclusion: Strong interaction can be found between Rhizoma Coptidis alkaloids and biomacromolecules including protein and DNA. The interaction of Rhizoma Coptidis alkaloidswith plasmid DNA varies greatly among different alkaloids and is similar with bovine serum albumin. 9, 10-methylene-dioxy groups and 2, 3-dimethoxy groups might have promoted the interaction between alkaloids and DNA.
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AIM@#Methicillin-resistant Staphylococcus aureus (MRSA) is a pathogenic bacterium that causes both hospital- and community-acquired infections, and for which single-drug treatments are becoming less efficient. Rhizoma coptidis has been used for more than two thousand years in China to treat diarrhea, fever, and jaundice. In this study, the anti-MRSA activity of Rhizoma coptidis is examined and its effective components sought.@*METHODS@#The mecA and norA genes were determined by PCR amplification and sequencing. Drug susceptibility of Staphylococcus aureus ATCC43300 was performed using the VITEK2 compact system. The chemical fingerprint of Rhizoma coptidis was investigated using HPLC and preparative liquid chromatography, and the anti-MRSA activity was determined using an improved broth microdilution method.@*RESULTS@#The drug susceptibility test revealed that the penicillin-binding protein phenotype of the strain changed in comparison to penicillin-sensitive Staphylococcus aureus. Ten batches of Rhizoma coptidis showed anti-MRSA activity on the norA-negative Staphylococcus aureus strain, as well as the strain that contained a norA gene. The spectrum-effect relationship revealed that the berberine alkaloids were the effective components, within which berberine, coptisine, palmatine, epiberberine, and jatrorrhizine were the major components.@*CONCLUSION@#This study lays a foundation for in vivo studies of Rhizoma coptidis and for the development of multi-component drugs.
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Anti-Bacterial Agents , Chemistry , Pharmacology , Bacterial Proteins , Genetics , Metabolism , China , Drugs, Chinese Herbal , Chemistry , Pharmacology , Methicillin-Resistant Staphylococcus aureus , Genetics , Metabolism , Microbial Sensitivity Tests , Methods , Ranunculaceae , Chemistry , Rhizome , ChemistryABSTRACT
AIM@#To investigate the cytotoxic effects of the six protoberberine alkaloids (PAs) from Rhizoma Coptidis on HepG2 cells.@*METHOD@#A systematic screening was conducted to investigate the dynamic response of HepG2 cells to the PAs using the impedance-based xCELLigence system. Cisplatin was selected as the positive control. The real time, concentration-response curves and the 50% inhibitory concentrations (IC50) were acquired to evaluate the anticancer activity of the PAs.@*RESULTS@#All of the six PAs inhibited cell growth and induce death in HepG2 cells in a time- and concentration-dependent manner. The IC50 values of cisplatin, berberine, columbamine, coptisine, epiberberine, jatrorrhizine, and palmatine were 5.13, 42.33, 226.54, 36.90, 302.72, 383.54, and 456.96 μg·mL(-1), respectively. The results obtained using the xCELLigence system corresponded well with those of the conventional methods.@*CONCLUSION@#The xCELLigence system is a reliable and efficient tool for real-time screening of the cytotoxic effect of compounds in cell-based in vitro assays. Coptisine and berberine, with methylenedioxy group at C2 and C3 on the phenyl ring showed stronger effect.than the other four PAs. However, compared with cisplatin, the six PAs didn't show obvious cytotoxic effect on HepG2 cells. These results provided some useful data for the evaluation of the anticancer compounds, and the clinical application of traditional Chinese medicine.
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Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Berberine , Pharmacology , Therapeutic Uses , Berberine Alkaloids , Pharmacology , Therapeutic Uses , Cell Death , Cisplatin , Pharmacology , Therapeutic Uses , Coptis , Chemistry , Drug Evaluation, Preclinical , Methods , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Electric Impedance , Hep G2 Cells , Hepatoblastoma , Drug Therapy , Inhibitory Concentration 50 , Liver Neoplasms , Drug Therapy , Phytotherapy , Rhizome , ChemistryABSTRACT
This study took geo-authentic medicinal material Rhizoma Coptidis as an example and analyzed soil characteristics of the growing environment of Rhizoma Coptidis . The methods of ISSR, HPLC, 1H-NMR and NIR were respectively used for exploring its genotype and investigating on its chemitype . In the respects of an-ti-endotoxin, anti-bacterial activities and insulin resistance that was related to the treatment of diabetes, the pharmacodynamic type was studied and the relationship was comprehensively analyzed . The quality evaluation of geo-authentic medicinal materials was preliminarily established based on ecotype , genotype chemitype and phar-macodynamic type of Rhizoma Coptidis . Simultaneously, quality standards of Rhizoma Coptidis were set up in combination with genuine character , which provided the scientific basis for establishing Chinese medicine char-acteristic methods of quality evaluation of Rhizoma Coptidis .
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The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers,and the compatibility mechanism of Jiao-Tai-Wan (JTW) composed of Rhizoma Coptidis granules and Cinnamon granules were investigated.The concentration of berberine in plasma of healthy male volunteers was determined directly by high performance liquid chromatography (HPLC) after an oral administration of Rhizoma Coptidis granules alone or combined with Cinnamon granules (JTW).The plasma concentration-time curves of berberine were plotted.The data were analyzed with Drug and Statistics (DAS) 2.0 pharmacokinetic program (Chinese Pharmacology Society)to obtain the main pharmacokinetic parameters.The results showed that the plasma concentration-time curve of berberine was described by a two-compartment model.The Cmax,Tmax,t1/2 and CLz/F of berberine in Rhizoma Coptidis granules were 360.883 μg/L,2.0 h,3.882 h,119.320 L·h-1·kg-1 respectively,and those of berberine in JTW were 396.124 μg/L,1.5 h,4.727 h,57.709 L·h-1·kg-1 respectively.It was suggested that Rhizoma Coptidis granules combined with Cinnamon granules could increase the plasma concentration of berberine,promote berberine absorption and lengthen the detention time of berberine in healthy male volunteers.
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AIM:To investigate the effects of Compound Rhizoma Coptidis ( Rhizoma eoptidis,Radix suctellariae,Cortex phellodendri Chinensis,Fructus gardeniae and Radix et Rhizoma glycyrrhizae) on vascular calcification in rats treated with warfarin and vitamin D_3.METHODS: Thirty-two male SD rats were assigned randomly into control group,calcified group,Compound Rhizoma Coptidis prevented group and treated group.The later three groups were treated with warfarin,and subcutaneously injected with vitamin K_1 and vitamin D_3 for one week to induce extensive calcification of the aorta.Compound Rhizoma Coptidis was given before the first warfarin dose in prevented group and the drug was given after the modeling in the treated group.The control group was treated with normal saline.The calcification in the aorta was analyzed and osteoprotegerin (OPG) mRNA and protein were determined using histomorphometry,RT-PCR and immunohistoehemistry after 4 weeks of drug intervention.RESULTS : The results of 32 rats was analyzed compared to the control group,the area of darkly stained regions by Von Kossa staining and the level of calcium content in aorta wall increased significantly[(608.32±42.29) μg/g vs (1 139.47±230.03) μg/g,P ＜0.05].The OPGmRNA and protein decreased in aortic sections.No artery calcification could be detected in Compound Rhizoma Coptidis prevented group and a little artery calcification could be detected in Compound Rhizoma Coptidis treated group.The level of calcium content in aorta wall significantly lower[(854.77±12.99) μg/g,(875.78±27.23 ) μg/g].The expresion of OPGmRNA and the protein significanfly increased in Compound Rhizoma Coptidis prevented and treated groups.CONCLUSION:Compound Rhizo-ma Coptidis may prevent or regress the vegcular calcifiation,that seems dependent on the upregression of aortic OPG levels.
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AIM: To investigate the changes of alkaloid in Rhizorrm Coptidis and Fructus Evodiae before and after combination. METHODS: The content of berberine hydrochloride,palmatine hydrochloride,jatrorrhizine hydrochloride in Rhizoma Coptidis and Fructus Evodiae before and after combination were determined by TLCS.RESULTS : After combination of Rhizoma Coptidis and Fructus Evodiae,contents of berberine hydrochioride,palmatine hydrochloride,jatrorrhizine hydrochloride significantly reduced,among which the reduction of berberine hydrochloride was more obvious.CONCLUSION: In decoction,Fructus Evodiae appears to restrict the alkaloid from Rhizoma Coptidis in order to lower the side effect of Rhizoma Coptidis.