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Objective:To explore the cognition and attitude of urological nurses towards patients′ sexual health education, and to provide basis for the development of urological patient sexual health education.Methods:The research was based on the phenomenology research method. Qualitative research were used to conduct semi-structured personal in-depth interviews with 18 nursing staff who are from 5 tertiary general hospitals in Shanghai, Shandong, Hainan, Anhui and Xinjiang Uygur Autonomous Region using a purposive sampling, data were analyzed by claizzi phenomenological data 7-step analysis method.Results:After refining, two categories and five themes were obtained, including vague concepts (confusion of concepts, lack of roles, lack of theoretical knowledge), neglect and avoidance (respect for patients′ wishes, low priority).Conclusions:Urological nurses have low ability to evaluate the needs of patients′ sexual health education, and the content of sexual health education was one-sided, the form was single, and the degree of preparation was low, so they can not provide personalized and standardized health education for patients. We should carry out education in multiple ways for urological nurses, develop a tool for assessing the needs of urological patients′ sexual health education in China as soon as possible, formulate a standardized and personalized sexual health education standard, and provide comprehensive, systematic and consistent sexual health education for patients, so as to improve the sexual health level of urological patients.
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Objective@#To analyze the mechanism of metformin in improving oxaliplatin resistance of colorectal cancer cells.@*Methods@#The expression levels of EIF3G in 71 cases of colorectal cancer and adjacent tissues were detected by RT-qPCR. The survival curve was established by Kaplan-Meier method. The survival rate difference between the two groups was compared by Log-rank test.HCT-116 cells were infected with shEIF3G lentivirus, HCT-116 L-OHP-resistant cell line was constructed.After treated with metformin, sensitivity to L-OHP was detected by CCK-8 assay, RT-qPCR and Western blot were used to analyze the EIF3G mRNA and protein levels. The subcutaneous tumor model of nude mice was constructed to observe the effect of metformin on tumor growth.@*Results@#The expression level of EIF3G mRNA in colorectal cancer tissues was up-regulated by (3.24±0.43) times compared with paraneoplastic tissues (P<0.01). EIF3G level was significantly correlated with the prognosis of colon cancer patients. Knockdown EIF3G could enhance the L-OHP sensitivity of HCT116/L-OHP cells (P<0.05); Metformin can reduce the expression level of EIF3G and improve the drug resistance of HCT116/L-OHP cells (P<0.05), and inhibit the development of colorectal cancer in vivo (P<0.05).@*Conclusion@#Metformin can inhibit the expression of EIF3G and improve the L-OHP resistance of HCT-116 cells.
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Objective To analyze the mechanism of metformin in improving oxaliplatin resistance of colorectal cancer cells.Methods The expression levels of EIF3G in 71 cases of colorectal cancer and adjacent tissues were detected by RT-qPCR.The survival curve was established by Kaplan-Meier method.The survival rate difference between the two groups was compared by Log-rank test.HCT-116 cells were infected with shEIF3G lentivirus,HCT-116 L-OHP-resistant cell line was constructed.After treated with metformin,sensitivity to L-OHP was detected by CCK-8 assay,RT-qPCR and Western blot were used to analyze the EIF3G mRNA and protein levels.The subcutaneous tumor model of nude mice was constructed to observe the effect of metformin on tumor growth.Results The expression level of EIF3G mRNA in colorectal cancer tissues was up-regulated by (3.24 ± 0.43) times compared with paraneoplastic tissues (P ＜ 0.01).EIF3G level was significantly correlated with the prognosis of colon cancer patients.Knockdown EIF3G could enhance the L-OHP sensitivity of HCT116/L-OHP cells (P ＜ 0.05);Metformin can reduce the expression level of EIF3G and improve the drug resistance of HCT116/L-OHP cells (P ＜ 0.05),and inhibit the development of colorectal cancer in vivo (P ＜ 0.05).Conclusion Metformin can inhibit the expression of EIF3G and improve the L-OHP resistance of HCT-116 cells.
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OBJECTIVE:To explore the multi-component,multi-target,multi-channel mechanism of Tibetan medicine Ptero-cephalus hookeri in the treatment of rheumatoid arthritis (RA). METHODS:The selected target compounds (10 chemical struc-tures of P. hookeri)were imported and stored by related software;target prediction and filtering were conducted by PharmMapper and DrugBank databases. The pathways of targets were acquired and analyzed by MAS 3.0 database. Finally P. hookeriactive com-ponent-targeting-pathwaynetwork was constructed by Cytoscape 3.4.0 software. RESULTS:The target information obtained in the PharmMapper database were compared with that of the DrugBank database for inflammation-related drugs,26 potential targets for the treatment of RA were obtained,in which MAPK14,RXRA,ALB,PDE4D,VDR may be the main potential target gene group in the treatment of RA. 57 functional pathways were obtained after 26 functional targets were annotated by pathway. In addition to 27 RA-related pathways,30 other pathways such as endocrine regulation and immune were involved. CONCLUSIONS:Base on the study of network pharmacology,P. hookeri plays the role in the treatment of RA by acting on inflammation,immune,endo-crine and related targets and pathways.
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Objective To evaluate evidence-based practice of catheter removal strategy in patients with short-term indwelling catheter after partial nephrectomy. Try to apply the best evidence into practice, and further to improvethe quality of clinical nursing through quality review. Methods Two rounds of quality review were carried out in the 2 wards from July to December in 2016. Using the 5 review criteria of best evidence, we reviewed baseline of catheter removal strategies for patients with short-term indwelling catheter after partial nephrectomy and developed appropriate evidence-based practice. Further, the best evidence was integrated into clinical nursing practice, and the prognosis was reviewed after then. Results In the baseline review, the compliance of the 5 review criteria was 0. However, after introducing the best evidence into nursing practice,the compliance was up to 100%. The mastering of evaluation knowledge of catheter removal of nurses increased from 73.00 ± 9.35 to 94.81 ± 3.38 with significant difference (t=12.72, P<0.01). The indwelling time of catheter shorted from (5.69±0.79) d to(4.24±0.82) d. The difference was significant (t=5.47, P<0.01). Conclusions Evidence-based nursing practice improvesthe strategies of short-term catheter removal after partialnephrectomy, while closer cooperation between nurses and doctors are still needed to promote the continuous improvement of nursing quality.
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Aim To establish the pharmacokinetic-pharmacodynamic(PK-PD) modeling to characterize the antipyretic effects of coptisine, an active component in coptis chinensis on rats.Methods Nine healthy male Sprague-Dawley(SD) rats were randomly divided into three groups, each with three.The rats in the first group were injected intravenously with lipopolysaccharide(LPS,100 μg·kg-1) alone.The second and third group rats were given coptisine high-dose(3.87 mg·kg-1) and coptisine low-dose(1.93 mg·kg-1) by tail vein injection at 30 min after LPS injection, respectively.Body temperature was measured at different time points, and blood samples from tail vein were collected simultaneously.The blood concentration of coptisine was determined by ultra performance liquid chromatography.Monolix software was used to model PK-PD of coptisine mean plasma concentration and temperature effects,by population computation with non-covariates.Besides.the model with advantage was selected by the fitting goodness.Results Coptisine could inhibit body temperature of endotoxin-induced fever in rats significantly.Two-compartment linear elimination model was used to describe the final PK model.Gaussian function, an input function of body temperature changes, which was used to depict PD model, the PK and PD models were connected by the Emax model.At last, the final model was fitted better;the fitting results indicated that the EC50 of antipyretic effect of coptisine was 89.7 μg·L-1, and the Emax was 1.88℃.Conclusions Coptisine has a powerful anti-pyretic effect on endotoxin-induced pyrexia of rats with high potency, Low in vivo distribution and quick clearance.
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OBJECTIVE:To establish the method for the determination of oleanolic acid and ursolic acid in different medicinal parts of Tibetan medicine Pteocephalus hookeri,and compare the differences among the different parts. METHODS:The contents of oleanolic acid and ursolic acid from different medicinal parts(whole plant,aerial part,underground part)of P. hookeri were de-termined by UPLC-PDA. The separation was performed on Acquity UPLC HSS T3 column(150 mm×2.1 mm,1.8 μm)with mobile phase consisted of methanol-0.1 mol/L ammonium acetate(88:12,V/V)at the flow rate of 0.2 mL/min. The detection wavelength was set at 210 nm,and column temperature was 30 ℃. The sample size was 5 μL. RESULTS:The linear ranges of oleanolic acid and ursolic acid were 10.65-1065 μg/mL (r=0.9996) and 18.8-1880 μg/mL (r=0.9994),separately. The recoveries were 96.95%(RSD=1.24%,n=9) and 98.12%(RSD=2.13%,n=9),separately. RSDs of precision,stability and reproducibility tests were all less than 3%. The contents of oleanolic acid and ursolic acid from different medicinal parts in P. hookeri were in de-scending order of aerial part>whole plant>underground part;the average total content of oleanolic acid and ursolic acid from whole plants was 0.35%,the aerial part reached 0.56% and underground part was 0.09%. CONCLUSIONS:The method is rapid, accurate and reproducible,and it is suitable for the content determination of oleanolic acid and ursolic acid in different medicinal parts of Tibetan medicine P. hookeri. The contents of oleanolic acid and ursolic acid from aerial part of P. hookeri are higher than whole plant and underground part. It is suggested to use aerial parts of medicine.
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The liquid-chromatography-mass technology was used in the metabolomic analysis of mouse's blood 1 hour after exhaustive exercise,in order to explore the potential mechanism of Rhodiola in fatigue elimination of exhaustive exercise mouse.The exhaustive mouse model was made by loaded-swimming.A total of 24 mice were randomly divided into theRhodiola + exercise group,exercise group andno-exercise group.The dose of Rhodiola was 0.4375 g·kg-1·d-1.The loaded-swimming was conducted after two successive weeks of medication.Blood was collected 1 h after swimming for the sample preparation.The enzyme assay and anthrone colorimetry were used to test blood lactate acid and glucose,respectively.UFLC-Q-TOF was used to detect metabolic profiles of each group.The principal component analysis (PCA),orthogonal partial least squares discriminant analysis (OPLS-DA) and heat map analysis were used to compare differences among groups with score chart and to obtain the characteristics biomarkers by load chart.The results showed that the blood lactate acid level of theRhodiola+ exercise group was significantly lower than that of theexercise group.And the glucose level of theRhodiola+ exercise group was significantly higher than that of theexercise group.The metabolomic analysis showed that there were no obvious changes on 1,25-(OH)2D3,diacylglycerol (DG) and inositol triphosphate (IP3).All three materials in theRhodiola + exercise group were significantly lower than those of theexercise group.They were much closer to theno-exercise group.And all three materials were related to the increasing of muscle tension.It was concluded that Rhodiola had the function of promoting fatigue eliminating.This effect may be related to cell membrane protection,regulation of 1,25-(OH)2-D3→IP3,DG pathway,and relieving of muscle tension after exercises.
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This article reviewed pharmacological study development of Punica granatum L. both at home and abroad in recent years. P. granatum has a long medical usage history. Different parts of P. granatum have wide applications in both traditional Chinese medicine (TCM) and other ethnic medicine. Its main chemical compositions were tannins, flavonoids, alkaloids and organic acids. It has obvious pharmacological activities. In recent years, the pharmacological research progress on P. granatum in terms of antibacterial, antiviral, hypoglycemic, antitumor, adjusting blood lipids, antioxidant, and immunoregulation has rapid development. The scientific collection and analysis on effects and new pharmacological research results of P. granatum are hoped to provide references for the study, clinical application, development and utilization of P. granatum and its products.
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Objective To develop a Chinese version of Frommelt Attitude Toward Care of the Dying scale (FATCOD) and evaluate its validity and reliability to provide a tool for the field of hospice care and death education used among nurses.Methods FATCOD scale was adopted according to Brislin's translation model for cross-cultural research and its reliability and validity of the new Chinese version was tested in 126 nurses.Factor analysis and correlation analysis were applied to establish the validity and reliability.Results The Chinese version of FATCOD scale consisted of 30 items.The Cronbach's α coefficient of the scale was 0.828; split-half coefficient of the whole scale was 0.807; the varimax rotation factor analysis of the scale identified twelve principal factors and explained for 69.5％ variances.Conclusions The Chinese version of FATCOD scale is valid and reliable in the sample of nurses,and can be used in the field of hospice care and death education.
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This study was aimed to reveal the species characteristics of Chinese patent medicines for antitussive ef-fect and provide references for developing new drugs. This research targeted Chinese patent medicines for antitussive effect which were included in the Pharmacopoeia of the People's Republic of China and the New National Chinese Patent Medicines as well as those characterized by keywords such as cough cure, cough alleviating, antitussive effect, cough, persistent cough. The analysis was made on the species characteristics, such as the number of Chinese patent medicines for antitussive effect, license number, ethnomedicine patent medicines, drugs for children use, protection of varieties of traditional Chinese medicine, the number of drugs, the generic names of drug, and drug forms. The results showed that 684 Chinese patent medicines for antitussive effect collected in this research had ac-counted for 8.60% of the total 7 260 of Chinese patent medicines. A total of 7 450 license numbers were approved, and 33% of the Chinese patent medicines shares one license number. One Chinese patent medicine owns 16.6 li-cense numbers on average. Ethnomedicine patent medicines had 3 Tibetan prescriptions such as the Shiwuwei Chenxiang pill and 4 Mongolian prescriptions, such as the Siwei Tumuxiang powder. Drugs for children accounted for 14%, including 9 forms. The type of the generic names of drug reached 16 and most of them originate from abbrevia-tions of the main drug in prescription. The number of drugs in prescription ranges from 8 to 16. Chinese patent medicines for antitussive effect involved 16 forms, of which the proportion of the use of solid preparation was higher than the liquid preparation. It was concluded that Chinese patent medicines for antitussive effect were characterized by such advantages such as a variety of species, various forms, the reasonable number of drugs, considerable medicine retail market share and drug for children use which can meet the clinical needs, and meanwhile some prob-lems, such as a lack of criteria for the generic names of drug, the homogenization of fierce competition, and inade-quacy of ethnomedicine patent medicines.
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This study was aimed to investigate the effects of extract from Tibetan medicine Berberis Cortex (TMBC) on expressions of protein kinase C (PKC-β), vascular endothelial growth factor (VEGF) and hypoxia-inducible factor (HIF-1α) in the retina of diabetic rats. Diabetic rats were established by one time intraperitoneal injection of strepto-zocin (STZ). Rats were randomly divided into the model group, low-dose TMBC group, medium-dose TMBC group, high-dose TMBC group, metformin group, calcium dobesilate group, berberine group and the normal control group. Intragastric administration was given. The medication amounts of TMBC in the low-dose, medium-dose and high-dose group were 5, 10, and 20 times to the adult medication dose. In the metformin group and the berberine group, 10 times of the adult medication dose were given. Distilled water was given in the model group and the normal con-trol group. After 6-week intragastric administration, all experimental rats were sacrificed. The expressions of PKC-β, VEGF and HIF-1α were examined by real-time fluorescence quantitative PCR assay and western blot. HIF-1α ex-pression was detected by immunohistochemistry. The results showed that compared with the normal control group, the mRNA and protein expression of PKC-β, VEGF and HIF-1α increased obviously in the retina of diabetic rats ( P<0.01). Compared with the model group, the mRNA expression of PKC-β, VEGF and HIF-1α in the high-dose and medium-dose TMBC group reduced obviously (P< 0.01). The protein expression levels of PKC-β, VEGF and HIF-1α were also obviously reduced (P< 0.05). The expressions of PKC-β, VEGF and HIF-1α in the low-dose TMBC group were obviously reduced (P < 0.05). It was concluded that TMBC can depress the expressions of HIF-1α, PKC-β and VEGF in the retina of diabetic rats, which can be served as a protective effect to prevent progress of di-abetic retinopathy.
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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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This study was aimed to reveal characteristics of functions, main indications and applications of Chinese patent medicines in order to provide references for development of new Chinese patent medicines for antitussive ef-fect. Chinese patent medicines recorded in the Pharmacopoeia of the People's Republic of China and the New Na-tional Chinese Patent Medicines were taken as research subjects. Chinese patent medicines classified in the function and indication with key words of cough-relieving, cough-suppressing, cough and chronic cough were col-lected. Analysis was made on the prescription characteristics, such as functions, main indications and applications. The results showed that there were 684 Chinese patent medicines and 462 terms, which were used for a total of 1533 times. The frequently-used terms are antitussive effect with expectorant, antitussive effect, expectorant, heat-clearing and exterior-releasing, antiasthmatic, wind-expelling and antipyretic, antitussive effect with antiasthmatic, purging lung heat, relieving exterior syndrome and moistening the lungs. All 684 Chinese patent medicines were used 48 ma-jor treatments for a total of 1107 times. The main indications include acute and chronic trachitis / bronchitis, exoge-nous wind-heat type of common cold, exogenous wind-cold type of common cold, cough with abundance of phlegm due to phlegm-heat obstructing the lung, acute upper respiratory tract infection, asthma, acute and chronic pharyngi-tis, lung heat cough, and etc. All 684 Chinese patent medicines used a total of 537 kinds of herbs and chemical medicines, including 441 kinds of herbal medicine, 36 kinds of animal medicine, 25 kinds of mineral medicine and 35 kinds of chemical medicine. The top ten herbs in terms of using frequency are Glycyrrhizae radix et rhizoma, Platycodonis radix, Armeniacae semen amarum, Menthae haplocalycis herba, Citri reticulatae pericarpium, Ephedrae herba, Scutellariae radix, Perilla frutescens (L.) Britt, Pinelliae rhizoma, Fritillariae cirrhosae bulbus. Among them, 1/4 of Chinese patent medicines used extract. Five kinds of food or fruits were also used, which were orange, fresh gin-ger, pear, watermelon and dried mushroom. It was concluded that Chinese patent medicines for antitussive effect can be adopted in the treatment of various kinds of diseases, especially for the treatment of cough(heat cough in partic-ular), abundance of phlegm, asthma, pharyngitis, laryngitis, and etc. The treatment methods of clearing heat, dis-pelling wind and relieving exterior syndrome played an important role in the realization of antitussive effect. However, the expression of functions and main indications is far from standardized and clear. Drugs commonly used are herbal medicine plus animal medicine, mineral medicine and chemical medicine as well as food and fruit. The discovery of preparations with certain clinical curative effect from ethnomedicine and the using of their extracts as a major ingre-dient are one important way to develop new Chinese patent medicines with antitussive effect.
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<p><b>OBJECTIVE</b>To observe dynamic changes of blood lead concentration in rats with long-term toxicity test with Goupi Gao by the flame atomic absorption spectrometry, in order to provide reference for safe administration of Goupi Gao.</p><p><b>METHOD</b>The rats were administered with Goupi Gao by high-dose (7 g x kg(-1)), medium-dose (3.5 g x kg(-1)), low-dose (1.75 g x kg(-1)) by external use for consecutively 90 days. Then, the blood samples were collected from the rats before the administration and at 10, 30, 45, 52, 60, 90 d after the administration respectively, as well as 16 d and 28 d after the drug withdrawal. The samples were dispelled with microwave digestion system and then were determined by graphite furnace atomic absorption spectrometry for blood lead levels.</p><p><b>RESULT</b>According to methodological study, the standard curve regression equation in this experiment was A = 0.004 9X + 0. 017, r = 0.999 5, with the detection limit up to 0. 380 microg x L(-1). The RSD was 1.4% by precision checks. Blood lead level of mixed blood samples was 175.77 microg x L(-1), whose RSD was 6. 0%. Blood lead concentration gradually increased after low-dose and medium-dose administration to rats and became stable at the 10th day and the 30th day by high-dose. Dose is directly related to blood lead concentration. Meanwhile, the blood lead concentration decreases after the drug withdrawal.</p><p><b>CONCLUSION</b>The method of determination in this experiment is so accurate and reliable that it can be used for the determination of blood lead. Long-term and high-dose external use of Goupi Gao can increase blood lead.</p>
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Animals , Female , Male , Rats , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Toxicity , Lead , Blood , Random Allocation , Rats, Sprague-Dawley , Spectrophotometry, Atomic , Methods , Time Factors , Toxicity TestsABSTRACT
<p><b>OBJECTIVE</b>To observe the effect of long-term external use of Goupi Gao on renal function and lead accumulation in rats.</p><p><b>METHOD</b>Rats were externally administered with Goupi Gao at different doses (7, 3.5 and 1.75 g x kg(-1)) for 90 d. At 45 days and 90 days after administration, the renal indicator, levels of blood urea nitrogen (BU) and creatinine (Cr) in serum, beta2-microglobulin (beta2-MG) and N-acetyl-beta-D-glucosaminidase (NAG) in urine were determined. Lead content in kidneys was detected by atomic absorption spectrometry.</p><p><b>RESULT</b>A 90-day administration with Goupi Gao significantly enhanced the renal indicator, levels of NAG in urine and lead content in renal, when compared with the normal rats. However, the levels of BUN and beta2-MG as well as renal pathology in Goupi Gao treated rats were not obviously changed.</p><p><b>CONCLUSION</b>Consecutive administration of Goupi Gao for 90 days can increase the renal indicator and levels of NAG in urine, enhance the accumulation of lead in renal, but with no effect on excretory function of kidneys and organic changes.</p>
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Animals , Female , Male , Rats , Acetylglucosaminidase , Urine , Blood Urea Nitrogen , Creatinine , Blood , Drugs, Chinese Herbal , Toxicity , Kidney , Metabolism , Pathology , Lead , Metabolism , Random Allocation , Rats, Sprague-Dawley , Spectrophotometry, Atomic , beta 2-Microglobulin , UrineABSTRACT
Objective To investigate the role of deoxycholic acid (DCA) in the pathogenesis of Barrett esophagus.Methods Normal human esophageal mucosal epithelial cells were cultured in vitro with defined keratinocyte serum-free media (D-KSFM).The cultured cells were treated with different concentrations of DCA and specific p38 mitogen activated protein kinase (MAPK) inhibitor. The expression of p38,phosphorylated p38 (p-p38) and caudal-related homeodomain transcription 2 (CDX2) at protein level were assessed by Western blot.The correlation between p-p38 and CDX2 was analyzed.The data were analyzed by one way ANOVA and LSD test.Results After being cultured with DCA for 24 h,the expression of p-p38 and CDX2 increased along with the increasing of DCA concentration.Compared with the control group (p-p38 was 13.7％ ± 1.0％ and CDX2 protein was 0),the difference was statistically significant (P＜ 0.05).When DCA was at 500 μmol/L,the expression of p-p38 and CDX2 reached the highest level (44.0％ ± 1.7％ and 8.59± 1.25).After pretreated with SB203580 for two hours and then 500 μmol/L DCA was added into cell culture,both expression level of p-p38 and CDX2 decreased compared with 500μmol/L DCA group (p-p38:28.3％ ±2.2％ vs50.5％±9.5％,CDX2:0.94±0.13 vs 2.31±0.41) after 24 h.Conclusions DCA can induce the expression of CDX2 in normal human esophageal mucosal epithelial cells,which is related with the activation of p38.The phosphorylation of p38 maybe involved in the pathogenesis of Barrett esophagus.
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<p><b>OBJECTIVE</b>To develop an HPLC method for determination of loganin in Pterocephalus hookeri.</p><p><b>METHOD</b>The analysis was performed on a Welchrom C18 column (4.6 mm x 250 mm, 5 microm) with acetonitrile-water (12:88) as the the mobile phase at a flow rate of 1 mL x min(-1) and the detection wavelength was 240 nm.</p><p><b>RESULT</b>The peak areas and injection amounts of loganin had a good linear relationship at the range of 0.06-1.2 microg. The average recovery was 97.0%, and the RSD was 1.4%.</p><p><b>CONCLUSION</b>The method is simple, accurate, and can be used for its quality control.</p>
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Chromatography, High Pressure Liquid , Methods , Iridoids , Medicine, Tibetan Traditional , Plants, Medicinal , ChemistryABSTRACT
The intestinal absorption of aloe-emodin was investigated using the single pass intestinal perfusion (SPIP) technique in S/D rats. SPIP was performed in each isolated segment of the intestine (i.e., duodenum, jejunum, ileum and colon) and the different concentrations inhibitor group of P-glycoprotein (P-gp) and multidrug resistance-associated protein (MRP2) with the concentrations of aloe-emodin (0.238 mg x L(-1)) at a flow rate of 0.28 mL x min(-1). The effective absorption rate constant (Ka) and apparent absorption coefficient (Papp) of aloe-emodin for each segment were determined before and after treated with different concentrations of inhibitors of P-gp and MRP2 respectively. Aloe-emodin exhibits a high intestinal permeability except the the ileum, indicative that the compounds are well absorbed. Decreases of Ka and Papp values in the duodenum, jejunum, colon and ileum, furthermore, the duodenum has significant increased compared with the ileum, there are have no significant difference in other isolated region of the intestine. Compared with the group which have no inhibitor of P-gp, the Ka and Papp were significantly increased in inhibitor of P-gp groups. Compared with the group of no inhibitor of MRP2, the Ka and Papp were significantly increased in inhibitor of MRP2 groups with the highest and the middle concentration. The results suggested that the inhibitors of P-gp and MRP2 all can promote the intestinal absorption of aloe-emodin.
Subject(s)
Animals , Female , Humans , Male , Rats , Anthraquinones , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , Intestinal Absorption , Intestines , Chemistry , Metabolism , Perfusion , Methods , Permeability , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To observe the impact of Rhizoma Coptidis (drug-chemical extract parts-components) on 3T3-L1 pre-adipocytes differentiation and adipocytes insulin resistance, and reveal the pharmacodyamic material basis of Rhizoma Coptidis on insulin resistance.</p><p><b>METHOD</b>3T3-L1 pre-adipocytes were well cultured, and then induced to differentiate into fat cells by using dexamethasone, 3-isobutyl-1-methyl-xanthine and insulin together, and establish the insulin resistance model. Based on the experience of traditional medicine use, the adipocytes differentiation and the glucose consumption in the cell culture medium were observed independently.</p><p><b>RESULT</b>Aqueous extract, different chemical extract fraction and different alkaloid extract from the herb showed inhibitory effects on 3T3-L1 pre-adipocytes differentiation, especially the compound coptisine significantly inhibited the differentiation in the concentration of 16.5 micromol x L(-1), but non-alkaloid extract from the herb promoted cell differentiation significantly in the concentration of 6.0 micromol x L(-1). Each treatment group, especially jatrorrhizine hydrochloride (in the concentration of 10.5 micromol x L(-1)) significantly decreased the concentration of glucose in 3T3-L1 adipocytes culture, at the same time improved insulin resistance. These effects are similar to the role of rosiglitazone maleate.</p><p><b>CONCLUSION</b>Rhizoma Coptidis significantly improved insulin resistance, prevented pre-adipocytes differentiation. Its efficacy may be the synergistic effect of various components. Meanwhile, its role in inhibiting differentiation of pre-adipocytes indicates that coptis to increasing glucose uptake dose not cause fat accumulation and weight increasing. This has some clinical significance in the insulin resistance and metabolic syndrome.</p>