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1.
To synthesize and characterize a novel metal complex of Mn (Ⅱ) with emodin, and evaluate its anti-cancer activity. The elemental analyses, IR, UV-vis, atomic absorption spectroscopy, TG-DSC, ^1H NMR, and ^13C NMR data were used to characterize the structure of the complex. The cytotoxicity of the complex against the human cancer cell lines HepG2, HeLa, MCF-7, B16, and MDA-MB-231 was tested by the MTT assay and flow cytometry. Emodin was coordinated with Mn(Ⅱ) through the 9-C=O and 1-OH, and the general formula of the complex was Mn(Ⅱ) (emodin)2.2H/O. In studies of the cytotoxicity, the complex exhibited significant activity, and the IC50 values of the complex against five cancer cell lines improved approximately three-fold compared with those of emodin. The complex could induce cell morphological changes, decrease the percentage of viability, and induce G0/G1 phase arrest and apoptosis in cancer cells. The coordination of emodin with Mn(Ⅱ) can improve its anticancer activity, and the complex Mn(Ⅱ) (emodin)2.2H2O could be studied further as a promising anticancer drug.  相似文献   

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AIM: Ursolic acid (UA), a pentacyclic triterpenoid, is used as an anti-inflammatory and anti-cancer agent. There were few studies on the effects of UA on differentiation, and this is the first time to elucidate the potential effect and molecular mechanism of UA on inducing differentiation in the human leukemia cell line U937. METHODS: Wright-Giemsa staining, nitroblue tetrazolium reduction assay and flow cytometric analysis were utilized to demonstrate the differentiation of U937 cells induced by UA. Western blotting and immunofluorescence assay were used to investigate the possible mechanism. RESULTS: It was found that UA could induce the differentiation of U937cells and Akt-activity was significantly increased during differentiation. Additionally, LY294002, a PI3K-Akt inhibitor, could block the differentiation of U937 cells induced by UA. CONCLUSION: UA could induce the differentiation of U937 cells by activating the PI3K/Akt pathway, and it could be a potential candidate as a differentiation-inducing agent for the therapy of leukemia.  相似文献   

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AIM: The aim of the work is to study the pyrolysis characteristics of Radix Rhizoma Rhei, Cortex Moudan Radicis, and Radix Sanguisorbae in an inert atmosphere of argon (Ar), and to investigate the mechanism of the carbonizing process of the three traditional Chinese herbs. METHODS: The pyrolysis characteristics of the crude materials and their extracts were studied by thermogravimetry-mass spectrometry (TG-MS) in a carrier gas of argon, coupled with Fourier transform infrared spectrometry (FTIR) and scanning electron microscopy (SEM) methods. Correlation of the pyrolysis behaviors with the carbonizing process by stir-frying of traditional Chinese medicines was made. RESULTS: Within the temperature range of 200-300 ℃, which is the testing range for the study of the carbonizing process of Chinese herbs, the temperatures indicated by the maximum weight loss rate peak of the above three extracts were taken as the upper-limit temperatures of the carbonizing process of the herbs, and which were 200, 240 and 247 ℃ for Radix Rhizoma Rhei, Cortex Moudan Radicis, and Radix Sanguisorbae, respectively. The ion monitoring signal peaks detected by the TG-MS method corresponded with reports that the level of chemical components of traditional Chinese medicinal materials would decrease after the carbonizing process. It was confirmed by Fourier transform infrared spectrometry (FTIR) and scanning electron microscopy (SEM) methods that better results of "medicinal property preservation" could be obtained by heating at 200 ℃ for Radix Rhizoma Rhei, at about 250 ℃ for Cortex Moudan Radicis, and Radix Sanguisorbae, as the relative intensity values of the common peaks were among the middle of their three carbonized samples by programmed heating. CONCLUSION: The upper-limit temperatures of the carbonizing process for Radix Rhizoma Rhei, Cortex Moudan Radicis and Radix Sanguisorbae were 200, 240 and 247 ℃ respectively. It is feasible to research the mechanism and technology of the carbonizing process of traditional Chinese medicinal materials using thermogravimetry, Fourier transform infrared spectrometry, and scanning electron microscopy methods.  相似文献   

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OBJECTIVE: To evaluate clinical articles published in the past 30 years using the Traditional Chinese Medicine(TCM) theory of the lung being connect- ed with large intestine to treat intestinal diseases. We also analyzed the relationship between symp- toms, drugs and therapies with data-excavating technology to aid management. METHODS: After retrieving relevant clinical arti- cles, we set up a database, used Microsoft Struc- tured Query Language Server 2005 Analysis Ser- vices as a data-excavating tool, and applied the association rule to study the relationship between the symptoms, drugs and therapies of intestinal diseases.RESULTS: The key symptoms of dyschesia, consti- pation, abdominal fullness, fatigue and pale tongue could be treated with Kuxingren(Semen Ar- meniacae Amarum), Huangqi(Radix Astragali Mon- golici) and Gualou(Fructus et Semen Trichosanthis) to invigorate Qi and moisten the intestine. Among these agents, Kuxingren(Semen Armeniacae Amarum) was used most frequently. Clearing Fu-or- gans was the most prevalent therapy for abdomi- nal fullness, dyschesia, constipation and red tongue. Clearing Fu-organs could be achieved with Kuxingren(Semen Armeniacae Amarum) and Gua- lou(Fructus et Semen Trichosanthis), whereas Qi could be invigorated using Huangqi(Radix Astraga- li Mongolici), Gancao(Radix Glycyrrhizae), Baizhu(Rhizoma Atractylodis Macrocephalae) and Kuxin- gren(Semen Armeniacae Amarum). Moistening the intestine was possible with Kuxingren(SemenArme- niacae Amarum), Huomaren(Fructus Cannabis) and Jiegeng(Radix Platycodi). Also, moistening the lungs was done with Kuxingren(Semen Armeniacae Amarum), ventilating the lungs with Kuxingren(Se- men Armeniacae Amarum) and Gualou(Fructus et Semen Trichosanthis), and nourishing the lungs with Huangqi(Radix Astragali Mongolici), Gancao(Radix Glycyrrhizae) and Kuxingren(Semen Armenia- cae Amarum). These data demonstrated that Kuxin- gren(SemenArmeniacaeAmarum) was a key agent. CONCLUSION: Our analyses of the literature showed clear relationships between symptoms(constipation, dyschesia, abdominal fullness), drugs [Gualou(Fructus et Semen Trichosanthis), Kuxingren(Semen Armeniacae Amarum), Huangqi(Radix As- tragali Mongolici)] and therapies(moistening the in- testine, clearing Fu-organs, invigorating Qi, ventilat- ing the lungs).  相似文献   

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AIM: To investigate the molecular signaling mechanism by which the plant-derived, pentacyclic triterpene maslinic acid (MA) exerts anti-diabetic effects. METHOD: HepG2 cells were stimulated with various concentrations of MA. The effects of MA on glycogen phosphorylase a (GPa) activity and the cellular glycogen content were measured. Western blot analyses were performed with anti-insulin receptor β (IRβ), protein kinase B (also known as Akt), and glycogen synthase kinase-3β (GSK3β) antibodies. Activation status of the insulin pathway was investigated using phospho-IRβ, as well as phospho-Akt, and phospho-GSK3β antibodies. The specific PI3-kinase inhibitor wortmannin was added to the cells to analyze the Akt expression. Enzyme-linked immunosorbent assay (ELISA) was used to measure the effect of MA on IRβ auto-phosphorylation. Furthermore, the effect of MA on glycogen metabolism was investigated in C57BL/6J mice fed with a high-fat diet (HFD). RESULTS: The results showed that MA exerts anti-diabetic effects by increasing glycogen content and inhibiting glycogen phosphorylase activity in HepG2 cells. Furthermore, MA was shown to induce the phosphorylation level of IRβ-subunit, Akt, and GSK3β. The MA-induced activation of Akt appeared to be specific, since it could be blocked by wortmannin. Finally, MA treatment of mice fed with a high-fat diet reduced the model-associated adiposity and insulin resistance, and increased the accumulated hepatic glycogen content. CONCLUSION: The results suggested that maslinic acid modulates glycogen metabolism by enhancing the insulin signaling pathway and inhibiting glycogen phosphorylase.  相似文献   

7.
AIMS: To develop an HPLC-MS/MS method for the quantification of platycodin D (PD) in rat plasma, and to acquire the main pharmacokinetic parameters of PD after oral administration of pure PD or of Platycodi Radix extract (PRE) containing PD. METHOD: Plasma samples were pretreated with solid-phase extraction using an Oasis HLB SPE cartridge. Madecassoside was used as the internal standard (IS). Chromatographic separation was achieved on an ODS column (100 mm x 2.1 mm i.d., 3.5 μm) with a mobile phase consisting of acetonitrile/water (30 : 70, V/F) containing 0,1 mmol·L-1 ammonium acetate at a flow rate of 0.25 mL.min-1. The detection was performed on a triple quadruple tandem mass spectrometer using an electros- pray ionization (ESI) source with a chromatographic rtm time of 3.0 rain. The detection was operated by multiple reaction monitoring (MRM) of the transitions of m/z 1 223.6→469.2 for PD and of m/z 973.6→469,2 for madecassoside (IS), respec- tively. RESULTS: The calibration curve was linear from 5 to 2 000 ng.mL-1 (re 〉0.99) with a lower limit of quantification (LLOQ) of 5 ng.mL^-1. The intra- and inter-day precision (relative standard deviation, RSD) values were below 15% and the accuracy (relative error, RE) was from -15% to +15% at three quality control (QC) levels. Plasma concentrations of PD were deter- mined for 24 h after i.v. administration of PD, and oral administration of PD and PRE, respectively. The absolute oral bioavailability of PD in rats was found to be (0.48 ± 0.19)% when administered PD, and to be (1.81 ± 0.89)% when adminis- tered PRE. CONCLUSION: The developed HPLC-MS/MS method was successfully applied to assess the pharmacokinetic parameters and oral bioavailability of PD in rats after administration of PD and Platycodi Radix extract.  相似文献   

8.
Objective: To explore the influence of charred Gossamer urocteae (CGU) on the functions of primary cultured mouse oral fibroblasts and reveal its mechanism in wound healing. Methods: CGU was extracted with different solvents and ethanol extract (EE), ethyl acetate fraction (EF), n-butanol fraction (BF) and aqueous fraction (AF) were obtained. The effects of different fractions on the proliferation, matrix metaUoproteinase-2,9 (MMP-2,9) activities, synthesis of collagen and tissue inhibitor of metalloproteinase 1 (TIMP-1) in the mouse oral fibroblasts were determined by MTT, gelatin zymography, chloramine-T method, and enzyme-linked immunosorbent assay (ELISA) respectively. Results: EE, EF and BF at high concentrations could significantly inhibit proliferation of fibroblasts (P〈0.05 or P〈0.01), and at low concentrations EF and BF could promote proliferation of fibroblasts, and BF and AF could significantly inhibit collagen synthesis (P〈0.05 or P〈0.01). EE, EF and AF at high concentrations could significantly increase the MMP-9 activity, and BF and AF could significantly inhibit synthesis of TIMP-1. Conclusion: CGU at high concentrations can inhibit the proliferations of fibroblasts and synthesis of collagen, and in healing of wound, CGU at high concentrations possibly has the functions of anti-fibrosis and anti-scar, and the mechanism to promote degradation of collagen is possibly related to the increase in MMP-9 activity and the inhibition of TIMP-1 synthesis.  相似文献   

9.
OBJECTIVE: To investigate a quantitative method for using radial artery pulse waveforms to assess the effect of pulsatile flow during cardiopulmonary bypass(CPB).METHODS: A total of 34 adults with heart disease who underwent open-heart surgery between April2010 and January 2011 were randomized into a pulsatile perfusion group(n=17) and a non-pulsatile perfusion group(n=17). Radial arterial pulse waveforms of pulsatile and non-pulsatile perfusion patients were observed and compared before and during CPB.RESULTS: No pulse waveform could be detected at patients' radial artery in both groups when the aorta was cross-clamped. Pulse waveforms could be detected at pulsatile perfusion patients' radial artery, but could not be detected at non-pulsatile perfusion patients' radial artery during CPB. Additionally, patients' pulse waveforms during pulsatile perfusion were lower than those before the operation.CONCLUSION: Our findings indicate that radial artery sphygmogram can be used as a valid indicator to evaluate the effectiveness of pulsatile perfusion during CPB.  相似文献   

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Objective To evaluate the content of rhaponticin and anti-oxidative activities of theethanol extracts from both the wild plants and suspension cell cultures of Rheum franzenbachii.Methods Quantitative analysis of rhaponticin was performed by HPLC.The anti-oxidative activities of the ethanol extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl(DPPH)scavenging assays.Results The content of rhaponticin in the roots of the wild plant was 4.36 mg/g,while the content was only 1.59 mg/g in the leaves.The content of rhaponticin in suspension cells cultured on Murashige and Skoog(MS)medium supplemented with 1.0 mg/L 6-benzylaminopurine(6-BAP)and 2.0 mg/L 2,4-dicholorophenoxy acetic acid(2,4-D)was 17.64 mg/g,which increased by 4.05 times compared with the content in the roots of the wild plants.The roots of wild plants displayed the strongest anti-oxidative activity,followed by thesuspension cells 5 and 6,and the scavenging percent was 91.96%,91.23%,and 89.27%,respectively,at the concentration of 100μg/mL.The IC50 values were 2.477,15.644,and 31.415μg/mL,respectively.In particular,the DPPH scavenging activity of the ethanol extracts from the roots of the wild plant was generally comparable to the control of ascorbic acid(VC),and the IC50 value of the extracts was lower than that of VC(2.502μg/mL).Conclusion Rhaponticin production in the cell culture can be modulated and the accumulation can be increased.The roots of the wild plant display the strongest anti-oxidative activity.These results suggest that R.franzenbachii could hold a good potential source for human health.  相似文献   

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OBJECTIVE: To probe insights into the reversal effect of bufalin on vincristine-acquired multidrug resistance(MDR) in human leukemia cell line K562/VCR.METHODS: Proliferative inhibition rate and the reversal index(RI) of bufalin were determined by Methyl thiazolyl tetrazolium assay. The uptake of Adriamycin(ADM) in K562/VCR cells, cell cycle and apoptosis rate were determined by flow cytometry(FCM). Cell morphologic changes were observed with Wright-Giemsa staining. The expression of P-glycoprotein(P-gp), multidrug-associated protein-1(MRP1), Bcl-x L and Bax protein were measured by immunocytochemistry.RESULTS: The human leukemia multidrug resistant K562/VCR cells showed no cross-resistance to bufalin. The RIs of bufalin at concentrations of 0.0002,0.001 and 0.005 μmol/L were 4.85, 6.94 and 14.77,respectively. Preincubation of 0.001 μmol/L bufalin for 2 h could increase intracellular ADM fluorescence intensity to 28.07%(P〈0.05) and down-regulate MRP1 expression simultaneously, but no remarkable effect was found on P-gp protein. Cell cycle analysis indicated increased apoptosis rate and apparent decreased G2/M phase proportion after treatment with bufalin. When exposed to 0.01μmol/L bufalin, typical morphological changes of apoptosis could be observed. Down-regulation of Bcl-x L and up-regulation of Bax expression in K562/VCR cells could be detected by immunocytochemistry.CONCLUSION: Bufalin could partly reverse the MDR of K562/VCR cells, with a possible mechanism of down-regulating MRP1 expression and activating apoptosis pathway by altering Bcl-x L/Bax ratio.  相似文献   

13.
OBJECTIVE: To analyze the essential oils from flowers, leaves, stems, roots, and fruits of Chaihu(Radix Bupleuri Chinensis).METHODS: We extracted essential oils from different parts of Chaihu(Radix Bupleuri Chinensis) using a steam distillation method. The essential oils were analyzed by gas chromatography-mass spectrometry(GC-MS). Data were collected in full scan mode(m/z 60-600). Volatile components were identified based on their retention indices and by comparing their mass spectra with those in the National Institute of Standards and Technology 2005 database assisted by tandem mass spectrometry information. The relative content of each constituent wasdetermined by area normalization.RESULTS: We identified 111 components, of which12 were common to all 5 parts, 30 were found only in roots, 14 were found only in flowers, 6 were found only in leaves, 4 were found only in stems,and 17 were found only in fruits.CONCLUSION: Our results show that the stems,flowers, leaves, and fruits of Chaihu(Radix Bupleuri Chinensis)contain a high concentration of essential oils, and that the exact composition of the essential oils differs among the plant parts. To develop new medicines and make full use of the Chaihu(Radix Bupleuri Chinensis)resource, it is important to characterize the essential oils from different parts of the plant. In future research, it will be important to determine the pharmacological effects of the various components and the essential oil mixtures.  相似文献   

14.
Objective: To establish a new and better model to investigate the properties of mast cells that could be involved in acupuncture process mechanisms. Methods: Connective tissue under the corium at the area of acupuncture point Zusanli (ST 36) from rat was acutely bluntly separated with forceps and scissors, and incubated in bath solution up to several hours. Mast cells in slices of that tissue were irradiated with laser light of 650 nm, and changes in the appearance were observed under microscope. In addition, patch-clamp technique in whole-cell configuration was employed to induce mechanosensitive currents by pressure applied through the patch pipette. Results: 1) A high density of mast cells embedded in the extracellular matrix was detected in the tissue slices using toluidine blue staining. The mast cells survived for up to several hours;  相似文献   

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Objective: The aim of this study is to evaluate the efficacy of Traditional Chinese Medicine (TCM) in the treatment of rash caused by epidermal growth factor receptor inhibitors (EGFRIs). Materials and Methods: Foreign language database (such as PubMed, Web of Science, Cochrane Library, EMBASE) and Chinese language database (such as China National Knowledge Infrastructure, VIP Database for Chinese Technical Periodicals [VIP], Wangfang, CBM disc) were searched for all trials of TCM in the treatment of rash caused by EGFRIs until January of 2019. We also looked through the references of relevant studies to supplement additional trials. The SPSS 25.0 was used for statistics of TCM with high frequency, and Review Manager 5.3 was used for meta-analysis. Results: A total of 22 studies were included in the study. We selected TCM whose frequency were >3.0%. They were Lonicera japonica(金银花), Licorice Roots Northwest Origin(生甘草), Cortex Dictamni(白鲜皮), Radix Sophorae Flavescentis(苦参), Schizonepeta(荆芥), Saposhnikovia Divaricate(防风). The meta?analysis revealed that the efficacy of TCM in treating EGFRIs?related rash was better than that of Western medicine or none. Conclusions: TCM could significantly relieve rash caused by EGFRIs, which is worth popularizing. Moreover, the mechanism deserves to be further explored.  相似文献   

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OBJECTIVE: To study antimicrobial effect of Sodi- um houttuyfonate (SH) on Staphylococcus epider- midis (SE) and Candida albicans (CA). METHODS: The prepared strain broths (OD600=0.05) containing SE and CA were firstly used to test the minimal inhibitory concentrations (MICs) of SH, azithromycin (AZM) and fluconazole (FLU) by mi- cro-dilution method. Then the biofilms of SE and CA were matured in 96-well plates, and co-cultured with SH, AZM and FLU for 1, 2 and 3 days to assess the antibiofilm efficacies of the agents with differ- ent concentrations by crystal violet staining meth- od. At last, the treated biofilms of SE and CA by 2× MIC agents were observed by scanning electronic microscope. RESULTS: The MlCs of SE and CA were 256 and 1024 μg/mL, respectively. After the 1st, 2nd and3rd day of medications, the suppressions of biofilm were about 60% (P〈0.01), 76% (P=0.000) and 75% (P=0.000) by 2×MIC SH, the suppressions of biofilm were about 90% (P=0.000), 88% (P=0.000) and 90% (P=0.000) by 2×MIC SH, which could be testified by scanning electron microscope results. However, the inhibitions of biofilm attachment had no significant difference for SE by SH and azithromycin and CA by SH and fluconazole. CONCLUSION: SH had widely anti-pathogenic ef- fect on pathogenic biofilm formation of either bac- teria or fungus, had more influence on enclosed cells of SE and CA than the traditional antibiotics, revealing its target might be the extracellular poly- meric substances, and was more active to inhibit the growth of CA than SE.  相似文献   

18.
OBJECTIVE: To investigate metabolic signatures in plasma of cancer patients with abnormal Savda using plasma-free amino acid profiles, and to evaluate the diagnostic potential of these profiles for the detection and explanation of the mechanisms of different symptoms in traditional Uyghur medicine.METHODS: Plasma samples from cancer patients with abnormal Savda(n=85) or non-abnormal Savda(n=105) and a healthy control group(n=65)were analyzed using high-performance liquid chromatography(HPLC). Orthogonal projection to latent structures with discriminant analysis was used for the classification and prediction of abnormal Savda, and spectral profiles were subjected to Student's t-tests to assess statistical significance.RESULTS: Compared with the healthy group, the levels of aspartic acid, glutamate, glycine, histidine,arginine, threonine, alanine, proline, methionine,isoleucine, leucine and phenylalanine decreased significantly in plasma of cancer patients with abnormal Savda(all P〈0.05). Serine, cystine, tyrosine,valine and lysine levels showed no significant differences(all P〉0.05). Compared with non-abnormal Savda syndrome patients, abnormal Savda syndrome patients showed high concentrations of glutamate, serine, valine, isoleucine, leucine and phenylalanine(all P〈0.05). The remaining plasma amino acids showed no significant differences(all P〉0.05).CONCLUSION: Plasma-free amino acid profiling has the potential to assist in understanding and determining abnormal Savda. A HPLC-based metabonomic platform could be a powerful tool for the classification of symptoms in traditional medicine.  相似文献   

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Objective:To search for specific metabolites in the lungs of pneumonia rats fed with a high-calorie diet,as well as explore the changes in the lung metabolites of young rats treated with Yinlai Decoction(YD)and its effects on inflammation-related metabolic pathways.Methods:Lipopolysaccharides(LPS)and a special high-calorie diet were used to induce Sprague Dawley(SD)rats to simulate the intestinal state of infant pneumonia.Liquid chromatography-mass spectrometry technology(LC-MS/MS)was used to detect metabolites in each group.Supervised orthogonal partial least squares discriminant analysis(OPLS-DA)model values were used for the detection results to find the differential metabolites.The metabolic pathways that are involved with the differential metabolites were clarified through enrichment analysis and topological analysis.Finally,the T cell receptor signaling pathway(TCR)signal conversion was analyzed by the network pharmacology method.Results:In the high-calorie diet combined with pneumonia group(M3),a total of 55 metabolites were determined to be different from the normal group(N).A total of 36 metabolites were determined to be different from those in the lung metabolites of the YD treatment group(T1).YD had a regulatory effect on glutathione metabolism,arginine and proline metabolism,ascorbic acid and aldehyde metabolism and phenylalanine metabolism.And the small molecule metabolites could act on the FYN and lymphocytespecific protein tyrosine kinase(LCK)target proteins in the TCR signaling pathway,thereby affecting the immune function of the lungs.Conclusion:A high-calorie diet can cause abnormal sphingolipid metabolism in the lungs of young rats,thereby creating chronic lung inflammation in young rats.YD has a beneficial effect when used to treat young rats with LPS-induced pneumonia fed on high-calorie diets.Its mechanisms of action may affect the body’s immune pathways by regulating the oxidative stress pathway affected by glutathione metabolism.  相似文献   

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Objective To establish a RP-HPLC method investigate the processing technique and mechanism of Eucommiae Cortex.Methods The RP-HPLC method was applied to simultaneously determining six ingredients,geniposidic acid,geniposide,genipin,chlorogenic acid,(+)-pinoresinol-di-β-D-glucopyranoside,and(+)-syringaresinol-di-β-D-glucopyranoside,in the different processed barks of Eucommia ulmoides.Results The valid method with good accuracy could be well used to study the processing technique of E.ulmoides;Besides,target ingredients in E.ulmoide were decreased within 6 h when they were processed.Conclusion Established RP-HPLC is a reliable method which could be used to research the processing technique of the barks of E.ulmoides.Moreover,the result of this study could be provided with significant evidence of processed barks of E.ulmoides.  相似文献   

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