Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 200
Filter
1.
International Eye Science ; (12): 21-26, 2021.
Article in Chinese | WPRIM | ID: wpr-837709

ABSTRACT

@#AIM: To investigate the protective effect and mechanism of luteolin on H2O2-induced oxidative damage of retinal pigment epithelium(RPE)cells. <p>METHODS:ARPE-19 cells were divided into the control group, H2O2 group, different doses of luteolin groups and Nrf2 inhibitor group, and the oxidative damage model of RPE was prepared by 100μmol/L H2O2, except for the control group. Cell activity was detected by Methyl thiazolyl tetrazolium(MTT)assay and proper experimental concentration of luteolin was determined. The cell morphology and activity was observed in each group. Cell apoptosis rate and reactive oxygen species(ROS)were detected by flow cytometry, malondialdehyde(MDA)and superoxide dismutase(SOD)were detected by kit method, and the expression of caspase-3, poly adeno-sine diphosphate ribose polymerase(PARP), B cell lymphoma-2(Bcl-2), nuclear factor erythroid 2-related factor 2(Nrf2)and heme oxygenase-1(HO-1)proteins were detected by Western blot. <p>RESULTS: 100μmol/L luteolin has toxic effects on ARPE-19 cells, so 25μmol/L and 50μmol/L luteolin were selected for subsequent experiments. The cell activity, SOD activity and the protein expression levels of Bcl-2, Nrf2, HO-1 in 25μmol/L and 50μmol/L luteolin groups were significantly higher than the H2O2 group(<i>P</i><0.05). The apoptosis rate, ROS, MDA content and the protein expression levels of Caspase-3 and PARP in 25μmol/L and 50μmol/L luteolin groups were significantly lower than the H2O2 group(<i>P</i><0.05). The cell activity, SOD activity \〖(13.83±1.49)U/mL <i>vs</i>(22.69±1.83)U/mL\〗 and the protein expression levels of Bcl-2, Nrf2 and HO-1 protein expression in the Nrf2 inhibitor group were significantly lower than the 50μmol/L luteolin group(<i>P</i><0.05). The apoptosis rate, ROS, MDA content \〖(654.96±26.99)<i>vs</i>(446.52±29.42),(3.89±0.29)nmol/mL <i>vs</i>(2.06±0.19)nmol/mL\〗 and the protein expression levels of Caspase-3 and PARP in the Nrf2 inhibitor group were significantly higher than the 50μmol/L luteolin group(<i>P</i><0.05).<p>CONCLUSION: Luteolin can improve the oxidative damage of RPE cells induced by H2O2, and its mechanism may be related to the activation of the Nrf2/HO-1 pathway.

2.
Article in Chinese | WPRIM | ID: wpr-921751

ABSTRACT

The aim of this study was to investigate the mechanism of luteolin regulating lipoxygenase pathway against oxygen-glucose deprivation/reperfusion(OGD/R) injury in H9 c2 cardiomyocytes. First, Discovery Studio 2019 was used for the molecular docking of luteolin with three key enzymes including lipoxygenase 5(ALOX5), lipoxygenase 12(ALOX12), and lipoxygenase 15(ALOX15) in lipoxygenase pathway. The docking results showed that luteolin had high docking score and similar functional groups with the original ligand. From this, H9 c2 cardiomyocytes were cultured in vitro, and then the injury model of H9 c2 cardiomyocytes was induced by deprivation of oxygen-glucose for 8 h, and rehabilitation of oxygen-glucose for 12 h. Cell viability was detected by tetrazolium(MTT) colorimetry. H9 c2 cardiomyocytes were observed with a fluorescence inverted microscope, and colorimetry was used to detect the level of lactate dehydrogenase(LDH) in cell supernatant. The results showed that luteolin could significantly protect the morphology of H9 c2 cells, significantly improve the survival rate of H9 c2 cardiomyocytes in OGD/R injury model, reduce the level of LDH in cell supernatant, inhibit cytotoxicity, and maintain the integrity of cell membrane. The inflammatory cytokines interleukin-6(IL-6) and tumor necrosis factor-α(TNF-α) were detected by enzyme-linked immunosorbent assay. Compared with the model group, luteolin can significantly reduce the release of IL-6 and TNF-α. Western blot was employed to detect the protein levels of ALOX5, ALOX12, and ALOX15 in lipoxygenase pathway. After luteolin intervention, the protein levels of ALOX5, ALOX12, and ALOX15 were significantly down-regulated compared with those in model group. These results indicate that luteolin can inhibit the release of IL-6 and TNF-α by restraining the activation of lipoxygenase pathway, thereby playing a protective role in the cardiomyocyte injury model induced by OGD/R.


Subject(s)
Apoptosis , Glucose , Humans , Lipoxygenases , Luteolin/pharmacology , Molecular Docking Simulation , Myocytes, Cardiac , Oxygen , Reperfusion Injury , Signal Transduction
3.
Article in Chinese | WPRIM | ID: wpr-888012

ABSTRACT

Isomers are widely distributed in Chinese herbal medicines,and can be discriminated by energy-resolved mass spectrometry( ER-MS). However,ER-MS was performed through direct injection of reference compounds with syringe pump,which encountered a significant technical barrier for high-throughput and automated measurements. Herein,online ER-MS was conducted using LC-MS platform,and a pair of isomers,kaempferol vs luteolin,were employed as a case study to illustrate and assess the utility of online ER-MS for isomeric discrimination. High-resolution tandem mass spectrometry data of both flavonoids were acquired on LC-QE-Orbitrap-MS,and the fragmentation pathways responsible for the primary fragment ions were proposed. The primary signal in MS1 occurred at m/z 285( [M-H]-),and the primary signals of either compound generated by retro-Diels-Alder fragmentation were observed at m/z 151 and 133. The spectral information was subsequently transferred onto LC-Qtrap-MS platform to carry out online ER-MS. Two precursor-to-product ion transition candidates were constructed as m/z 285>151 and 285>133,and either afterward derived a set of pseudo-ion transitions( PITs) and so forth,exactly corresponding to a series of progressive collision energies( eg-5,-8,-11 e V,and so on). All PITs were typed into the monitoring list of multiple reaction monitoring program to generate the peak area datasets. Either dataset was normalized using the highest values in the set and imported into Graph Pad Prism software to plot the Gaus-sian-shaped curve that was termed as the break-down graph. The apex of the regressive curve was termed as optimal collision energy( OCE). The OCE values corresponding to m/z 285>151 were calculated as-29. 06 e V and-35. 71 e V for kaempferol and luteolin,respectively. In the case of m/z 285>133,the OCEs were yielded as-44. 15 e V for kaempferol and-49. 01 e V for luteolin. With re-ference to their chemical structures,the location of hydroxyl group was regarded to be responsible for the differences of either m/z 285>151 or 285>133 between the isomers,attributing to their different bond properties. Above all,online ER-MS offers an eligible tool for isomeric discrimination,and provides meaningful information for the accurate chemical composition characterization based on LC-MS,which is not limited to Chinese herbal medicines.


Subject(s)
Chromatography, Liquid , Flavonoids , Kaempferols , Luteolin , Tandem Mass Spectrometry
4.
Article in Chinese | WPRIM | ID: wpr-879141

ABSTRACT

To investigate the potential molecular mechanism of the combination of Platycodonis Radix and Lilii Bulbus with the homology of medicine and food in the treatment of pneumonia by means of network pharmacology and in vitro verification experiment. Under the condition of bioavailability(OB)≥30% and drug-like(DL)≥0.18, the active components of Platycodonis Radix and Lilii Bulbus were screened in TCMSP database; the prediction targets of active components were searched from TCMSP, DrugBank and other databases, and the potential targets of pneumonia were obtained through GeneCards and OMIM database. The common targets were obtained by the intersection of drug and disease targets. The PPI network of common targets was constructed by STRING 11.0, and the core targets were obtained by topological analysis. Then the core targets received GO and KEGG analysis with use of WebGestalt and Metascape. The "component-target-pathway" network was constructed with the help of Cytoscape 3.7.1 software, and the component-target molecular docking verification was carried out with Discovery Studio 2016 software. Finally, the core targets and pathways were preliminarily verified in vitro. In this study, 12 active components were screened, 225 drug prediction targets and 420 potential diseases targets were obtained based on data mining method, and 14 core targets were obtained by topological analysis, including TNF, MMP9, AKT1, IL4 and IL2. The enrichment results of GO and KEGG showed that "Platycodonis Radix and Lilii Bulbus" drug pair may regulate inflammation, cell growth and metabolism by acting on 20 key signaling pathways such as TNF and IL-17, thereby exerting anti-pneumonia effects. The results of molecular docking showed that 12 active components had good binding ability with 14 core targets. In vitro experiment results showed that the core components of "Platycodonis Radix and Lilii Bulbus" drug pair could inhibit the expression of MMP9 and TNF-α by regulating TNF signal pathway. This study confirmed the scientificity and reliability of the prediction results of network pharmacology, and preliminarily revealed the potential molecular mechanism of the compatibility of Platycodonis Radix and Lilii Bulbus in the treatment of pneumonia. It provides a novel insight on systematically exploring the mechanism of the compatible use of Platycodonis Radix and Lilii Bulbus, and has a certain reference value for the research, development and application of new drugs.


Subject(s)
Drugs, Chinese Herbal , Humans , Medicine, Chinese Traditional , Molecular Docking Simulation , Pneumonia/drug therapy , Reproducibility of Results
5.
Article in Chinese | WPRIM | ID: wpr-846688

ABSTRACT

Objective: To research the chemical constituents from Trigonella foenum-graecum. Methods: The chemical constituents were separated and purified by sephadex LH-20, silica gel, semi-prepared HPLC and other chromatography techniques. Their structures were elucidated by their physicochemical properties and NMR data. Results: Six steroidal saponins and flavonoids (1-6) were isolated from the ethanol extracts of T. foenum-graecum and identified as 22-methoxy-trigoneoside IIb (1), gitogenin (2), diosgenin (3), luteolin (4), cynaroside (5), and luteolin-7-O-rutinoside (6). Conclusion: Compound 1 is a new compound, and compounds 5 and 6 are obtained for the first time from T. foenum-graecum.

6.
Article in Chinese | WPRIM | ID: wpr-846570

ABSTRACT

Objective: To provide the theoretical basis for determining the best harvesting plant organ and harvesting period, and investigate the content of chemical constituents of Callicarpa nudiflora in different plant organs and different growth periods. Methods: The contents of total flavonoids, total phenolic acid and total saponins were determined by ultraviolet spectrophotometry, and the seven components were determined by HPLC. The ANOVA and PCA methods were used to analyze the content of each constituent. Results: The dry extract rate, the contents of total flavonoids, total phenolic acid, total saponins, forsythiaside B, acteoside, isoacteoside, and apigenin-7-O-β-D-glucopyranoside in functional leaves were the highest, while the contents of caffeic acid, galuteolin and luteolin in tender leaves were the highest, and all of them were significantly different from the young shoots (P 0.05). The contents of total phenolic acid, total saponins, forsythiaside B, and acteoside were the highest in the FB period, and there was no significant difference with the EFS period (P > 0.05). The contents of galuteolin and apigenin-7-O-β-D-glucopyranoside were the highest in the earlier fruit maturation (EFM) period and the later fruit maturation (LFM) period, respectively, and there was no significant difference with the EFS period (P > 0.05). The contents of each chemical component were reduced to the minimum at the fruit-drop (FD) period, and it was significantly different from that at the EFS period and the FB period (P < 0.05). According to the comprehensive evaluation model constructed by PCA, the comprehensive score of the EFS period was the highest (F = 3.252), followed by the FB period (F = 3.011). Conclusion: Main chemical constituents of C. nudiflora were significantly different in harvesting parts and growth periods. The contents of main chemical constituents were higher in functional leaves and tender leaves, and the contents of main chemical constituents were higher from FB period to EFS period.

7.
Article in Chinese | WPRIM | ID: wpr-846507

ABSTRACT

Objective: To explore the potential material basis of Kangbingdu Granules for the treatment of coronavirus disease 2019 (COVID-19) through network pharmacology and molecular docking technology. Methods: The chemical constituents and action targets of Isatidis Radix, Forsythiae Fructus, Gypsum Fibrosum, Anemarrhenae Rhizoma, Phragmitis Rhizoma, Rehmanniae Radix Praeparata, Pogostemon cablin, Acoritataninowii Rhizoma and Curcumae Radix in Kangbingdu Granules were searched by TCMSP. The gene corresponding to the target was searched by UniProt database, and Cytoscape 3.6.1 was used to build a medicinal material-compound-target (gene) network. DAVID was used to perform gene ontology (GO) function enrichment analysis and KEGG pathway enrichment analysis to predict its mechanism. Molecular docking of the top 15 components was carried out in the medicinal material-compound-target network with SARS-CoV-2 3CL hydrolase, and molecular docking with bicuculline, luteolin, quercetin and angiotensin-converting enzyme II (ACE2) was performed. Results: The medicinal material-compound-target (gene) network contained eight medicinal materials, 75 compounds and 255 targets. GO function enrichment analysis revealed 161 GO items (P < 0.05), including 65 biological process (BP) items, 36 cell composition (CC) items, and 60 molecular function (MF) items. KEGG pathway enrichment screened 131 signaling pathways (P < 0.05). The results of molecular docking showed that the core active compounds such as bicuculline, luteolin, and quercetin in the Kangbingdu Granules had similar affinities with those recommended by COVID-19. Conclusion: The active compounds in Kangbingdu Granules can interact with angiotensin-converting enzyme II (ACE2) via targets PTGS2, HSP90AB1, and PTGS1 to regulate multiple signaling pathways, thereby exerting therapeutic effects on COVID-19.

8.
Article in Chinese | WPRIM | ID: wpr-846483

ABSTRACT

Objective: To study the mechanism of Tanreqing Injection (TRQI) on treatment of coronavirus disease 2019 (COVID-19) through network pharmacology and molecular docking, so as to provide theoretical basis for clinical treatment. Methods: The active compounds of TRQI were searched by literature, BATMAN-TCM, and TCMSP database. The potential targets of TRQI active compounds were searched by TCMSP. In Genecards database, “coronavirus” was used as the key word to search for coronavirus targets and the common targets were selected by mapping with TRQI. The network between the active compounds and common targets was established by Cytoscape 3.2.1. The common targets were imported into a STRING database for protein-protein interaction analysis, and the target protein interaction network diagram (PPI) was constructed. The key antiviral targets of TRQI were screened by combining two networks. “GlueGO 2.5.5” plug-in unit in Cytoscape 3.2.1 was used to perform GO biological process and KEGG pathway enrichment analysis. Results: A total of 54 components of TRQI were obtained and corresponding to 287 targets. Among them, there were 54 common targets and 34 key targets. GO analysis obtained 29 biological processes related to the treatment effect of TRQI, and KEGG analysis obtained 70 pathways. The results of molecular docking showed that kaempferol, quercetin, baicalein luteolin, and wogonin had good affinity with SARS-CoV-2 3CL hydrolase. Conclusion: The active compounds in TRQI may act as an antiviral agent by binding SARS-CoV-2 3CL hydrolase and regulating multiple signaling pathways. The molecular mechanism of TRQI in the treatment of COVID-19 indicated the synergistic features of multi-component, multi-target, and multi-pathway of traditional Chinese medicine, which provided an important scientific basis for further elucidating the mechanism of TRQI in the treatment of COVID-19.

9.
Article in Chinese | WPRIM | ID: wpr-846479

ABSTRACT

Objective: To explore the active compounds of Maxingyigan Decoction for the treatment of coronavirus disease 2019 (COVID-19). Methods: The chemical constituents and action targets of Ephedra sinica, Armeniacae Semen Amarum, Coicis Semen, and Glycyrrhizae Radix et Rhizoma in Maxingyigan Decoction were retrieved from TCMSP. The database of UniProt and GeneCards were used to query the target genes that corresponding to the active compounds, and then a compound-target (gene) network was constructed by Cytoscape 3.6.1. GO functional enrichment analysis and KEGG enrichment analysis were performed through WebGestalt database to predict its mechanism of action. The main active ingredients were docked with SARS-CoV-2 3CL hydrolase and angiotensin converting enzyme II (ACE2). Results: The compound-target network contained 126 compounds and 266 corresponding targets. The key targets genes included PTGS2, ESR1, PCP4, PPARG, HSP90AA1, NCOA2, etc. GO function enrichment analysis found that 522 GO items were affected by Maxingyigan Decoction, including 12 biological process items, 20 cell composition items, and 17 molecular function items. KEGG enrichment analysis showed that 168 signal pathways were enriched, involving interferon-γ signaling pathway, MAP kinase cascade, T cell activation, chemokines and cytokine signaling pathway-mediated inflammation pathways, etc. The molecular docking results showed that core compounds such as luteolin and quercetin had similar affinity with the recommended drugs used to treat COVID-19. Conclusion: The active compounds in Maxingyigan Decoction may have a therapeutic effect on COVID-19 through binding with 3CL hydrolase and ACE2 to act on targets such as PTGS2, ESR1, PCP4, PPARG, HSP90AA1 and NCOA2 so as to regulate multiple signal pathways.

10.
Article in Chinese | WPRIM | ID: wpr-846477

ABSTRACT

Objective: To explore the active compounds and mechanism of Lianhua Qingwen Prescription for the treatment of coronavirus, and provide a reference for the treatment of COVID-19. Methods: With the help of TCMSP, Batman, Swiss Target Prediction and other databases, the chemical constituents and targets of Lianhua Qingwen Prescription were retrieved. Coronavirus disease targets were screened by GeneCards. Cytoscape software was used to construct a “drug-component-target-disease” interaction network map and potential target interactions, and the action mechanism was predicted through enrichment analysis. The main active ingredients of Lianhua Qingwen Prescription were verified by molecular docking with Mpro and ACE2. Results: A total of 100 active ingredients, 636 drug targets, and 347 disease targets were excavated, and 67 drug-disease common targets were obtained. The key targets involved PTGS2, IL6, CASP3, MAPK1, EGFR, ACE2, etc. A total of 1 946 entries were obtained by GO enrichment analysis, which mainly involved T cell activation, viral receptors, and inflammatory responses. KEGG pathway enrichment screened 166 signaling pathways, including renin-angiotensin system, Toll-like receptor signaling pathway, JAK-STAT signaling pathway, T cell receptor signaling pathway, TNF signaling pathway and so on. The molecular docking results showed that kaempferol, quercetin and luteolin had good binding ability with Mpro; And glycyrrhetinic acid, stigmasterol, indigo had good binding ability with ACE2. Conclusion: Lianhua Qingwen Prescription acts on coronavirus through multiple components, multiple targets, and multiple pathways. The main components have good binding ability with Mpro and ACE2, so as to have a therapeutic effect on COVID-19.

11.
Article in Chinese | WPRIM | ID: wpr-846476

ABSTRACT

Objective: To explore the active compounds of Feiduqing in the treatment of coronavirus disease 2019 (COVID-19) pneumonia. Methods: The Chinese medicine system pharmacology analysis platform (TCMSP) was used to obtain the three Chinese medicine-related components and targets of Oroxylum indicum, Gardenia jasminoides and Sophora flavescens of Feiduqing, and the genes corresponding to the targets were queried through the UniProt database. The STRING platform was used to build the target PPI network. DAVID was used to perform GO biological processes and KEGG pathway enrichment analysis was used to perform network topology analysis on core targets. Cytoscape 3.7.0 was used to construct a component-target network analysis to predict the mechanism of Feiduqing. The core active compound of Feiduqing was molecularly docked with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL hydrolase, and the first three compounds with the lowest binding energy were docked with angiotensin converting enzyme II (ACE2). Results: The component-target network included 269 nodes and 4 204 edges, including 50 components such as quercetin, beta-sitosterol, kaempferol, etc, and key targets included JUN, AKT1, TP53, PTGS2, FOS, ESR1, etc. The function enrichment analysis of GO yielded 2 187 (P < 0.05), including 1 877 biological process (BP) entries, 105 cellular components (CC) entries, and 205 molecular functions (MF) entries. Twenty-five signal pathways were screened by KEGG enrichment analysis (P < 0.05), mainly including hepatitis B, pathways in cancer, TNF signaling pathway, pancreatic cancer, toxoplasmosis pathway, etc. The active ingredients with the lowest molecular docking binding energy acting on SARS-CoV-2 3CL hydrolase were luteolin (-26.78 kJ/mol), quercetin (-26.36 kJ/mol), 8-prenyl-kaempferol (-25.94 kJ/mol). Conclusion: The active compound of Feiduqing may have a therapeutic effect on COVID-19 through the action on targets such as JUN, AKT1, TP53, PTGS2, FOS, ESR1, binding with angiotensin converting enzyme II (ACE2) and regulating many signaling pathways.

12.
Article in Chinese | WPRIM | ID: wpr-846414

ABSTRACT

Objective: Based on the concept of quality marker (Q-marker), the components and the quality of the ethyl acetate extract of Polygonum orientale (POEa) was analyzed and studied. Methods: Firstly, the components of POEa were identified using the UPLC-ESI-HRMS method and standard compounds. Secondly, the main active compounds were determined by HPLC. Antitumor activities of these compounds were reviewed and its Q-marker was predicted. Finally, we evaluated the effects of POEa and the compound of gallic acid, isoquercetin, valerin, vitexin, luteolin, and quercetin on proliferation, apoptosis and migration of A549 cells. Results: A new quality method for simultaneous determining these six compounds of POEa was established. The six chemical ingredients were detected in each sample and the total content was more than 10%. The number of apoptotic cells in A549 cells treated with POEa and six chemical mixtures were all substantial increased, and the migration amount were significantly decreased. Tow groups showed no significantly differeances. Conclusion: The six components are scientific and reasonable to be considered as potential Q-marker represented the anti-tumor activity of POEa. The HPLC method can be used as accurate and stable quality control strategy of POEa.

13.
Article in Chinese | WPRIM | ID: wpr-846394

ABSTRACT

Objective: To study the anti-fatigue mechanism of Epimedii Folium by network pharmacology. Methods: The main active ingredients of Epimedii Folium and the targets of active ingredients were obtained by TCMSP. The GeneCards was used to predict and screen the anti-fatigue targets. The Cytoscape 3.6.1 software was used to construct the active ingredient-disease-target network. The protein interactions network was constructed using the String database. The GO enrichment and KEGG pathways of the targets were analyzed by using DAVID database. Results: Nine active ingredients were screened from Epimedii Folium, including chrysoeriol, kaempferol, anhydroicaritin, C-homoerythrinan,1,6-didehydro-3,15,16-trimethoxy-,(3.beta.)-, 8-(3-methylbut-2-enyl)-2-phenyl- chromone, luteolin, magnograndiolide, quercetin, 8-isopentenyl-kaempferol, which acted on 31 fatigue targets such as PPARG, GABRA1, CASP3, ICAM1, etc. Biological function analysis showed that the targets of Epimedii Folium included cellular response to hypoxia, regulation of apoptotic, positive regulation of nitric oxide biosynthetic, cellular response to hydrogen peroxide, cellular response to hyperoxia, and negative regulation of lipid storage. Signaling pathway analysis showed that Epimedii Folium exerted the anti-fatigue effect by regulating PI3K-Akt, P53, HIF-1, TNF, FoxO, ErbB, MAPK, and other pathways. Conclusion: This study reflects the characteristics of multi-component, multi-target, and multi-pathway of Epimedii Folium, which provides reference for further research on the mechanism of anti-fatigue effects of Epimedii Folium.

14.
Article in Chinese | WPRIM | ID: wpr-846361

ABSTRACT

Objective: To probe active components of Scutellariae Barbatae Herba (SBH) and its underlying complex mechanism in treating pancreatic cancer based on network pharmacology and molecular experimental validation. Methods: Active compounds of SBH and potential targets of these compounds were screened via Traditional Chinese Medicine Systems Pharmacology (TCMSP) database. Then the pancreatic cancer target database was established by using Comparative Toxicogenomics Database (CTD), Therapeutic Target Database (TTD), and Pharmacogenomics Knowledgebase (PharmGKB). Based on the matching results between SBH potential targets and pancreatic cancer targets, a PPI network was structured and then the hub targets were screened by using topology analysis. Furthermore, DAVID bioinformatics was utilized for both Gene ontoloty (GO) functional enrichment analysis and KEGG pathway enrichment analysis. At last, Western blotting was used to validate the regulating function of luteolin on P53, Bax and Bcl-2 targets of PANC-1 cells. Results: A total of 28 active ingredients including quercetin, luteolin and wogonin were screened out, and 24 hub targets of 91 targets including TP53, AKT1, JUN and VEGF were obtained. The results of DAVID enrichment analysis indicated that 73 cellular biological processes and 18 pathways were found to participate in the treatment of pancreatic cancer, mainly involving in regulating inflammatory microenvironment, cell cycle arrest, pro-apoptosis and anti-angiogenesis through NF-κB, p53, PI3K-AKT and VEGF signal pathways. Luteolin from SBH was validated to regulate key targets in the p53 signaling pathway to play a role in pro-apoptosis, which proved the reliability of results of network pharmacology. Conclusion: This study confirmed the synergistic effect of multiple component-multiple target-multiple pathway of SBH on the treatment of pancreatic cancer, which offered a theory for its clinical application.

15.
Article in Chinese | WPRIM | ID: wpr-846276

ABSTRACT

Objective: To establish an UHPLC-MS/MS method for rapid and simultaneous determination of the content of 13 components in Ainsliaea fragrans. Methods: The UHPLC-MS/MS method was performed on UPLC BEH C18 (100 mm × 2.1 mm, 1.7 μm) with acetonitrile-water (containing 0.1% formic acid and 5 mmol ammonium formate) as mobile phase for gradient elution. Flow rate was 0.25 mL/min and column temperature was 40 ℃. A triple quadrupole mass spectrometer equipped with electrospray ionization source (ESI) was applied in negative ion mode with the following parameters: ion spray, -4 500 V, ion source temperature, 500 ℃, curtain gas, 344.5 kPa, nubulizer (GS1), 344.5 kPa, heater gas (GS2), 206.7 kPa, and multiple reaction monitoring (MRM) was performed for quantitative analysis of these compounds. Results: Under the optimized MS/MS condition, the linearity ranges of protocatechuic acid, caffeic acid, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, 1,3-dicaffeoylquinic acid, 1,5-dicaffeoylquinic acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 4,5-dicaffeoylquinic acid, luteolin, luteoloside and apigenin were 1.099-274.800 ng/mL, 1.006-100.600 ng/mL, 1.080-1 080.000 ng/mL, 83.12-8 312.00 ng/mL, 19.92-996.00 ng/mL, 1.076-269.000 ng/mL, 5.555-555.500 ng/mL, 4.420-4 420.000 ng/mL, 44.76-17 904.00 ng/mL, 48.00-9 600.00 ng/mL, 2.108-210.800 ng/mL, 4.136-413.600 ng/mL, 1.070-107.000 ng/mL (r ≥ 0.9958), respectively, with good linearity. The average recovery rate of thirteen compounds in the samples were in the range of 96.54%-99.75%, and the RSD range was from 0.48% to 0.96%. The RSD values of precision, stability and repeatability test were all less than 3.90%. Conclusion: The method had good repeatability, high specificity, stability and controllability, and could be used for quality control of A. fragrans and its preparations.

16.
Article in Chinese | WPRIM | ID: wpr-846139

ABSTRACT

Objective: To study the chemical constituents of the rhizomes of Schoenoplectus tabernaemontani. Methods: Compounds were isolated and purified by a combination of column chromatography including silica gel, polyamide and Sephadex LH-20. Their structures were elucidated by physiochemical properties and NMR analysis. Results: Twelve compounds were obtained from water extract of the rhizome of S. tabernaemontani and identified as 5,7,2',4'-tetrahydroxy-3, 5'-dimethoxyflavone (1), tricin (2), hesperetin (3), quercetin (4), luteolin (5), eriodictyol (6), apigenin (7), naringenin (8), chrysin (9), 5,7-dihydroxychromone (10), catechin (11) and tricin-7-O-β-D-glucoside (12), respectively. Conclusion: Compound 1 is a new flavone named schoenin. Compounds 2-5 and 7-12 are isolated from the Cyperaceae for the first time. Compound 6 is isolated from the genus Scirpus for the first time.

17.
Article in Chinese | WPRIM | ID: wpr-846043

ABSTRACT

Objective: To establish an ultra-high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry (UPLC-ESI-HRMS) determination method for simultaneous determination of 11 components from raw, wine-broiled, carbon-fried and steamed Rheum pumilum roots. Methods: The chromatographic separation was performed on a KinetexTM C18 column (150 mm × 4.6 mm, 2.6 μm) with a gradient elution of acetonitrile and 0.1% formic acid in water at flow rate 0.3 mL/min, the injection volume was 1 μL and column temperature was 32 ℃. The mass spectrometry was detected using ESI ion source and negative ion mode. Results: Eleven components gallic acid, epicatechin, polydatin, rhaponticin, luteolin, emodin-8-O-β-D-glucoside, aloe-emodin, rhein, emodin, chrysophanol and physcion showed a good linear relationship within a certain concentration range. The precision, repeatability and stability of the method were good for the determination of 11 components. The average recoveries varied between 91.31% and 107.08% and the RSD were between 1.73% and 3.58%. The content of gallic acid, polydatin, emodin-8-O-β-D-glucoside and emodin changed in processsed products of R. pumilum roots. The content of gallic acid and emodin increased significantly in the wine-broiled and carbon-fried process. The content of emodin-8-O-β-D-glucoside in the carbon-fried process was significantly reduced, and the content of polydatin was significantly reduced in all processed products. Conclusion: This determination method is simple, stable, accurate and reliable. It can be applied for rapid quantitative determination of 11 components in raw and processsed products of R. pumilum, which laid the foundation for further research on R. pumilum roots.

18.
Article in Chinese | WPRIM | ID: wpr-843046

ABSTRACT

@#To prepare and optimize luteolin nanostructured lipid carriers (Lut-NLCs) and investigate their antibacterial activity in vitro. Lut-NLCs were prepared by hot melt emulsification-ultrasonic method. The solid lipid concentration (X1),liquid lipid concentration (X2) and surfactant concentration (X3) were used as independent variables,with the average particle size (Y1) and the encapsulation efficiency (Y2) as the dependent variables. The optimal formulation of Lut-NLCs was obtained through Box-Behnken experiment design. The microstructure of Lut-NLCs was observed by transmission electron microscopy(TEM). The in vitro release characteristics of Lut-NLCs were investigated. Furthermore, the in vitro antibacterial activities of luteolin and Lut-NLCs were compared. The formulation composition of Lut-NLCs was optimized as follows:the concentration of the solid lipid, liquid lipid and surfactant were 13.0 mg/mL,15.0 mg/mL,and 15.0 mg/mL,respectively. Three batches of Lut-NLCs were prepared with an average particle size of (210.4±17.3) nm,and an encapsulation efficiency of (88.4±1.2)%. Lut-NLCs were observed to be spheroidal,with a smooth surface and a uniform particle size distribution by TEM. The drug release profiles of Lut-NLCs showed a bursting release in the early stage and a slow and stable release in the later stage. Moreover, the cumulative release amount of drug reached 95% in 12 hours. The results of antibacterial circle experiment showed that the antibacterial effect of Lut-NLCs on Staphylococcus aureus and Escherichia coli was higher than that of luteolin raw materials. In this study,the formulation of Lut-NLCs prepared by simple preparation process is reasonable,and Lut-NLCs also exhibited the significant in vitro antibacterial activity. It is expected to be an effective way for external application of luteolin.

19.
Article in English | WPRIM | ID: wpr-811391

ABSTRACT

BACKGROUND/OBJECTIVES: Non-small cell lung cancer is mostly recognized among other types of lung cancer with a poor prognosis by cause of chemotherapeutic resistance and increased metastasis. Luteolin has been found to decrease cell metastasis. However, its underlying mechanisms remain unresolved. The objective of this study was to examine the effect (and its mechanism) of luteolin on the migration and invasion of human non-small cell lung cancer A549 cells.MATERIALS/METHODS: Cell viability was investigated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Wound healing and transwell assays were evaluated to assess migration and invasion, respectively. Western blot analysis and immunofluorescence were further performed to investigate the role of luteolin and its mechanisms of action.RESULTS: Administration with up to 40 µM luteolin showed no cytotoxic activity on lung cancer A549 cells or non-cancer MRC-5 cells. Additionally, luteolin at 20–40 µM significantly suppressed A549 cells' migration, invasion, and the formation of filopodia in a concentration-dependent manner at 24 h. This is similar with western blot analysis, which revealed diminished the phosphorylated focal adhesion kinase (pFAK), phosphorylated non-receptor tyrosine kinase (pSrc), Ras-related C3 botulinum toxin substrate 1 (Rac1), cell division control protein 42 (Cdc42), and Ras homolog gene family member A (RhoA) expression levels.CONCLUSIONS: Overall, our data indicate that luteolin plays a role in controlling lung cancer cells' migration and invasion via Src/FAK and its downstream Rac1, Cdc42, and RhoA pathways. Luteolin might be considered a promising candidate for suppressing invasion and metastasis of lung cancer cells.

20.
Article in English | WPRIM | ID: wpr-828975

ABSTRACT

Objective@#This study aimed to investigate the effect of exposure to a 900 MHz electromagnetic field (EMF) on the cervical spinal cord (CSC) of rats and the possible protective effect of luteolin (LUT) against CSC tissue damage.@*Methods@#Quantitative data were obtained stereological, biochemical, immunohistochemical, and histopathological techniques. We investigated morphometric value, superoxide dismutase (SOD) level, and the expression of high-mobility group box 1 protein molecules, as well as histological changes.@*Results@#The total number of motor neurons in the EMF group significantly decreased in comparison with that in the control group ( < 0.05). In the EMF + LUT group, we found a significant increase in the total number of motor neurons compared with that in the EMF group ( < 0.05). SOD enzyme activity in the EMF group significantly increased in comparison with that in the control group ( < 0.05). By contrast, the EMF+LUT group exhibited a decrease in SOD level compared with the EMF group ( < 0.05).@*Conclusion@#Our results suggested that exposure to EMF could be deleterious to CSC tissues. Furthermore, the protective efficacy of LUT against SC damage might have resulted from the alleviation of oxidative stress caused by EMF.


Subject(s)
Animals , Antioxidants , Pharmacology , Electromagnetic Fields , Luteolin , Pharmacology , Male , Rats , Rats, Wistar , Spinal Cord , Radiation Effects
SELECTION OF CITATIONS
SEARCH DETAIL