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Paeonol has inhibitory effect on a variety of tumor cells, whereas cadherin is a kind of glycoprotein that is associated with the occurrence and development of different tumor.In this study, the interactions of paeonol and E-cadherin have been investigated by fluorescence spectrometry and atomic force microscopy (AFM).Fluorescence spectrometry results revealed that the addition of paeonol significantly quenched the fluorescence of E-cadherin.Based on the results of the quenching constant, it was inferred that the interaction of paeonol and E-cadherin was a static quenching process.The thermodynamic parameters ΔH and ΔS were calculated to be -4.3×10.5 J/mol and -1.3×10.3 J/(mol·K), respectively, which proved the involvement of weak interactive forces such as hydrogen bond van der Waals force.AFM results revealed that cadherin molecules were assembled into the long-chain structure.The addition of paeonol could significantly disrupt these assembling structures into short chains, which could be ascribed to the damage of the interdigitation model from the adjacent cadherin molecules.All these results reveal that cadherin is an important target of paeonol to modulate its activity.
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OBJECTIVE:To prepare and characterize Ibuprofen (IBU) nano-powder,and to investigate its transdermal ability in vitro. METHODS:Using chloroform-ethanol(7:3,V/V)as organic phase,deionized water as aqueous phase and polysorbate 80 as surfactant,the emulsification method was used to prepare IBU nano-powder. Laser granulometric analysis,Fourier transform in-frared spectroscopy(FT-IR),X-ray diffraction(XRD),differential scanning calorimetry(DSC)were used to characterize IBU na-no-powder. IBU nano-powder was compared with bulk drug in respects of saturation solubility,dissolution rate and transdermal rate in vitro. RESULTS:The optimum condition was as follows that the concentration of polysorbate 80 was 5 mg/mL;the volume ra-tio of water phase-organic phase was 40:1;the concentration of IBU was 250 mg/mL;homogenate speed was 5000 r/min;homog-enate time was 2 min. Prepared IBU nano-powder was polyporous crumbly coralliform,and its chemical structure kept stable;the nano-powder changed from crystal to amorphous state;the particle size was 179.6 nm,and drug-loading amount was 8.99%;satu-ration solubility,dissolution rate and transdermal rate of IBU nano-powder were 148,1.23 and 4.08 times of bulk drug. CONCLU-SIONS:The prepared IBU nano-powder shows good water-solubility and percutaneous permeability.
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OBJECTIVE:To prepare the betulinic acid nanoparticles,and characterize them. METHODS:Using ethanol as sol-vent and water as anti-solvent,anti-solvent recrystallization method was used to prepare betulinic acid nanoparticles. Using particle size as indicator,single factor test and orthogonal test were adopted to optimize the mass concentration of betulinic acid solution, anti-solvent-solvent volume ratio,anti-solvent drip rate,reaction temperature and stirring speed in formulation technology of betulin-ic acid nanoparticles,and verification test was conducted. The betulinic acid nanoparticles were characterized by scanning electron microscopy,laser particle size analyzer,Fourier infrared spectrometer and mass spectrum analyzer. RESULTS:The optimal technol-ogy was as follow as betulinic acid solution mass concentration of 3 mg/mL,anti-solvent-solvent volume ratio of 1:1,anti-solvent drip rate of 8 mL/min,reaction temperature of 20 ℃ and stirring speed of 900 r/min. The average size of prepared betulinic acid nanosuspension was(156.0±8.6)nm(n=3)and the particle size was(235.0±12.2)nm(n=3)after freeze-drying,with nearly spherical appearance,uniform size and regular form. Compared with raw material of betulinic acid,the chemical structure of pre-pared betulinic acid nanoparticles did not change,and there were no significant changes in molecular weight and mass ratio. CON-CLUSIONS:Betulinic acid nanoparticles are successfully prepared.
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An enhance matrix removal ( EMR) QuEChERS method for simultaneous determination of 22 triazine herbicide residuals such as atrazine, propazine, terbumeton, and desmetryn in corn was established and validated. The corn samples were initially extracted with acetonitrile ( MeCN ) in high-speed homogenization, and the targeted pesticides were prepared using EMR-Lipid (Enhanced matrix removal-lipid) method to clean-up and EMR-Polish to salt out, separated on a Kinetex XB-C18 with acetonitrile and 0. 1%formic acid aqueous as eluant, and then detected by UFLC-MS / MS under positive ( ESI+ ) electrospray ionization and MRM models. The average recoveries of 22 herbicides were in the range of 72% -105% at the spiked level of 5, 10 and 20 μg / kg. The relative standard deviations were less than 15% . In the method validation, correlation coefficients were higher than 0. 993 with the linear range from 1. 0 μg / L to 50 μg / L. The qualitative analysis and quantitative analysis were investigated by UFLC-MS / MS and matrix-matched calibration curves. The results showed that EMR QuEChERS combined with UFLC-MS / MS purification method was rapid, accurate and sensitive for the determination of 22 triazine herbicides residues in corn.
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<p><b>OBJECTIVE</b>To determine glycyrrhetinic acid concentration in rat plasma and concentration of calcium (Ca), copper (Cu), iron (Fe), potassium (K), magnesium (Mg) and sodium (Na) in rat serum after oral administration by LC-MS/MS and the flame atomic absorption method, and analyze the effect of glycyrrhetinic acid on the six elements in serum.</p><p><b>RESULT</b>A similar variation trend between the concentration of glycyrrhetinic acid in plasma and that of Na, Cu elements in serum after oral administration of glycyrrhetinic acid was observed. Glycyrrhetinic acid in plasma at 2 h after administration reached the peak. Meanwhile, the concentration of Na and Cu at 4 h after the administration of glycyrrhetinic acid exhibited a significant increase (P < 0.05). Moreover, an increasing glycyrrhetinic acid dosage could result in the accumulation of Cu and Na in rat serum. Compared with the control group, the concentration of Cu and Na in the the glycyrrhetinic acid administration group with doses of 200 and 400 mg x kg(-1) revealed a significant increase (P < 0.05). However, glycyrrhetinic acid did not exhibit the great impact on the concentration of other elements in serum.</p><p><b>CONCLUSION</b>This study focuses on the effect of oral administration of glycyrrhetinic acid on six metal elements in rat serum and provides an experimental basis for the adverse effect of glycyrrhetinic acid in clinical-applications.</p>
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Animais , Feminino , Masculino , Ratos , Administração Oral , Ácido Glicirretínico , Farmacologia , Metais , Sangue , Ratos Sprague-DawleyRESUMO
<p><b>OBJECTIVE</b>The content of vindoline, catharanthine and vinblastine in the root, stem, leaf, flower and fruit of Catharanthus roseus at various developmental stages were determined, and the biomass allocation was also determined to find the best harvest time.</p><p><b>METHOD</b>The content of vindoline, catharanthine and vinblastine in the root, stem, leaf, flower and fruit of C. roseus were determined by HPLC.</p><p><b>RESULT</b>The content of these alkaloids were influenced by season and it varied in the different tissues of the plant. The content of vindoline and catharanthine in the leaves were the highest, and there was no vindoline detected in the root, but the content of vinblastine in the flower was the highest; the content of vindoline and catharanthine reached the maximum between the August and September, and the content of vinblastine reached the highest after the September. The biomass was the highest in the initial stage of September.</p><p><b>CONCLUSION</b>The best harvest time was in the initial stage of September.</p>
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Catharanthus , Química , Metabolismo , China , Cromatografia Líquida de Alta Pressão , Flores , Química , Metabolismo , Extratos Vegetais , Metabolismo , Folhas de Planta , Química , Metabolismo , Raízes de Plantas , Química , Metabolismo , Estações do Ano , Vimblastina , Metabolismo , Alcaloides de Vinca , MetabolismoRESUMO
<p><b>OBJECTIVE</b>To investigate the extraction method of polyglycosides from Tripterygium wilfordii.</p><p><b>METHOD</b>The extraction method of pressurized liquid extraction was employed and chromogenic colorimetric technique were used for quantitative analysis. Based on the single-factor experiment, according to the center combination design this paper used three factors and three levels of response surface methodology for process optimization.</p><p><b>RESULT</b>The optimized conditions were as follows: ratio of solid to liquid was 1:9.5, at the temperature of 115 degrees C for 80 minutes, the actual extract ratio and purity of polyglycosides obtained were 0.21% and 0.52%, respectively.</p><p><b>CONCLUSION</b>The method of pressurized liquid extraction has obvious advantages over conventional reflux extracting.</p>
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Glicosídeos , Extratos Vegetais , Química , Pressão , Tripterygium , QuímicaRESUMO
With cDNA from Phellodendron amurense seedlings treated with drought stress as tester and cDNA from this plant in normal growth as driver, we construct cDNA subtracted library using suppression subtractive hybridization (SSH). In the library, the rate of recombination was 95%, the size of inserts was 300-800 bp. Two hundred and sixty-five new genes were obtained by DNA sequencing 816 positive clones picked randomly, and partitioned to 16 classes after nucleotide Blast and BlastX homological analysis against NT, NR, SWISSPROT, KEGG database. Forty-four drought stress associated genes, such as heat shock protein cognate 70, dehydration responsive protein 22, universal stress protein, metallothionein II, late embryogenesis abundant protein, were obtained, which made 16.6% of the overall genes. These genes included osmotic regulator, signal component regulatory protein and antioxidant enzyme. The research had established a basis for cloning stress resistance genes and further studying genes expression in P. amurense seedlings under drought stress.
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Adaptação Fisiológica , Genética , Clonagem Molecular , Secas , Expressão Gênica , Perfilação da Expressão Gênica , Biblioteca Gênica , Hibridização de Ácido Nucleico , Métodos , Phellodendron , Genética , Fisiologia , Plântula , Genética , FisiologiaRESUMO
The protective function of a plant type-2 metallothionein was analysed after expression in Escherichia coli and in Arabidopsis thaliana seedlings. BjMT2 from Brassica juncea was expressed in E. coli as a TrxABjMT2 fusion protein. After affinity chromatography and cleavage from the TrxA domain, pure BjMT2 protein was obtained which strongly reacted with the thiol reagent monobromobimane. Escherichia coli cells expressing the TrxABjMT2 fusion were more tolerant to Cu2+ and Cd2+ exposure than control strains. Likewise, when BjMT2 cDNA was expressed in A. thaliana under the regulation of the 35S promoter, seedlings exhibited an increased tolerance against Cu2+ and Cd2+ based on shoot growth and chlorophyll content. Analysis of transiently transformed cells of A. thaliana and tobacco leaves by confocal laser scanning microscopy (CLSM) revealed exclusive cytosolic localization of a BjMT2::EGFP (enhanced green fluorescent protein) fusion protein in control and heavy metal-exposed plant cells. Remarkably, ectopic expression of BjMT2 reduced root growth in the absence of heavy metal exposure, whereas in the presence of 50 or 100 microM Cu2+ root growth in control and transgenic lines was identical. The results indicate that in A. thaliana, root and shoot development are differentially affected by ectopic expression of BjMT2.
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Arabidopsis/efeitos dos fármacos , Cádmio/farmacologia , Cobre/farmacologia , Escherichia coli/efeitos dos fármacos , Metalotioneína/fisiologia , Mostardeira , Proteínas de Plantas/fisiologia , Oligoelementos/farmacologia , Arabidopsis/genética , Arabidopsis/crescimento & desenvolvimento , Caulimovirus/genética , Escherichia coli/genética , Metalotioneína/genética , Metalotioneína/metabolismo , Mostardeira/genética , Folhas de Planta/genética , Folhas de Planta/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Raízes de Plantas/efeitos dos fármacos , Raízes de Plantas/genética , Raízes de Plantas/crescimento & desenvolvimento , Brotos de Planta/efeitos dos fármacos , Brotos de Planta/genética , Brotos de Planta/crescimento & desenvolvimento , Plantas Geneticamente Modificadas/crescimento & desenvolvimento , Plantas Geneticamente Modificadas/metabolismo , Regiões Promotoras Genéticas , Proteínas Recombinantes de Fusão/análise , Proteínas Recombinantes de Fusão/metabolismo , Plântula/efeitos dos fármacos , Plântula/genética , Plântula/crescimento & desenvolvimento , Tiorredoxinas/genética , Nicotiana/genéticaRESUMO
Object To establish the process of purification for ?-linolenic acid from the fruit oil of Camptotheca acuminata Decne.. Methods Complexometry by AgNO 3 was applied. Results The optimal conditions: the AgNO 3 concentration was 4 mol/L, the complexometric temperature was lower than 15 ℃, and the complexometric time was 2 h. The purity of ?-linolenic acid was 91.25%. Conclusion The concentration of ?-linolenic acid from the fruit oil of C. acuminata can reach to 45.8%, therefore it is a new abundant resource for ?-linolenic acid. ?-linolenic acid can be well purified in the fruit oil by this process.
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Objective To clone and sequence the cDNA encoding phenylalanine ammonia-lyase(PAL)gene from Astragalus membranaceus.Methods RT-PCR and RACE Techniques were used to clone a phenylalanine ammonia-lyase gene from A.membranaceus roots with the total RNA as the template.Results The cloned gene named as AmPAL and the Genbank registry number is EF567076.Squence analysis showed that the full-length of AmPAL cDNA was 2 650 bp,including a 2 154 bp open reading frame(ORF).AmPAL was a new number of PAL family that consisted of 718 amino acids with prediated mole-cular weight of 7.805?104 and isoelectric point(PI)of 5.96.At the same time,AmPAL had the homo-logy with PAL of known leguminous plants and shared above 80% identity of amino acid sequences.Conclusion It is the first report that a novel PAL gene is cloned from A.membranaceus.This work lays a foundation for regulating phenylpropanoid pathway of medical plant with AmPAL.
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Object To develop a new process for the extraction of camptothecin from leaves of Camptotheca acuminata Decne Methods By uniform experimental design after proper choice of solvent Results The optimal conditions were extraction with 16 times of 0 3% NaOH for three hours each time Conclusion This is the first attempt to use dilute NaOH solution for the extraction of camptothecin from the previously seldom utilized leaves of C acuminata, which resulted in a yield well over 0 1% The process resulted in a lower production cost and require less fire protection measures as compaired with the conventional use of alcohol
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Object To establish the process of supercritical CO 2 extraction of glycyrrhetic acid from Glycyrrhiza uralensis Fisch.. Methods The comparison methods among supercritical CO 2 extraction, Soxhleth extraction and ultrasonic extraction were conducted. Results The optimized supercritical CO 2 extraction conditions were 30 MPa, pressure; 70 meshes, granularity of material; 80% ethanol, modifying agent; 45 ℃, extraction temperature; 2 hours, extraction time. Conclusion The results show that supercritical CO 2 extraction has an advantage over any other extractions of glycyrrhetic acid from G. uralensis.