Search results for " concentration"

showing 10 items of 1684 documents

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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Considering syntrophic acetate oxidation and ionic strength improves the performance of models for food waste anaerobic digestion.

2021

Current mechanistic anaerobic digestion (AD) models cannot accurately represent the underlying processes occurring during food waste (FW) AD. This work presents an update of the Anaerobic Digestion Model no. 1 (ADM1) to provide accurate estimations of free ammonia concentrations and related inhibition thresholds, and model syntrophic acetate oxidation as acetate-consuming pathway. A modified Davies equation predicted NH3 concentrations and pH more accurately, and better estimated associated inhibitory limits. Sensitivity analysis results showed the importance of accurate disintegration kinetics and volumetric mass transfer coefficients, as well as volatile fatty acids (VFAs) and hydrogen up…

ADM1Environmental EngineeringHydrogenchemistry.chemical_elementBioengineeringAcetatesModellingAmmoniachemistry.chemical_compoundBioreactorsMass transferAnaerobic digestionAnaerobiosisWaste Management and DisposalDavies equationchemistry.chemical_classificationAmmonia inhibitionRenewable Energy Sustainability and the EnvironmentOsmolar ConcentrationSyntrophic acetate oxidationGeneral MedicineRefuse DisposalAnaerobic digestionFood wastechemistryIonic strengthFoodEnvironmental chemistryPropionateMethaneBioresource technology
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An alternative conception of PM10 concentration changes after short-term precipitation in urban environment

2018

Abstract In the article, a linear model is presented which describes a reduction of PM10 mass concentration in relation to the type of precipitation and water vapour content in the air. The model was built using covariance analysis. In studies of PM10 concentration changes, the results of 247 observations were used, which were carried out in the urban area. Concentration changes were archived during short-term (30 min) convection and large-scale rainfalls. For the determination of PM10 mass concentration, the reference method was used. To describe changes in PM10 concentration in the air after precipitation, a series of linear models were created, in which the explanatory variables were: th…

ANCOVAFluid Flow and Transfer ProcessesAtmospheric ScienceEnvironmental EngineeringCoefficient of determination010504 meteorology & atmospheric sciencesTroposphereRainLinear modelMechanical EngineeringLinear modelHumidity010501 environmental sciencesParticulatesAtmospheric sciences01 natural sciencesPollutionSnowHomoscedasticityEnvironmental scienceMass concentration (chemistry)PrecipitationAerosolWater vapor0105 earth and related environmental sciencesJournal of Aerosol Science
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Acid sensitivity of neomycin-resistant mutants ofOenococcus oeni: a relationship between reduction of ATPase activity and lack of malolactic activity

1999

Mutants of Oenococcus oeni were isolated as spontaneous neomycin-resistant mutants. Three of these mutants harbored a significantly reduced ATPase activity that represented 50% of that of the wild-type strain. Their growth rates were also impaired at pH 5.3 (46-86% of the wild-type level). However, the profiles of sugar consumption appeared identical to those of the parental strain. At pH 3.2, all the mutant strains failed to grow and a drastic decrease in viability was observed after an acid shock. Surprisingly, all the isolated mutants were devoid of malolactic activity. These results suggest that the ATPase and malolactic activities of O. oeni are linked to each other and play a crucial …

ATPaseMutantMalatesMicrobiologyMicrobiologyGeneticsmedicineMalolactic fermentationLactic AcidMolecular BiologyHeat-Shock ProteinsOenococcus oeniAdenosine Triphosphataseschemistry.chemical_classificationbiologyStrain (chemistry)Drug Resistance MicrobialNeomycinNeomycinHydrogen-Ion Concentrationbiology.organism_classificationAnti-Bacterial AgentsGram-Positive CocciEnzymeBiochemistrychemistrybiology.proteinHeat-Shock ResponseLeuconostocBacteriamedicine.drugFEMS Microbiology Letters
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Utilization of impedance spectroscopy to investigate the self-assembly behavior of amphiphiles soluble in supercritical carbon dioxide: Preliminary r…

2007

Abstract A mixture of CO 2 , water, methyl orange (MO) and Dynol 604 surfactant was analyzed at 309 K and 20 MPa simultaneously by impedance and UV–vis spectroscopy. A plot of the static dielectric constant as a function of the surfactant concentration was obtained using a suitable equivalent circuit to elaborate impedance data. Experimental points can be fitted by two different straight lines whose intersection occurs at about 0.13% (w/w) concentration of Dynol. When the surfactant concentration crossed the aforementioned value, a peak was detectable in the UV–vis spectrum at a wavelength range corresponding to the absorption of MO; absorbance of the peak increased with the surfactant conc…

AbsorbanceSupercritical carbon dioxidePulmonary surfactantChemistryGeneral Chemical EngineeringCritical micelle concentrationAnalytical chemistryMicroemulsionPhysical and Theoretical ChemistryCondensed Matter PhysicsSpectroscopySupercritical fluidDielectric spectroscopyThe Journal of Supercritical Fluids
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Improving Dissolution Behavior and Oral Absorption of Drugs with pH-Dependent Solubility Using pH Modifiers: A Physiologically Realistic Mass Transpo…

2021

Orally dosed drugs must dissolve in the gastrointestinal (GI) tract before being absorbed through the epithelial cell membrane. In vivo drug dissolution depends on the GI tract's physiological conditions such as pH, residence time, luminal buffers, intestinal motility, and transit and drug properties under fed and fasting conditions (Paixao, P. et al. Mol. Pharm. 2018 and Bermejo, et al. M. Mol. Pharm. 2018). The dissolution of an ionizable drug may benefit from manipulating in vivo variables such as the environmental pH using pH-modifying agents incorporated into the dosage form. A successful example is the use of such agents for dissolution enhancement of BCS class IIb (high-permeability,…

Absorption (pharmacology)Chemistry PharmaceuticalAdministration OralBiological AvailabilityPharmaceutical ScienceModels BiologicalDosage formAcid dissociation constantExcipientsFumaratesDrug DiscoveryHumansComputer SimulationDissolution testingSolubilityTartratesDissolutionChromatographyChemistryHydrogen-Ion ConcentrationStomach emptyingBetaineDrug LiberationSolubilityGastrointestinal AbsorptionDrug DesignMolecular MedicineWeak baseMolecular Pharmaceutics
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Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro ex…

2014

Concomitant food intake can diminish oral absorption of drugs with limited permeability and an absorption window in the proximal intestine, due to viscosity-mediated decrease in dosage form disintegration time and drug dissolution rate. Three poorly-permeable drugs (atenolol, metformin hydrochloride, and furosemide) exhibiting negative food effect, and one highly-soluble and highly-permeable (metoprolol tartrate), serving as a negative control, were selected for the study. In vitro and in silico tools were used to evaluate the influence of media viscosity on drug bioperformance under fasted and fed conditions. The obtained results demonstrated that increased medium viscosity in the presence…

Absorption (pharmacology)DrugMetoprolol Tartratemedia_common.quotation_subjectPharmaceutical ScienceAdministration OralPharmaceutical formulationPharmacologyDosage formPermeabilityFood-Drug InteractionsPharmacokineticsPoorly-permeable drugsFurosemideHumansDissolution testingSolubilityDisintegrationmedia_commonChromatographyChemistryViscosityReproducibility of ResultsHydrogen-Ion ConcentrationFood effectMetforminAtenololIntestinal AbsorptionSolubilityFoodDissolutionAbsorption simulationEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
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DNA-binding of zinc(II) and nickel(II) salphen-like complexes extrapolated at 1 M salt concentration: Removing the ionic strength bias in physiologic…

2020

Abstract The DNA-binding of two salphen-like metal complexes of nickel(II) (1) and zinc(II) (2) was investigated in different ionic strength solutions by absorption spectroscopy. The data analysis allowed us to obtain the values of their extrapolated DNA-binding constant in physiological conditions, with DNA-binding strength in the order Ni > Zn, and to give relative weight to the electrostatic and non-electrostatic contributions to their DNA-interaction.

Absorption spectroscopyInorganic chemistryStatic ElectricitySalt (chemistry)chemistry.chemical_elementRelative weightZincPhenylenediaminesSodium Chloride010402 general chemistry01 natural sciencesBiochemistryInorganic ChemistryMetalchemistry.chemical_compoundIonic strengthCoordination ComplexesNickelSalphenchemistry.chemical_classification010405 organic chemistryChemistrySpectrum AnalysisOsmolar ConcentrationDNA0104 chemical sciencesNickelZincIonic strengthSettore CHIM/03 - Chimica Generale E Inorganicavisual_artvisual_art.visual_art_mediumUV–visible absorptionDNAJournal of Inorganic Biochemistry
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On the Low-Lying Excited States ofsym-Triazine-Based Herbicides

2005

We report a joint computational and luminescence study on the low-lying excited states of sym-triazines, namely, 1,3,5-triazine (1) and the ubiquitous herbicides atrazine [6-chloro-N2-ethyl-N4-isopropyl-1,3,5-triazine-2,4-diamine (2)] and ametryn [6-methylthio-N2-ethyl-N4-isopropyl-1,3,5-triazine-2,4-diamine (3)]. Geometrical structures, energetics, and transition and state properties of I and 2 were computed at the TD-DFT, CASSCF, and CASPT2 levels of theory. The fluorescence and phosphorescence emission spectra, lifetimes, and fluorescence quantum yields were measured for the three compounds, and from these, the energies of the lowest excited states and their corresponding radiative rates…

Absorption spectroscopyQuantum yieldPhotochemistryMolecular physicsAbsorptionAb initio quantum chemistry methodsOscillometryPressureRadiative transferEmission spectrumPhysical and Theoretical ChemistryMolecular StructureChemistry PhysicalHerbicidesTriazinesChemistryTemperatureHydrogen-Ion ConcentrationModels TheoreticalAtomic and Molecular Physics and OpticsSpectrometry FluorescenceModels ChemicalSpectrophotometryExcited stateAtrazineIndicators and ReagentsPhosphorescenceLuminescenceSoftwareChemPhysChem
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Metabolic shift of polyphosphate-accumulating organisms with different levels of polyphosphate storage

2012

Previous studies have shown that polyphosphate-accumulating organisms (PAOs) are able to behave as glycogen-accumulating organisms (GAOs) under different conditions. In this study we investigated the behavior of a culture enriched with Accumulibacter at different levels of polyphosphate (poly-P) storage. The results of stoichiometric ratios Gly degraded/HAc uptake, PHB synthesized/HAc uptake, PHV synthesized/HAc uptake and P release/HAc uptake confirmed a metabolic shift from PAO metabolism to GAO metabolism: PAOs with high poly-P content used the poly-P to obtain adenosine tri-phosphate (ATP), and glycogen (Gly) to obtain nicotinamide adenine dinucleotide (NADH) and some ATP. In a test whe…

Accumulibacter Type IIWaste component removalUnclassified drugPhysiologyChemical compositionMicrobial metabolismStorageWastewaterNicotinamide adenine dinucleotidePolyhydroxyalkanoic acidchemistry.chemical_compoundBacteriumBioreactorsPolyphosphatesGlycolysisAnaerobiosisBiomassPolyphosphate-accumulating organismsWaste Management and DisposalAccumulibacter Type IGlycogen accumulating organismPriority journalWater Science and TechnologyFluorescence microscopyPolyhydroxyvalerateSewageGlycogenHydrolysisFluorescence in situ hybridizationEcological ModelingPhosphorusHydrogen-Ion ConcentrationBioaccumulationPollutionStoichiometryWaste treatmentPolyphosphate-accumulating organismsBiodegradation EnvironmentalEnhanced biological phosphorus removalBiochemistryGlycogen-accumulating metabolism (GAM)Nicotinamide adenine dinucleotideAccumulibacter type 1Accumulibacter type 2GlycolysisGlycogenMetabolic Networks and PathwaysAccumulibacterAdenosine triphosphateEnvironmental EngineeringBiologyAcetic acidArticleAssociative storagePolyphosphate-accumulating metabolism (PAM)PolyphosphateGlycogen-accumulating organismsGlycogen-accumulating metabolismsTECNOLOGIA DEL MEDIO AMBIENTEPolyphosphate accumulating organismCivil and Structural EngineeringPolyphosphate-accumulating organisms (PAO)BacteriaPolyphosphateMetabolismIn situ measurementGlycogen-accumulating organisms (GAO)Polyphosphate-accumulating metabolismsNonhumanAmidesCarbonMetabolismchemistryPolyphosphate (poly-P)Bacterial metabolismCell cultureVolatilizationWater Research
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