Search results for "Propidium"

showing 10 items of 73 documents

MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate

2019

Polo-like kinase (PLK1) has been identified as a potential target for cancer treatment. Although a number of small molecules have been investigated as PLK1 inhibitors, many of which showed limited selectivity. PLK1 harbors a regulatory domain, the Polo box domain (PBD), which has a key regulatory function for kinase activity and substrate recognition. We report on 3-bromomethyl-benzofuran-2-carboxylic acid ethyl ester (designated: MCC1019) as selective PLK1 inhibitor targeting PLK1 PBD. Cytotoxicity and fluorescence polarization-based screening were applied to a library of 1162 drug-like compounds to identify potential inhibitors of PLK1 PBD. The activity of compound MC1019 against the PLK1…

PBD Polo box domainMTD maximal tolerance doseCDC25 cell division cycle 25HIF-1α hypoxia-inducible factor 1 αMST microscale thermophoresisIC50 50% inhibition concentrationMFP M phase promoting factorPARP-1 poly(ADP-ribose) polymerase-10302 clinical medicineFOXO forkhead box ONec-1 necrostatin 1CDC2 cell division cycle protein 2 homologGeneral Pharmacology Toxicology and PharmaceuticsMitotic catastropheCDK cyclin-dependent kinase0303 health sciencesChemistryPolo-like kinaseMono-targeted therapyCell cycleBUBR1 budding uninhibited by benzimidazole-related 1Polo box domain030220 oncology & carcinogenesisPLK1 Polo-like kinaseNecroptosisSpindle damagePLK1IHC immunohistochemistryOriginal articleNecroptosisCell cyclePLK1APC/C anaphase-promoting complex/cyclosomePLK3ABC avidin-biotin complexPI propidium iodide03 medical and health sciencesFBS fetal bovine serumPDB Protein Data BankKd the dissociation constantKinase activity030304 developmental biologyAkt/PKB signaling pathwayCell growthlcsh:RM1-950LC3 light chain 3lcsh:Therapeutics. PharmacologyCancer researchDAPKs death-associated protein kinase3-MA 3-methyladenineDAPI 4′6-diamidino-2-phenylindoleSAC spindle assembly checkpointActa Pharmaceutica Sinica B
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Infarct Size Measurement by Triphenyltetrazolium Chloride StainingVersus In VivoInjection of Propidium Iodide

1997

Infarct size delineation by triphenyltetrazolium chloride (TTC) staining is dependent on sufficient reperfusion. We therefore evaluated the possibility of using propidium iodide (PI), a reagent conventionally used in flow cytometry to fluorescently stain dead cells, for infarct size analysis after short periods of reperfusion. Forty-five rabbits were subjected to either 15 min, 2 h or 4.5 h of coronary artery occlusion without reperfusion, or to 15 min, 30 min and 2 h of coronary artery occlusion followed by 30 min, 1 h and 3 h of reperfusion. Fifteen min before terminating the experiment, PI was injected into the left atrium. Patent blue violet was used to delineate the area at risk. Follo…

Pathologymedicine.medical_specialtyCell Membrane PermeabilityMyocardial InfarctionTetrazolium SaltsMyocardial ReperfusionStainFlow cytometrychemistry.chemical_compoundIn vivoOcclusionmedicineAnimalscardiovascular diseasesPropidium iodideColoring AgentsMolecular BiologyStaining and Labelingmedicine.diagnostic_testChemistrybusiness.industryMyocardiumHistologymedicine.diseaseCoronary VesselsStainingInjections Intra-ArterialRabbitsCardiology and Cardiovascular MedicineNuclear medicinebusinessReperfusion injuryPropidiumJournal of Molecular and Cellular Cardiology
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Swelling, Acidosis, and Irreversible Damage of Glial Cells from Exposure to Arachidonic Acid in vitro

1994

Swelling and damage of C6 glioma cells and of primary cultured astrocytes were analyzed in vitro during incubation with arachidonic acid (AA; 20:4). The cells were suspended in a physiological medium supplemented with AA at concentrations of 0.001–1.0 m M. Cell swelling was quantified by flow cytometry with hydrodynamic focusing. Flow cytometry was also utilized for assessment of cell viability by exclusion of the fluorescent dye propidium iodide and for measurement of the intracellular pH (pHi) by 2′,7′-bis-(2-carboxyethyl)−5(and −6)carboxyfluorescein. Administration of AA caused an immediate dose-dependent swelling of C6 glioma cells, even at a concentration of 0.01 m M. At this level cel…

Pathologymedicine.medical_specialtyCell SurvivalLinoleic acidIntracellular pHBiologychemistry.chemical_compoundTumor Cells CulturedmedicineLactic AcidViability assayPropidium iodideCell damageArachidonic AcidFatty AcidsSodiumHydrogen-Ion Concentrationmedicine.diseaseMolecular biologyNeurologychemistryCell cultureAstrocytesLactatesSteroidsArachidonic acidNeurology (clinical)Swellingmedicine.symptomAcidosisCardiology and Cardiovascular MedicineNeurogliaJournal of Cerebral Blood Flow & Metabolism
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Exploratory study on the effects of biodegradable nanoparticles with drugs on malignant B cells and on a human/mouse model of Burkitt lymphoma.

2010

The aim of this study was to determine if Rituximab coated Biodegradable Nanoparticles (BNPs) loaded with Chlorambucil and Hydroxychloroquine could induce apoptosis of B-Chronic Lymphocytic Leukemia (B-CLL), MEC-1 and BJAB cells in vitro and evaluate their toxic and therapeutic effects on a Human/Mouse Model of Burkitt Lymphoma at an exploratory, proof of concept scale. We found that Rituximab-Chlorambucil-Hydroxychloroquine BNPs induce a decrease in cell viability of malignant B cells in a dose-dependent manner. The mediated cytotoxicity resulted from apoptosis, and was confirmed by monitoring the B-CLL cells after Annexin V/propidium iodide staining. Additional data revealed that these BN…

Pathologymedicine.medical_specialtyCell Survivalhuman/mouse model of Burkitt lymphoma.human lymphomamodel SCID mouseAntineoplastic Agentschemistry.chemical_compoundAntibodies Monoclonal Murine-DerivedMicerituximabimmune system diseasesAnnexinhemic and lymphatic diseasesnanoparticles; rituximab; human lymphoma; model SCID mouseTumor Cells CulturedMedicineAnimalsHumansPharmacology (medical)Propidium iodideGeneral Pharmacology Toxicology and PharmaceuticsCytotoxicityB-LymphocytesChlorambucilDose-Response Relationship Drugbusiness.industrymalignant B cellnanoparticleDrug SynergismGeneral MedicineBiodegradable nanoparticles with drugmedicine.diseaseBurkitt LymphomaLymphomaMice Inbred C57BLLeukemiaDisease Models AnimalDrug CombinationschemistryApoptosisMonoclonalCancer researchNanoparticlesChlorambucilbusinessRituximabmedicine.drugHydroxychloroquine
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Clinical concentrations of efavirenz (EFV) reduce cellular proliferation and viability in several human cell lines

2008

Results MTT assays upon 24 h of culture in the presence of the drug revealed reduced viability in the human hepatoma cell line Hep3B (significant for all three concentrations and calculated as 84.59 ± 8.82% decrease for 50 μM EFV), human cervix carcinoma cell line HeLa (71.92 ± 5.49% reduction for 50 μM EFV) and primary Human Umbilical Vein Endothelial cells (HUVEC), (96.76 ± 0.27% reduction for 50 μM EFV). This result was corroborated with 3day-proliferation experiments in which Hep3B were exposed to different concentrations of EFV; a significant reduction (60.1 ± 6.54% after 3 days) was detected with 25 μM EFV whereas cytotoxicity (97.01 ± 1.13% reduction) was observed with 50 μM, however…

Pathologymedicine.medical_specialtyCytochrome cPublic Health Environmental and Occupational HealthBiologybiology.organism_classificationMolecular biologyUmbilical veinHeLachemistry.chemical_compoundInfectious DiseaseschemistryAnnexinApoptosisCell culturebiology.proteinmedicinePropidium iodideCytotoxicityJournal of the International AIDS Society
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AB0069 Conditioned media from adipose-derived mesenchymal stem cells decreases senescence and enhances collagen ii expression in osteoarthritic chond…

2013

Background Adipose-derived mesenchymal stem cells (ASC) might act as a cellular source of soluble factors exerting anti-inflammatory or trophic effects on cells. Osteoarthritis (OA) is characterized by the progressive loss of structure and functionality of articular cartilage. Objectives In the present study we explored the effect of conditioned medium from adipose-derived mesenchymal stem cells (ASC-CM) on the metabolism of OA chondrocytes in primary culture. Methods ADC were isolated from adipose tissue of patients subjected to abdominal lipectomy surgery, by collagenase treatment. Cells were incubated in DMEM/F12 + 15% human serum. Cell phenotype was analysed by flow cytometry with speci…

Pathologymedicine.medical_specialtymedicine.medical_treatmentImmunologyMesenchymal stem cellAdipose tissueInterleukinBiologyMatrix metalloproteinaseGeneral Biochemistry Genetics and Molecular BiologyAndrologyCell therapychemistry.chemical_compoundCytokineRheumatologychemistrymedicineCollagenaseImmunology and AllergyPropidium iodidemedicine.drugAnnals of the Rheumatic Diseases
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Vital dyes and virtual deaths.

2013

Dear Editor, In 2009 and 2012, Cell Death & Differentiation has published recommendations of the Nomenclature Committee on Cell Death (NCCD) for the Classification of cell death and Molecular definitions of cell death subroutines, respectively. Under the subtitle When is a cell ‘dead'?, and in an accompanying table entitled Molecular or morphological criteria to define dead cells, the 2009 paper featured a set of three criteria; the fulfillment of any single one is considered to indicate cell death.1 The first criterion in this list is Loss of plasma membrane integrity, and parameters commonly used to assess integrity of the plasma membrane were mentioned, namely exclusion from cells of vit…

Programmed cell deathCell DeathVesicleCellPerforation (oil well)Cell BiologyBiologyCell cycleArticleCell biologychemistry.chemical_compoundMembranemedicine.anatomical_structurechemistryTerminology as TopicCorrespondencemedicineAnimalsHumansPropidium iodideMolecular BiologyFlux (metabolism)Cell death and differentiation
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Novel path to apoptosis: small transmembrane pores created by staphylococcal alpha-toxin in T lymphocytes evoke internucleosomal DNA degradation.

1994

Peripheral-blood human T lymphocytes were treated with Staphylococcus aureus alpha-toxin. Membrane permeabilization was assessed by measuring efflux of K+ and Rb+ and influx of Na+, Ca2+, and propidium iodide. Cellular ATP and [3H]thymidine incorporation following lectin stimulation were measured as parameters for cell viability. Internucleosomal cleavage characteristic of programmed cell death was assessed by agarose gel electrophoresis and by quantifying low-molecular-weight, [3H]thymidine-labeled DNA fragments. Nanomolar concentrations of alpha-toxin evoked protracted, irreversible ATP depletion in both activated and resting T lymphocytes. Toxin-damaged cells also lost their ability to i…

Programmed cell deathCell Membrane PermeabilityStaphylococcusT-LymphocytesImmunologyBacterial ToxinsApoptosisBiologyMicrobiologychemistry.chemical_compoundHemolysin ProteinsAdenosine TriphosphateHumansPropidium iodideViability assaySodiumT lymphocyteDNANucleosomesInfectious DiseaseschemistryBiochemistryApoptosisAgarose gel electrophoresisBiophysicsPotassiumParasitologyCalciumThymidineAdenosine triphosphateResearch Article
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Cytotoxicity and antimitotic activity of Rhinella schneideri and Rhinella marina venoms.

2019

Abstract Ethnopharmacological relevance Rhinella schneideri and Rhinella marina are toad venoms distributed in different parts of the world, including Brazil, Columbia and amazon. Venoms extracted from different species have many clinical applications such as antimicrobial cardiotonics and treatment of cancer. Aim of the study; In this study, we aim to investigate the effect of venoms extracted from R. schneideri and R. marina on cancer cells and verify possible mechanism of action. Material and method Cytotoxicity analyses was performed using the resazurin reduction assay, where different concentrations of venoms were tested against sensitive CCRF-CEM and P-gp overexpressing ADR/CEM5000 le…

Programmed cell deathCell SurvivalAntimitotic AgentsLethal Dose 5003 medical and health scienceschemistry.chemical_compound0302 clinical medicineTubulinRhinella schneideriCell Line TumorDrug DiscoveryAnimalsHumansPropidium iodideCytotoxicity030304 developmental biologyPharmacology0303 health sciencesbiologyBufalinCell Cycle Checkpointsbiology.organism_classificationBufonidaeMolecular Docking SimulationTubulinchemistryBiochemistryApoptosis030220 oncology & carcinogenesisCancer cellbiology.proteinAmphibian VenomsJournal of ethnopharmacology
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Biological activities of the LXRα and β agonist, 4β-hydroxycholesterol, and of its isomer, 4α-hydroxycholesterol, on oligodendrocytes: effects on cel…

2013

The biochemical and biological properties of 4β-hydroxycholesterol and of its isomer, 4α-hydroxycholesterol, are not well known. So, we determined the ability of 4α- and 4β-hydroxycholesterol to react with LXRα and LXRβ, and we characterized the activities of these oxysterols on oligodendrocytes which are myelin synthesizing cells. The effects of 4α- and 4β-hydroxycholesterol were studied on 158N murine oligodendrocytes to assess their activities on cell growth and viability, oxidative and inflammatory status. To this end different parameters were used: cell counting with trypan blue; identification of dead cells and cell cycle analysis with propidium iodide; evaluation of mitochondrial dep…

Programmed cell deathCell SurvivalBiologyBiochemistrychemistry.chemical_compoundMiceIsomerismpolycyclic compoundsmedicineAnimalsPropidium iodideProtein Structure QuaternaryCell ProliferationLiver X ReceptorsInflammationSuperoxideCell growthAcridine orangeDepolarizationGeneral MedicineOrphan Nuclear ReceptorsOligodendrocyteActinsHydroxycholesterolsCell biologyMitochondriaOligodendrogliamedicine.anatomical_structurechemistryCytokineslipids (amino acids peptides and proteins)Trypan blueProtein MultimerizationLysosomesReactive Oxygen SpeciesOxidation-ReductionBiochimie
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