Search results for "HL-60 Cells"

showing 10 items of 41 documents

Investigation into mechanisms mediating the inhibitory effect of 1,4-benzodiazepines on mast cells by gene expression profiling.

2013

Abstract Aims This study aims to identify by a molecular genetic approach potential targets in mast cells at which 1,4-benzodiazepines may cause their inhibitory effect on mast cell activity. Main methods Gene expression analyses with microarray gene chip and/or quantitative PCR were performed using 1,4-benzodiazepine-treated human mast cell leukemia HMC-1.2 cells, promyelocytic leukemia HL-60 cells and human mast cells from healthy volunteers and patients with mast cell activation disease (MCAD). Pathway analysis was applied to search for enriched biological functions and canonical pathways within differentially regulated genes. Key findings Both neoplastic and normal human mast cells expr…

AdultMalegenetics [Mastocytosis]Gene ExpressionHL-60 CellsFlunitrazepamBiologyPolymerase Chain ReactionGeneral Biochemistry Genetics and Molecular BiologyClonazepamLYNddc:570medicineTranslocator proteinpharmacology [Flunitrazepam]HumansMast CellsGeneral Pharmacology Toxicology and Pharmaceuticsmethods [Polymerase Chain Reaction]Interleukin 5AgedRegulation of gene expressionBenzodiazepinonesGene Expression Profilingdrug effects [Gene Expression]General MedicineMiddle AgedMast cell leukemiamedicine.diseaseMast cellMicroarray Analysis4'-chlorodiazepamCell biologyInterleukin 33Gene expression profilingmedicine.anatomical_structuremethods [Microarray Analysis]biology.proteinpharmacology [Clonazepam]drug effects [Mast Cells]Femalepharmacology [Benzodiazepinones]Mastocytosismethods [Gene Expression Profiling]
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Changes in metabolism of inorganic polyphosphate in rat tissues and human cells during development and apoptosis

1997

Age-dependent studies show that the amount of inorganic polyphosphate in rat brain strongly increases after birth. Maximal levels were found in 12-months old animals. Thereafter, the concentration of total polyphosphate decreases to about 50%. This decrease in the concentration of total polyphosphate is due to a decrease in the amount of insoluble, long-chain polyphosphates. The amount of soluble, long-chain polyphosphates does not change significantly in the course of ageing. In rat embryos and newborns, mainly soluble polyphosphates could be detected. In rat liver, the age-dependent changes are less pronounced. The changes in polyphosphate level are accompanied by changes in exopolyphosph…

AgingBiophysicsApoptosisHL-60 CellsDNA FragmentationBiochemistrychemistry.chemical_compoundPolyphosphatesAnimalsHumansRats Wistarskin and connective tissue diseasesMolecular BiologyExopolyphosphatasechemistry.chemical_classificationCell NucleusChemistryPolyphosphateBrainMetabolismEmbryo MammalianRatsEnzymeBiochemistryAnimals NewbornLiverAgeingCell cultureApoptosisDNA fragmentationsense organs
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Induction of apoptosis by the adenosine derivative IB-MECA in parental or multidrug-resistant HL-60 leukemia cells: possible relationship to the effe…

2004

<i>Background:</i> The effects of the A<sub>3</sub> adenosine receptor (A<sub>3</sub>AR) agonist IB-MECA were examined in HL-60 leukemia and in its multidrug-resistant variant HL-60R cells. <i>Methods:</i> Cytotoxicity was evaluated by MTS assays and apoptosis by flow cytometry analyses of DNA fragmentation and phosphatidylserine exposure. The mRNAs of A<sub>3</sub>AR and inhibitor of apoptosis proteins (IAPs) were determined by RT-PCR. <i>Results:</i> A<sub>3</sub>AR expression was similar in HL-60 and HL-60R cells. At ≧100 µ<i>M</i>, IB-MECA exhibited strong cytotoxic and apoptotic effects in H…

AgonistProgrammed cell deathAdenosinemedicine.drug_classApoptosisHL-60 CellsBiologyInhibitor of apoptosisInhibitor of Apoptosis ProteinsDrug DiscoverymedicineNeoplasmHumansPharmacology (medical)PharmacologyGeneral Medicinemedicine.diseaseAdenosine A3 receptorFlow CytometryAdenosineDrug Resistance MultipleLeukemiaInfectious DiseasesOncologyBiochemistryApoptosisDrug Resistance NeoplasmA 3 adenosine receptor IB-MECA Apoptosis Multidrug resistance Inhibitor of apoptosis proteinsCancer researchmedicine.drugChemotherapy
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Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells wit a non-specific phase mechanism

2006

Several stilbenes, related to known resveratrol, have been synthesized and tested for their anticancer effect on HL60 leukemia cell line, taking particular care of the cell cycle analysis. The most potent compound was the known (Z)-3,4',5-trimethoxystilbene (6b) which was active as apoptotic agent at 0.24 microM. Differently from other stilbenes (including resveratrol) that induced a prevalent recruitment of cells in S phase of cell cycle, we found a peculiar behavior of 6b that caused a decrease of cells in all phases of cell cycle (G0-G1, S, and G2-M) and a proportional increase of apoptotic cells. The potent pro-apoptotic activity shown by compound 6b and its effects on cell cycle make t…

AntimonyHL60Clinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsHL-60 CellsResveratrolBiochemistryStructure-Activity Relationshipchemistry.chemical_compoundStilbenesDrug DiscoverymedicineHumansStructure–activity relationshipMolecular BiologyS phaseCell ProliferationMolecular StructureOrganic ChemistryCell cycleMechanism of actionchemistryBiochemistryAnticancer agentResveratrolCell cultureApoptosisResveratrol analogueCell cycle analysisMolecular Medicinemedicine.symptom
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Identification of Biphenyl-Based Hybrid Molecules Able To Decrease the Intracellular Level of Bcl-2 Protein in Bcl-2 Overexpressing Leukemia Cells

2009

With the aim of enhancing the structural complexity and diversity of an existing collection of bi- and terphenyl compounds, we synthesized hybrid molecules comprising of spirocyclic ketones (a complexity-bearing core) and bi/terphenyls (privileged fragments). Compounds 1, 3, 4, and 6 showed well-defined activity on apoptosis and differentiation, making them potential leads for development as new anticancer agents and chemical probes to study signaling networks in neoplastic cells.

Antineoplastic AgentsApoptosisHL-60 CellsChemical synthesisStructure-Activity RelationshipLeukemia Myelogenous Chronic BCR-ABL PositiveTerphenyl CompoundsDrug DiscoverymedicineHumansSpiro CompoundsChemistryBiphenyl CompoundsCell DifferentiationBiological activityKetonesmedicine.diseaseIn vitroLeukemiaProto-Oncogene Proteins c-bcl-2BiochemistryApoptosisCell cultureMolecular MedicineTerphenyl CompoundsK562 CellsIntracellularJournal of Medicinal Chemistry
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Antimicrobial and antiproliferative activity of Peucedanum nebrodense (Guss.) Strohl.

2003

Abstract Acetone extract of Peucedanum nebrodense (Guss.) Strohl., a rare endemic species from the Madonie mountains (Sicily), was tested in vitro for its antimicrobial activity against bacterial reference strains and antiproliferative activity against K562 (human chronic myelogenous leukemia), HL-60 (human leukemia) and L1210 (murine leukemia) cell lines. The acetone extract showed antiproliferative IC 50 values in the range of 14–0.27 μg/ml.

Antineoplastic AgentsHL-60 CellsBiologyPlant RootsAcetoneMiceAnti-Infective Agentshemic and lymphatic diseasesDrug DiscoverymedicinePeucedanum nebrodenseCoumarins Antimicrobial Antiproliferative activityAnimalsHumansLeukemia L1210PharmacologyTraditional medicinePlant ExtractsBiological activityPlant Components AerialAntimicrobialmedicine.diseaseIn vitroLeukemiaCell cultureK562 CellsPeucedanum nebrodenseCell DivisionChronic myelogenous leukemiaK562 cellsApiaceaeJournal of ethnopharmacology
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Microwave-Assisted Synthesis of New Selenazole Derivatives with Antiproliferative Activity

2013

New aryl-hydrazinyl-1,3-selenazole and aroyl-hydrazonyl-1,3-selenazoles were synthesized via Hantzsch type condensation reactions of selenosemicarbazides with α-halogenocarbonyl derivatives, under classical versus microwave heating conditions. Excellent yields and shorter reaction times were obtained under irradiation conditions. The structures of the synthesized compounds were assigned based on spectroscopic data (FT-IR, 1 H-NMR), MS and elemental analysis. Selenazole derivatives were screened for their anti-proliferative effects against two leukemia cell lines (CCRF-CEM and HL60) and three carcinoma cell lines (MDA-MB231, HCT116 and U87MG).

AzolesHL60Pharmaceutical ScienceAntineoplastic AgentsHL-60 CellsMicrowave assistedArticleLeukemia cell lineAnalytical Chemistrylcsh:QD241-441Inhibitory Concentration 50chemistry.chemical_compoundlcsh:Organic chemistryselenazole; microwave assisted synthesis; cytotoxicityCell Line TumorOrganoselenium CompoundsCarcinoma CellDrug DiscoveryHumansPhysical and Theoretical ChemistryMicrowavesCell ProliferationOrganic ChemistryselenazoleHCT116 CellsCondensation reactionCombinatorial chemistrychemistryChemistry (miscellaneous)Elemental analysisMicrowave heatingcytotoxicityMolecular Medicinemicrowave assisted synthesisMolecules
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Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3’-C-…

2011

Histone deacetylase (HDAC) inhibitors are a new class of epigenetic agents that were reported to enhance the cytotoxic effects of classical anticancer drugs through multiple mechanisms. However, which of the possible drug combinations would be the most effective and clinically useful are to be determined. We treated the HL60 and NB4 promyelocytic leukaemia cells with a combination of the ribonucleotide reductase (RR) inhibitor 3'-C-methyladenosine (3'-Me-Ado) and several hydroxamic acid-derived HDAC inhibitors, including two recently synthesized molecules, MC1864 and MC1879, and the reference compound trichostatin A (TSA). The results showed significant growth inhibitory and apoptotic syner…

Cancer ResearchAdenosineHL60CellDeoxyribonucleotidesAntineoplastic AgentsApoptosisHL-60 CellsRibonucleotide reductase inhibitorBiologyHydroxamic AcidsHDAC inhibitors RR inhibitors Apoptosis Leukaemia ROSchemistry.chemical_compoundRibonucleotide ReductasesmedicineHumansCell ProliferationLeukemiaG1 PhaseCell cycleHistone Deacetylase InhibitorsRibonucleotide reductasemedicine.anatomical_structureTrichostatin AOncologychemistryApoptosisCancer researchSettore BIO/14 - FarmacologiaHistone deacetylaseReactive Oxygen Speciesmedicine.drug
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Selective induction of apoptosis in multidrug resistant HL60R cells by the thiazolobenzoimidazole derivative 1-(2,6-difluorophenyl)-1H,3H-thiazolo [3…

1999

We investigated the antitumour effects of 1-(2,6-difluorophenyl)-1H,3H-thiazolo [3,4-a]benzimidazole (TBZ) a new anti-HIV-1 agent, on human promyelocytic HL60 leukaemia, both a parental and a multidrug resistant form (HL60R). HL60R overexpresses P-glycoprotein and, like HL60, lacks p53 protein expression. HL60 and HL60R show similar levels of Bcl-2 protein. In contrast to the conventional chemotherapeutic agents daunorubicin, etoposide and mitoxantrone, TBZ caused equal or even greater cytotoxicity in HL60R than in HL60, and this result was associated with a more marked induction of apoptosis in the drug resistant cells. The antitumour activity of TBZ occurred in the range of concentrations…

Cancer ResearchBenzimidazoleAnti-HIV AgentsDaunorubicinHL60ApoptosisHL-60 CellsDrug resistancePharmacologychemistry.chemical_compoundmedicineHumansATP Binding Cassette Transporter Subfamily B Member 1CytotoxicityP-glycoproteinbiologyFlow CytometryVirologyDrug Resistance MultipleMultiple drug resistanceThiazolesProto-Oncogene Proteins c-bcl-2OncologychemistryDrug Resistance NeoplasmApoptosisbiology.proteinBenzimidazolesDrug Screening Assays AntitumorTumor Suppressor Protein p53medicine.drugEuropean Journal of Cancer
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Expression of the IAPs in multidrug resistant tumor cells

2003

We have investigated the expression of the IAPs (inhibitory of apoptosis proteins) in the human HL-60 leukemia and in its multidrug resistant, P-glycoprotein (P-gp) over-expressing variant, HL-60R. HL-60R exhibits resistance to apoptosis induced from P-gp substrate drugs and also from other triggers (cisplatin, TNF-alpha, Fas ligation, TRAIL, IFN-gamma and serum starvation) not related to the multidrug transporter. Except for c-IAP-1 mRNA, HL-60R significantly over-expressed both the mRNAs and the proteins of all the IAPs studied, i.e. c-IAP-1, c-IAP-2, XIAP, NAIP and survivin. Determination of the DNA-binding capacity of NF-kappaB (p50 or p65 subunits) indicated that, while HL-60 cells sho…

Cancer ResearchBlotting WesternCellApoptosisHL-60 CellsBiologyInhibitor of Apoptosis Proteinsmultidrug resistanceSurvivinmedicineHumansRNA MessengerCisplatinOncogeneReverse Transcriptase Polymerase Chain ReactionNF-kappa BProteinsGeneral MedicineIAPCell cycleapoptosiMolecular biologyDrug Resistance MultipleXIAPGene Expression Regulation Neoplasticmedicine.anatomical_structureOncologyDrug Resistance NeoplasmApoptosisCancer researchNAIPmedicine.drugOncology Reports
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