Search results for " K562"

showing 5 items of 5 documents

Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation

2016

Signal Transducer and Activator of Transcription 5 (STAT5) protein, a component of the STAT family of signaling proteins, is considered to be an attractive therapeutic target because of its involvement in the progression of acute myeloid leukemia. In an effort to discover potent molecules able to inhibit the phosphorylation-activation of STAT5, twenty-two compounds were synthesized and evaluated on the basis of our knowledge of the activity of 2-(3’,4’,5’-trimethoxybenzoyl)-3-iodoacetamido-6-methoxy benzo[b]furan derivative 1 as a potent STAT5 inhibitor. Most of these molecules, structurally related to compound 1, were characterized by the presence of a common 3’,4’,5’-trimethoxybenzoyl moi…

0301 basic medicineApoptosisAntineoplastic Agentchemistry.chemical_compoundBenzophenone0302 clinical medicinehemic and lymphatic diseasesFuranDrug DiscoverySTAT5 Transcription FactorTumor Cells CulturedThiopheneMoietyPhosphorylationSTAT5Molecular StructurebiologyChemistryBiological activityGeneral MedicineApoptosis; BCR/ABL expressing leukemia; In vitro antiproliferative activity; STAT5 inhibitors; Structure-activity relationship; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyLeukemia Myeloid Acute030220 oncology & carcinogenesisBCR/ABL expressing leukemiaApoptosis; BCR/ABL expressing leukemia; In vitro antiproliferative activity; STAT5 inhibitors; Structure-activity relationship; Antineoplastic Agents; Apoptosis; Benzofurans; Benzophenones; Cell Proliferation; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Humans; K562 Cells; Leukemia Myeloid Acute; Molecular Structure; Phosphorylation; STAT5 Transcription Factor; Structure-Activity Relationship; Tumor Cells Cultured; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyHumanStereochemistryAntineoplastic AgentsArticleNOBenzophenones03 medical and health sciencesK562 CellHumansStructure–activity relationshipBenzofuransCell ProliferationPharmacologyIndole testDose-Response Relationship DrugIn vitro antiproliferative activitySTAT5 inhibitorsDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryApoptosiSTAT5 inhibitorStructure-activity relationshipIn vitro030104 developmental biologybiology.proteinBenzofuranDrug Screening Assays AntitumorK562 Cells
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The Mucus of Actinia equina (Anthozoa, Cnidaria): An Unexplored Resource for Potential Applicative Purposes

2015

The mucus produced by many marine organisms is a complex mixture of proteins and polysaccharides forming a weak watery gel. It is essential for vital processes including locomotion, navigation, structural support, heterotrophic feeding and defence against a multitude of environmental stresses, predators, parasites, and pathogens. In the present study we focused on mucus produced by a benthic cnidarian, the sea anemone Actinia equina (Linnaeus, 1758) for preventing burial by excess sedimentation and for protection. We investigated some of the physico-chemical properties of this matrix such as viscosity, osmolarity, electrical conductivity, protein, carbohydrate, and total lipid contents. Som…

CnidariaErythrocytesCarbohydratesPharmaceutical ScienceSea anemonePolysaccharideActinia equina; Antibacterial activity; Cytotoxicity; Hemolytic activity; Mucus; Tumor cell line K562; Drug Discovery3003 Pharmaceutical ScienceArticleActinia equinaBiological FactorsCnidarian Venomsantibacterial activityDry weightCell Line TumorAnthozoaDrug DiscoveryAnimalsHumanshemolytic activitylcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)chemistry.chemical_classification<i>Actinia equina</i>tumor cell line K562biologyCytotoxinsHemolytic AgentsEcologyDrug Discovery3003 Pharmaceutical SciencemucuAnthozoabiology.organism_classificationInvertebratesMucusAnti-Bacterial AgentsMucusSea Anemoneslcsh:Biology (General)chemistryBiochemistryMucucytotoxicityRabbitsK562 CellsAntibacterial activityActiniaMarine Drugs
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Biochemical and chemical characterization of Cynara cardunculus L. extract and its potential use as co-adjuvant therapy of chronic myeloid leukemia

2017

Abstract Ethnopharmacological relevance Ancient mediterranean diet was characterized by consuming the spontaneous forms of Cynara cardunculus L. (CCL), commonly called artichoke. Cultivated and/or spontaneous forms of CC studies have demonstrated that methanol extract of CCL flower and/or cynaropicrin showed remarkable anti-proliferative activity in vitro models of leukocyte cancer cell. Aim of the study Chronic myeloid leukemia (CML) is associated with a reciprocal translocation of the long arms of chromosomes 9 and 22 generating the BCR/ABL fusion gene, translated in the p210 BCR/ABL oncoprotein kinase. This chimeric protein is the target of a kinase inhibitor, imatinib, but the developme…

Cynara cardunculus L.Sesquiterpene0301 basic medicineSettore MED/06 - Oncologia MedicaFusion Proteins bcr-ablPharmacologyAntineoplastic AgentLactoneschemistry.chemical_compound0302 clinical medicinehemic and lymphatic diseasesDrug DiscoveryK562 cellABLChemistryChronic myeloid leukemiabreakpoint cluster regionMyeloid leukemiaLactoneCynaropicrinImatinib resistantChemotherapy Adjuvant030220 oncology & carcinogenesisImatinib MesylateChronic myeloid leukemia; Cynara cardunculus L.; Imatinib resistant; K562 cells; P210BCR/ABLoncoprotein; Antineoplastic Agents; Antineoplastic Agents Phytogenic; Cell Survival; Chemotherapy Adjuvant; Cynara; Drug Resistance Neoplasm; Fusion Proteins bcr-abl; Humans; Imatinib Mesylate; K562 Cells; Lactones; Leukemia Myelogenous Chronic BCR-ABL Positive; Plant Extracts; Sesquiterpenes; Pharmacology; Drug Discovery3003 Pharmaceutical ScienceSesquiterpenesHumanmedicine.drugCell SurvivalAntineoplastic AgentsCynaraPlant Extract03 medical and health sciencesLeukemia Myelogenous Chronic BCR-ABL PositivemedicineHumansViability assayneoplasmsPharmacologyPlant ExtractsCell growthDrug Discovery3003 Pharmaceutical ScienceImatinibAntineoplastic Agents PhytogenicP210BCR/ABLoncoprotein030104 developmental biologyDrug Resistance NeoplasmCancer researchK562 CellsK562 cellsJournal of Ethnopharmacology
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A lytic mechanism based on soluble phospholypases A2 (sPLA2) and b-galactoside specific lectins is exerted by Ciona intestinalis (ascidian) unilocula…

2011

Abstract Hemocytes from the ascidian Ciona intestinalis exert in vitro Ca 2+ -dependent cytotoxic activity toward mammalian erythrocytes and K562 cells. To examine the lytic mechanism, hemocyte populations were separated (B1–B6 bands) through a Percoll discontinuous density gradient, the hemocyte cytotoxic activity (HCA) and the lytic activity of the hemocyte lysate supernatant (HLS) were assayed. In addition the separated hemocytes were cultured and the cell-free culture medium (CFM) assayed after 3 h culture. Results support that unilocular refractile hemocytes (URGs), enriched in B5, are cytotoxic. The B5-HLS contains lysins and the activity of B5-CFM shows that lysins can be released in…

HemocytesPhospholipase A2 Inhibitorsmedicine.medical_treatmentLysinDibucaineSettore BIO/05 - ZoologiaAquatic ScienceBiologyFucoseCell membranechemistry.chemical_compoundmedicineEnvironmental ChemistryAnimalsHumansCiona intestinalisLectins C-TypeEnzyme InhibitorsProteaseErythrocyte MembraneGeneral Medicinebiology.organism_classificationCytotoxicity Tests Immunologicbeta-GalactosidaseGalactosideCiona intestinalisPhospholipases A2medicine.anatomical_structurechemistryBiochemistryLytic cycleInvertebrate immunity Ciona intestinalis Hemocyte Cytotoxicity Soluble phospholipase A2 Rabbit erythrocyte K562QuinacrineCaspasesImmunologyMicroscopy Electron ScanningRabbitsK562 CellsPercoll
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Cytotoxic effects of polyphenols from waste-water of extra virgin olive oil on human HL60 and K562 cell lines.

2009

Polyphenols HL60 K562 apoptosisSettore BIO/14 - FarmacologiaSettore BIO/09 - Fisiologia
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