Search results for "Dose"

showing 10 items of 2247 documents

Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells

2017

A series of new artemisinin-derived hybrids which incorporate cholic acid moieties have been synthesized and evaluated for their antileukemic activity against sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells. The new hybrids 20-28 showed IC50 values in the range of 0.019µM-0.192µM against CCRF-CEM cells and between 0.345µM and 7.159µM against CEM/ADR5000 cells. Amide hybrid 25 proved the most active compound against both CCRF-CEM and CEM/ADR5000 cells with IC50 value of 0.019±0.001µM and 0.345±0.031µM, respectively. A relatively low cross resistance to hybrids 20-28 in the range of 5.7-fold to 46.1-fold was measured. CEM/ADR5000 cells showed higher resistance than CCRF-CEM to al…

0301 basic medicinevirusesClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBiochemistryAntileukemic agentStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compound0302 clinical medicineimmune system diseaseshemic and lymphatic diseasesAmideDrug DiscoveryTumor Cells CulturedmedicineHumansCytotoxic T cellDoxorubicinArtemisininMolecular BiologyIC50Cross-resistanceCell ProliferationLeukemiaDose-Response Relationship DrugMolecular StructureOrganic ChemistryCholic acidhemic and immune systemsArtemisinins030104 developmental biologyBiochemistrychemistry030220 oncology & carcinogenesisMolecular MedicineDrug Screening Assays Antitumormedicine.drugBioorganic & Medicinal Chemistry
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Metabolic detoxification: implications for thresholds.

2000

The fact that chemical carcinogenesis involves single, isolated, essentially irreversible molecular events as discrete steps, several of which must occur in a row to finally culminate in the development of a malignancy, rather suggests that an absolute threshold for chemical carcinogens may not exist. However, practical thresholds may exist due to saturable pathways involved in the metabolic processing, especially in the metabolic inactivation, of such compounds. An important example for such a pathway is the enzymatic hydrolysis of epoxides via epoxide hydrolases, a group of enzymes for which the catalytic mechanism has recently been established. These enzymes convert their substrates via…

040301 veterinary sciencesDNA damageEpoxide10050 Institute of Pharmacology and Toxicology610 Medicine & healthToxicology030226 pharmacology & pharmacyPathology and Forensic MedicineXenobiotics0403 veterinary science1307 Cell Biology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineEnzymatic hydrolysis1312 Molecular BiologyAnimalsHumansComputer SimulationEpoxide hydrolaseMolecular BiologyCarcinogenchemistry.chemical_classificationEpoxide HydrolasesDose-Response Relationship Drug3005 Toxicology04 agricultural and veterinary sciencesCell Biology2734 Pathology and Forensic MedicineEnzymechemistryBiochemistryCovalent bondEpoxide HydrolasesInactivation MetabolicCarcinogensMicrosomes Liver570 Life sciences; biologyMutagensToxicologic pathology
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Synthesis, characterization, and cytotoxic activity of copper(II) and platinum(II) complexes of 2-benzoylpyrrole and X-ray structure of bis[2-benzoyl…

2004

Copper(II) and platinum(II) complexes of 2-benzoylpyrrole (2-BZPH) were synthesized and characterized with IR, 1 H and 1 3 C NMR spectroscopies and coordination geometry with ligands arranged in transoid fashion. The crystal structure of [Cu I I (2-BZP) 2 ] was determined by X-ray diffraction. Death of complex treated Jurkat cells was measured by flow cytometry. The bis-chelate complexes [Cu I I (2-BZP) 2 ] and [Pt I I (2-BZP) 2 ] adopt square-planar coordination geometry with ligands, arranged in transoid fashion. Concentrations of 1-10 μM Platinum(II) complexes reduced cell survival from 100% to 20%, in contrast to the copper(II) complex which caused no cell death at a concentration of 10…

2-BenzoylpyrroleCopper(II) and platinum(II) complexesCytotoxicityMagnetic Resonance SpectroscopySpectrophotometry InfraredCell SurvivalMolecular Conformationchemistry.chemical_elementAntineoplastic AgentsCrystal structureCrystallography X-RayLigandsBiochemistryJurkat cellsInorganic ChemistryJurkat CellsOrganometallic CompoundsHumansPyrrolesCytotoxicityCoordination geometryPlatinumFormazansCell DeathDose-Response Relationship DrugMolecular StructureX-rayHydrogen Bonding2-benzoylpyrrole; copper(ii) and platinum(ii) complexes; cytotoxicityCarbon-13 NMRFlow CytometryCopperCrystallographycopper(ii) and platinum(ii) complexeschemistryxray cristallogrphycytotoxicityIndicators and ReagentsPlatinumCopper2-benzoylpyrroleJournal of inorganic biochemistry
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Estimation of the committed radiation dose resulting from gamma radionuclides ingested with food

2014

The objective of the study was to estimate the value of the radiation dose absorbed in consequence of consumption of popular food products for individual age groups. Potatoes, corn and sugar beet were selected for the study. Edible parts of these plants were collected in experimental fields of the KWS Lochow Polska Sp. z o.o. seeding company in Kondratowice (Poland). On the basis of the obtained study results, it can be stated that in consequence of consumption of the selected food products, people may receive increased doses from both natural and artificial radioactive isotopes. The doses calculated for several age groups do not show any health hazards in consequence of consumption of the …

40K137CsHealth Toxicology and MutagenesisArticleAnalytical ChemistryInorganic ChemistryToxicologyAge groupsRadiology Nuclear Medicine and imagingSpectroscopyRadionuclidebiologybusiness.industryEffective weighted doseRadiation dosedigestive oral and skin physiologyPublic Health Environmental and Occupational Healthfood and beveragesbiology.organism_classificationPollutionNuclear Energy and EngineeringFoodFood productsAbsorbed doseEnvironmental scienceSugar beetNuclear medicinebusinessJournal of Radioanalytical and Nuclear Chemistry
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A Phase I/II Dose-Escalation Multi-Center Study to Evaluate the Safety of Infusion of Natural Killer Cells or Memory T Cells As Adoptive Therapy in C…

2021

Abstract Background: Adoptive cell immunotherapies for opportunistic virus in immunocompromised patients using haploidentical memory T cells have shown to be safe and effective. Since severe cases of COVID-19 present a dysregulated immune system with T cell lymphopenia and a hyper-inflammatory state we have proposed that a similar strategy could be proven to be efficient for COVID-19 patients. This is a study protocol of an open-label, multicenter, double-arm, randomized, dose-finding phase I/II clinical trial to evaluate the feasibility, safety, tolerability, and efficacy of the administration of a single dose of allogenic SARS-CoV-2 specific memory CD45RA - T cells and Natural Killer (NK)…

704.Cellular Immunotherapies: Clinicalbusiness.industryImmunologyCell BiologyHematologymedicine.disease_causemedicine.diseaseBiochemistryPneumoniaPhase i iiMulti center studyImmunologymedicineDose escalationbusinessCoronavirusBlood
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New Tripentone Analogs with Antiproliferative Activity

2017

Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 a…

8H-thieno[23-b]pyrrolizinonePyridinesPharmaceutical SciencetripentonesApoptosis01 natural sciencesAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryThiopheneCytotoxic T cellCytotoxicityMolecular StructureCell Cycletripentoneproapoptotic agentsCell cycleBiochemistryChemistry (miscellaneous)MCF-7 CellsMolecular Medicineaza-indolesAntineoplastic Agents010402 general chemistryArticlelcsh:QD241-441Structure-Activity Relationshiplcsh:Organic chemistryCell Line TumormedicineHumansantitumor activityPhysical and Theoretical ChemistryMode of actionCell ProliferationDose-Response Relationship Drug010405 organic chemistryOrganic ChemistryCancermedicine.diseaseHCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciences8H-thieno[23-b]pyrrolizinoneschemistryApoptosisCell cultureaza-indoletripentones; aza-indoles; 8<i>H</i>-thieno[23-<i>b</i>]pyrrolizinones; antitumor activity; proapoptotic agentsCaco-2 CellsMolecules; Volume 22; Issue 11; Pages: 2005
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Planting Date and Different N-Fertilization Rates Differently Modulate Agronomic and Economic Traits of a Sicilian Onion Landrace and of a Commercial…

2022

The onion is one of the most widespread bulb vegetables worldwide. Onion cultivation is common in Sicily, as is the use of local genotypes. Cultivation practices are of particular interest in optimizing yield, quality, and profits. The aim of this study was to assess the agronomic response of a Sicilian landrace (Bianca Calda di Comiso, coded L1) and a commercial variety (Bianca di Maggio, coded V1) to different planting dates and N fertilization rates. An economic appraisal was also performed. The two genotypes were assessed using an experimental split-split-plot design with four levels of nitrogen rates (0, 80, 160, and 220 kg N ha&minus;1) and two different planting dates (8 October 2005…

<i>Allium cepa</i> L.; nitrogen dose; planting date; local genotype; cultivar; cost–benefit analysisPlant ScienceAllium cepa L cost–benefit analysis cultivar local genotype nitrogen dose planting dateHorticultureSettore AGR/02 - Agronomia E Coltivazioni ErbaceeHorticulturae
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A computation study to evaluate indoor gamma dose-rate on the basis of outdoor measurements

2006

A computation study to evaluate indoor gamma dose-rate on the basis of outdoor measurementsSettore MED/42 - Igiene Generale E Applicata
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DOSE RECOSTRUCTION IN IRRADIATED FOOD CONTAINING HYDROXIAPATITE USING ESR SPECTROMETRY

2012

ALIMENTI IRRADIATIRICOSTRUZIONE DELLA DOSESPETTROSCOPIA ESRSettore FIS/07 - Fisica Applicata(Beni Culturali Ambientali Biol.e Medicin)
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Human ABCB1 confers cells resistance to cytotoxic guanidine alkaloids from Pterogyne nitens.

2015

Multidrug resistance (MDR) caused by human ABCB1 (P-glycoprotein/MDR1) is one of the major obstacles in chemotherapy. To understand the mechanism of MDR by ABCB1 and circumvent the MDR, in the present study, we established human ABCB1-expressing cells (Flp-In-293/ABCB1 cells) and examined the cytotoxic effects of four guanidine alkaloids from Pterogyne nitens (galegine, nitensidine A, pterogynidine and pterogynine) using Flp-In-293/Mock and Flp-In-293/ABCB1 cells. The activity of ABCB1 in Flp-In-293/ABCB1 cells were confirmed by typical substrates for ABCB1 (taxol and vinblastine) in MTT assay. Flp-In-293/ABCB1 cells were also resistant to the four guanidine alkaloids as well as taxol and v…

ATP Binding Cassette Transporter Subfamily BCell SurvivalATPaseBiomedical EngineeringGuanidinesBiomaterialschemistry.chemical_compoundAlkaloidsmedicineCytotoxic T cellHumansMTT assayGuanidineCytotoxicityP-glycoproteinCaesalpiniabiologyDose-Response Relationship DrugCytotoxinsGeneral MedicineDrug Resistance MultipleVinblastineMultiple drug resistanceHEK293 CellschemistryBiochemistrybiology.proteinMultidrug Resistance-Associated Proteinsmedicine.drugBio-medical materials and engineering
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