Search results for "Cytotoxicity"

showing 10 items of 865 documents

Bistacrine derivatives as new potent antimalarials

2016

Linking two tacrine molecules results in a tremendous increase of activity against Plasmodia in comparison to the monomer. This finding prompted the synthesis of a library of monomeric and dimeric tacrine derivatives in order to derive structure-activity relationships. The most active compounds towards chloroquine sensitive Plasmodium strain 3D7 and chloroquine resistant strain Dd2 show IC50 values in the nanomolar range of concentration, low cytotoxicity and target the cysteine protease falcipain-2, which is essential for parasite growth.

0301 basic medicinePlasmodiumSpectrometry Mass Electrospray IonizationStereochemistryProton Magnetic Resonance SpectroscopyClinical BiochemistryPharmaceutical Science01 natural sciencesBiochemistryAntimalarialsInhibitory Concentration 50Structure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundChloroquineResistant strainDrug DiscoverymedicineAnimalsStructure–activity relationshipCarbon-13 Magnetic Resonance SpectroscopyCytotoxicityMolecular BiologyStrain (chemistry)010405 organic chemistryOrganic ChemistryCysteine protease0104 chemical sciences030104 developmental biologyMonomerchemistryBiochemistryTacrineTacrineMolecular MedicineDimerizationmedicine.drugBioorganic & Medicinal Chemistry
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Cytotoxicity ofSalvia miltiorrhizaAgainst Multidrug-Resistant Cancer Cells

2016

Salvia miltiorrhiza Bunge (Lamiaceae) is a well-known Chinese herb that possesses numerous therapeutic activities, including anticancer effects. In this study, the cytotoxicity and the biological mechanisms of S. miltiorrhiza (SM) root extract on diverse resistant and sensitive cancer cell lines were investigated. CEM/ADR5000 cells were 1.68-fold resistant to CCRF-CEM cells, while HCT116 (p53[Formula: see text] and U87.MG[Formula: see text]EGFR cells were hypersensitive (collateral sensitive) compared to their parental cells. SM root extract stimulated ROS generation, cell cycle S phase arrest and apoptosis. The induction of the intrinsic apoptotic pathway was validated by increased cleavag…

0301 basic medicinePoly ADP ribose polymerasep38 mitogen-activated protein kinasesApoptosisSalvia miltiorrhizaCaspase 3PharmacologyBiologySalvia miltiorrhiza03 medical and health sciences0302 clinical medicineCell Line TumorNeoplasmsHumansCytotoxicityCell Cycle CheckpointsGeneral MedicineCell cycleAntineoplastic Agents PhytogenicMolecular biology030104 developmental biologyComplementary and alternative medicineDrug Resistance NeoplasmApoptosisCaspases030220 oncology & carcinogenesisCancer cellReactive Oxygen SpeciesDrugs Chinese HerbalThe American Journal of Chinese Medicine
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Release of copper-amended particles from micronized copper-pressure-treated wood during mechanical abrasion

2016

Background We investigated the particles released due to abrasion of wood surfaces pressure-treated with micronized copper azole (MCA) wood preservative and we gathered preliminary data on its in vitro cytotoxicity for lung cells. The data were compared with particles released after abrasion of untreated, water (0% MCA)-pressure-treated, chromated copper (CC)-pressure-treated wood, and varnished wood. Size, morphology, and composition of the released particles were analyzed. Results Our results indicate that the abrasion of MCA-pressure-treated wood does not cause an additional release of nanoparticles from the unreacted copper (Cu) carbonate nanoparticles from of the MCA formulation. Howev…

0301 basic medicinePreservativeCopper particlesAbrasion (mechanical)Cell SurvivalCytotoxicityIn vitro cytotoxicityBiomedical EngineeringNanoparticlechemistry.chemical_elementMedicine (miscellaneous)Pharmaceutical ScienceBioengineering010501 environmental sciences01 natural sciencesApplied Microbiology and BiotechnologyMass SpectrometryCell LineExposure03 medical and health sciencesPressureHumansCytotoxicity0105 earth and related environmental sciencesChemistryResearchtechnology industry and agricultureWaterCytotoxicity; Copper particles; Debris; Exposure; Inhalation; Wood dustMechanical abrasionCopperWood030104 developmental biologyInhalationA549 CellsMolecular MedicineNanoparticlesComposition (visual arts)DebrisReactive Oxygen SpeciesCopperWood dustNuclear chemistry
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A naturally occuring triterpene saponin ardisiacrispin B displayed cytotoxic effects in multi-factorial drug resistant cancer cells via ferroptotic a…

2018

WOS: 000432722700010

0301 basic medicineProgrammed cell deathCytotoxicitySaponinPharmaceutical ScienceApoptosisFlow cytometryCell Cycle Distribution03 medical and health sciencesArdisiacrispin BCell Line TumorDrug DiscoverymedicineFerroptosisHumansCytotoxic T cellOleanolic AcidCytotoxicityCaspaseMembrane Potential MitochondrialPharmacologybiologymedicine.diagnostic_testMitochondrial Membrane PotentialChemistryHep G2 CellsSaponinsHCT116 Cellsmedicine.diseaseAntineoplastic Agents PhytogenicDrug Resistance MultipleLeukemia030104 developmental biologyComplementary and alternative medicineDoxorubicinDrug Resistance NeoplasmApoptosisCaspasesCancer cellbiology.proteinCancer researchMolecular MedicineReactive Oxygen SpeciesPhytomedicine
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The alkaloid, soyauxinium chloride, displays remarkable cytotoxic effects towards a panel of cancer cells, inducing apoptosis, ferroptosis and necrop…

2020

Abstract The cytotoxic potential of a naturally occurring indoloquinazoline alkaloid, soyauxinium chloride (SCHL), was determined on a broad panel of animal and human cancer cell lines, including various sensitive and drug-resistant phenotypes. The cytotoxicity, SCHL-induced autophagic, ferroptotic, and necroptotic cell death were evaluated by the resazurin reduction assay (RRA). Caspase-Glo assay was used to detect the activity of caspases using spectrophotometric analysis. Flow cytometry was applied for cell cycle analysis (PI staining), apoptosis (annexin V/PI staining), mitochondrial membrane potential (MMP) (JC-1) and reactive oxygen species (ROS) (H2DCFH-DA). SCHL and doxorubicin (ref…

0301 basic medicineProgrammed cell deathNecroptosisAntineoplastic AgentsApoptosisToxicology03 medical and health sciences0302 clinical medicineCell Line TumorCytotoxic T cellFerroptosisHumansRegulated Cell DeathCytotoxicityCaspasebiologyChemistryCell CycleGeneral MedicineMolecular biology030104 developmental biologyCell cultureApoptosis030220 oncology & carcinogenesisCancer cellMitochondrial MembranesNecroptosisbiology.proteinReactive Oxygen SpeciesChemico-biological interactions
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Cytotoxicity of a naturally occuring spirostanol saponin, progenin III, towards a broad range of cancer cell lines by induction of apoptosis, autopha…

2020

Abstract This study was aimed to investigate the cytotoxic potential of a natural compound, progenin III on a broad range of cancer cell lines, including various sensitive and drug-resistant phenotypes. The cytotoxicity, progenin III-induced autophagic, ferroptotic and necroptotic cell death were evaluated by the resazurin reduction assay (RRA). Spectrophotometric analysis of caspases activity was performed using caspase-Glo assay. Flow cytometry was applied for cell cycle analysis (PI staining), apoptosis (annexin V/PI staining), mitochondrial membrane potential (MMP) (JC-1) and reactive oxygen species (ROS) (H2DCFH-DA). Progenin III and the reference molecule, doxorubicin exerted cytotoxi…

0301 basic medicineProgrammed cell deathNecroptosisMelanoma ExperimentalApoptosisToxicologyFlow cytometry03 medical and health sciences0302 clinical medicineAnnexinCell Line TumorAutophagySpirostansmedicineHumansCytotoxic T cellCytotoxicityCaspaseMembrane Potential MitochondrialCell Deathmedicine.diagnostic_testbiologyPlant ExtractsChemistryCell CycleHep G2 CellsGeneral MedicineSaponinsHCT116 CellsAntineoplastic Agents PhytogenicMolecular biology030104 developmental biologyDoxorubicinDrug Resistance NeoplasmApoptosisCaspases030220 oncology & carcinogenesisNecroptosisbiology.proteinReactive Oxygen SpeciesChemico-Biological Interactions
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Cytotoxicity of epunctanone and four other phytochemicals isolated from the medicinal plants Garcinia epunctata and Ptycholobium contortum towards mu…

2018

Abstract Introduction Resistance of cancer cells is a serious impediment to chemotherapy and several phytochemicals are active against multi-drug resistant (MDR) phenotypes. The cytotoxicity of five naturally occurring compounds: betulin (1), mundulea lactone (2), seputhecarpan A (3), seputheisoflavone (4) and epunctanone (5) was evaluated on a panel of 9 cancer cell lines including various sensitive and drug-resistant cell lines. The modes of action of compound 5 were further investigated. Methods The resazurin reduction assay was used to evaluate cytotoxicity of samples and ferroptotic cell death induced by compound 5; caspase-Glo assay was used to detect the activation of caspases in CCR…

0301 basic medicineProgrammed cell deathPhytochemicalsPharmaceutical ScienceApoptosisFlow cytometry03 medical and health sciences0302 clinical medicineCell Line TumorDrug DiscoverymedicineCytotoxic T cellHumansCytotoxicityPharmacologyMembrane Potential MitochondrialPlants Medicinalmedicine.diagnostic_testMolecular StructureChemistryPlant ExtractsFabaceaeHep G2 Cellsmedicine.diseaseMolecular biologyAntineoplastic Agents PhytogenicDrug Resistance MultipleLeukemia030104 developmental biologyComplementary and alternative medicineCell cultureApoptosisDoxorubicinDrug Resistance Neoplasm030220 oncology & carcinogenesisCaspasesCancer cellMolecular MedicineGarciniaReactive Oxygen SpeciesPhytomedicine : international journal of phytotherapy and phytopharmacology
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Leaf and Root Extracts from Campomanesia adamantium (Myrtaceae) Promote Apoptotic Death of Leukemic Cells via Activation of Intracellular Calcium and…

2017

Phytochemical studies are seeking new alternatives to prevent or treat cancer, including different types of leukemias. Campomanesia adamantium, commonly known as guavira or guabiroba, exhibits pharmacological properties including antioxidant, antimicrobial, and antiproliferative activities. Considering the anticancer potential of this plant species, the aim of this study was to evaluate the antileukemic activity and the chemical composition of aqueous extracts from the leaves (AECL) and roots (AECR) of C. adamantium and their possible mechanisms of action. The extracts were analyzed by LC-DAD-MS, and their constituents were identified based on the UV, MS, and MS/MS data. The AECL and AECR s…

0301 basic medicineProgrammed cell deathnatural productsbioprospectingCaspase 3PharmacologyJurkat cellsCalcium in biology03 medical and health scienceschemistry.chemical_compound0302 clinical medicinemedicinal plantcancerPharmacology (medical)Propidium iodideCytotoxicityCaspasePharmacologybiologylcsh:RM1-950LC-MSlcsh:Therapeutics. Pharmacology030104 developmental biologychemistryBiochemistryApoptosis030220 oncology & carcinogenesisbiology.proteinFrontiers in Pharmacology
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2018

High grade gliomas are the most common brain tumors in adult. These tumors are characterized by a high infiltration in microglial cells and macrophages. The immunosuppressive tumor environment is known to orient immune cells toward a pro-tumoral and anti-inflammatory phenotype. Therefore, the current challenge for cancer therapy is to find a way to reorient macrophages toward an antitumoral phenotype. Previously, we demonstrated that macrophages secreted antitumoral factors when they were invalidated for the proprotein converstase 1/3 (PC1/3) and treated with LPS. However, achieving an activation of macrophages via LPS/TLR4/Myd88-dependent pathway appears yet unfeasible in cancer patients. …

0301 basic medicineProprotein convertase 1medicine.diseaseBiochemistryMicrovesicles3. Good healthAnalytical Chemistry03 medical and health scienceschemistry.chemical_compound030104 developmental biologyImmune systemPaclitaxelchemistryCell cultureGliomaCancer researchTLR4medicineCytotoxicityMolecular BiologyMolecular & Cellular Proteomics
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Subacute effects of ozone exposure on cultivated human respiratory mucosa.

2001

This study was designed to investigate subacute effects of long-term exposure of both healthy and chronically inflamed human respiratory mucosa to ozone. Functional and metabolic effects on ciliary beat frequency (CBF), release of interleukin 8 (IL-8), interleukin 4 (IL-4), and γ interferon (g-INF), as well as cellular viability and cytotoxicity, were monitored. Cell cultures of 60 specimens (healthy mucosa: n = 30, inflamed mucosa: n = 30) were exposed to synthetic air and to ozone-enriched synthetic air in different concentrations of WO, 500, and WOO μg/m3. Continuous expositions were performed using an air/liquid interface cell culture technique for a period of 4 weeks. CBF was monitore…

0301 basic medicineRespiratory MucosaAdultmedicine.medical_specialtyTime FactorsAdolescentMucociliary clearanceCell Survivalmedicine.medical_treatmentRespiratory Mucosa03 medical and health scienceschemistry.chemical_compoundInterferon-gamma0302 clinical medicineOzoneLactate dehydrogenaseInternal medicinemedicineHumansInterleukin 8CiliaCytotoxicityInterleukin 4Cells CulturedAged030102 biochemistry & molecular biologybusiness.industryAirInterleukin-8Middle AgedCytokineEndocrinologyOtorhinolaryngologychemistry030220 oncology & carcinogenesisAnesthesiaRespiratory epitheliumInterleukin-4businessAmerican journal of rhinology
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