Search results for "TOXICITY"

showing 10 items of 2261 documents

Saponins-mediated potentiation of cisplatin accumulation and cytotoxicity in human colon cancer cells.

2002

The triterpene saponins jenisseensosides A, B, C, D were found to increase the accumulation and cytotoxicity of the anticancer agent cisplatin in human colon tumor cells. These compounds are glycosides of quillaic acid whose fucose residue was acylated by a trans- or cis-p methoxycinnamic acid. In contrarst, other saponins derivatives without this acyl moiety were not found to potentiate the accumulation and cytotoxicity of cisplatin. These results suggested the importance of the acyl moiety for activity.

Cell SurvivalSaponinPharmaceutical SciencePlant RootsFucoseAnalytical Chemistrychemistry.chemical_compoundStructure-Activity RelationshipTriterpeneDrug DiscoverymedicineMoietyHumansOleanolic AcidCytotoxicitySilenePlatinumPharmacologychemistry.chemical_classificationCisplatinDose-Response Relationship DrugPlant ExtractsOrganic ChemistryGlycosideBiological activityDrug SynergismSaponinsTriterpenesComplementary and alternative medicinechemistryBiochemistryMolecular Medicinelipids (amino acids peptides and proteins)CisplatinHT29 Cellsmedicine.drugPlanta medica
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Cyclic heptapeptides from the soil-derived fungus Clonostachys rosea

2019

Abstract Three new cyclic heptapeptides (1–3) together with three known compounds (4–6) were isolated from a solid rice culture of the soil-derived fungus Clonostachys rosea. Fermentation of the fungus on white beans instead of rice afforded a new γ-lactam (7) and a known γ-lactone (8) that were not detected in the former extracts. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. Compounds 1 and 4 exhibited significant cytotoxicity against the L5178Y mouse lymphoma cell line with IC50 values of 4.1 and 0.1 µM, respectively. Compound 4 also displayed cytotoxicity against the A2780 human ovarian cancer cell line with an IC50…

Cell SurvivalStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsFungusPeptides Cyclic01 natural sciencesBiochemistryMiceStructure-Activity RelationshipCell Line TumorDrug DiscoveryIc50 valuesAnimalsHumansCytotoxicityMolecular BiologyIC50Cell ProliferationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryChemistryOrganic ChemistryGliocladiumbiology.organism_classification0104 chemical sciences010404 medicinal & biomolecular chemistryCell cultureFermentationClonostachys roseaMolecular MedicineFermentationDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopyBioorganic & Medicinal Chemistry
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Toxicity evaluation of individual and mixed enniatins using an in vitro method with CHO-K1 cells

2013

Enniatins (ENs) A, A1, B and B1 are produced by Fusarium species. They are known as emerging fusario- toxins, and can cause outbreaks in both humans and animals. ENs elicits a wide range of different biolog- ical properties and toxicological effects, and their co-occurrence may enhance the extent of these hazards. As the potential toxins reach in vitro cells in the same way as they would in vivo, cytotoxicity was studied with CHO-K1, which is considered one of the most sensitive cell lines for preliminary screen- ing of cytotoxicity studies. In this study, individual cytotoxic effects of ENs were evaluated by MTT assay after exposing ENs to CHO-K1 cells for 24, 48, and 72 h. The IC50 values…

Cell SurvivalStereochemistryTetrazolium SaltsCHO CellsGeneral MedicineMycotoxinsBiologyToxicologyMolecular biologyIn vitroThiazolesSensitive cellCricetulusIn vivoCricetinaeDepsipeptidesToxicity TestsToxicityAnimalsCytotoxic T cellMTT assayCytotoxicityAntagonismToxicology in Vitro
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Zinc overload mediated by zinc oxide nanoparticles as innovative anti-tumor agent

2017

The predicted global cancer burden is expected to surpass 20 million new cancer cases by 2025. Despite recent advancement in tumor therapy, a successful cancer treatment remains challenging. The emerging field of nanotechnology offers great opportunities for diagnosis, imaging, as well as treatment of cancer. Zinc oxide nanoparticles (ZnO NP) were shown to exert selective cytotoxicity against tumor cells via a yet unknown mechanism, most likely involving the generation of reactive oxygen species (ROS). These nanoparticles are a promising therapeutic opportunity as zinc is a nontoxic trace element and its application in medically-related products is considered to be safe. We could show that …

Cell SurvivalSurface PropertiesNanoparticlechemistry.chemical_elementAntineoplastic AgentsApoptosisZinc010501 environmental sciences01 natural sciencesBiochemistryInorganic ChemistryStructure-Activity Relationship03 medical and health sciences0302 clinical medicineTumor Cells CulturedHumansCytotoxic T cellParticle SizeCytotoxicityCell Proliferation0105 earth and related environmental scienceschemistry.chemical_classificationReactive oxygen speciesDose-Response Relationship DrugChemistryCell growthZincApoptosisCell cultureCancer researchNanoparticlesMolecular MedicineZinc Oxide030217 neurology & neurosurgeryJournal of Trace Elements in Medicine and Biology
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In vitro effects of aminobisphosphonates on Vgamma9Vdelta2 T cell activation and differentiation.

2006

In this study we have evaluated the in vitro effects of four different aminobisphosphonates, alendronate, risedronate, neridronate and zoledronate, on Vγ9Vδ2 T cell activation and differentiation. All tested aminobisphosphonates induce an IL-2-dependent activation and expansion of Vγ9Vδ2 T lymphocytes in primary PBMC cultures of healthy donors. Most notably, they also determine a different distribution of Vγ9Vδ2 T cell subsets, with decrease of Tnaive and TCM cells and increase of TEM and TEMRA Vγ9Vδ2 cells, indicating that in vitro treatment with aminobisphosphonates induces Vγ9Vδ2 T lymphocytes to differentiate towards an effector/cytotoxic phenotype. Accordingly, Vγ9Vδ2 T lymphocytes cu…

Cell SurvivalT cellT-LymphocytesImmunologyLymphocyte ActivationPeripheral blood mononuclear cellMonocytesFlow cytometry03 medical and health sciencesInterferon-gamma0302 clinical medicinemedicineImmunology and AllergyCytotoxic T cellHumansCytotoxicityImage CytometryPharmacologymedicine.diagnostic_testBone Density Conservation AgentsDiphosphonatesChemistryEffectorCell DifferentiationFlow CytometryPhenotypeIn vitromedicine.anatomical_structure030220 oncology & carcinogenesisCancer research030215 immunologyInternational journal of immunopathology and pharmacology
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Study of the cytotoxic activity of beauvericin and fusaproliferin and bioavailability in vitro on Caco-2 cells.

2010

Abstract Beauvericin (BEA) is a cyclohexadepsipeptide mycotoxin which has insecticidal properties and produces cytotoxic effects in mammalian cells. Fusaproliferin (FUS) is a mycotoxin that has toxic activity against brine shrimp, insect cells, and teratogenic effects on chicken embryos. The aim of this study was to determine the cytotoxicity of BEA and FUS in human epithelial colorectal adenocarcinoma HT-29 and Caco-2 cells, the transepithelial transport and the bioavailability using Caco-2 cells as a simulated in vitro gastrointestinal model of the human intestinal epithelium. The inhibitory concentration (IC 50 ) evidenced by BEA in the Caco-2 cells was 24.6 and 12.7 μM at 24 and 48 h ex…

Cell SurvivalTerpenesBiological AvailabilityGeneral MedicinePharmacologyBiologyToxicologyIntestinal epitheliumIn vitroBeauvericinBioavailabilitychemistry.chemical_compoundInhibitory Concentration 50chemistryCaco-2DepsipeptidesCytotoxic T cellHumansCaco-2 CellsDrug Screening Assays AntitumorCytotoxicityMycotoxinFood ScienceChromatography LiquidFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association
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Multiparametric evaluation of the cytoprotective effect of the Mangifera indica L. stem bark extract and mangiferin in HepG2 cells.

2012

Abstract Objective Mango (Mangifera indica L.) stem bark extract (MSBE) is a natural product with biological properties and mangiferin is the major component. This paper reported the evaluation of the protective effects of MSBE and mangiferin against the toxicity induced in HepG2 cells by tert-butyl hydroperoxide or amiodarone. Method Nuclear morphology, cell viability, intracellular calcium concentration and reactive oxygen species (ROS) production were measured by using a high-content screening multiparametric assay. Key findings MSBE and mangiferin produced no toxicity below 500 mg/ml doses. A marked recovery in cell viability, which was reduced by the toxicants, was observed in cells pr…

Cell SurvivalXanthonesPharmaceutical ScienceAmiodaronePharmacologychemistry.chemical_compoundtert-ButylhydroperoxidemedicineHumansMangiferaViability assayATP Binding Cassette Transporter Subfamily B Member 1MangiferinP-glycoproteinPharmacologychemistry.chemical_classificationReactive oxygen speciesMangiferabiologyDose-Response Relationship DrugPlant StemsPlant ExtractsHep G2 Cellsmedicine.diseaseCytoprotectionMitochondrial toxicityBiochemistrychemistryToxicitybiology.proteinPlant BarkCalciumReactive Oxygen SpeciesThe Journal of pharmacy and pharmacology
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Cell Culture Characterization of Prooxidative Chain-Transfer Agents as Novel Cytostatic Drugs

2021

Prooxidative therapy is a well-established concept in infectiology and parasitology, in which prooxidative drugs like artemisinin and metronidazole play a pivotal clinical role. Theoretical considerations and earlier studies have indicated that prooxidative therapy might also represent a promising strategy in oncology. Here, we have investigated a novel class of prooxidative drugs, namely chain-transfer agents, as cytostatic agents in a series of human tumor cell lines in vitro. We have found that different chain-transfer agents of the lipophilic thiol class (like dodecane-1-thiol) elicited half-maximal effective concentrations in the low micromolar range in SY5Y cells (human neuroblastoma)…

Cell Survivallipophilic thiolCellular differentiationPharmaceutical ScienceOrganic chemistryfree radical chain reactionAntineoplastic AgentschemotherapyAntioxidantsArticleAnalytical Chemistryradical propagationHeLaQD241-441Coordination ComplexesNeuroblastomaDrug DiscoverymedicineTumor Cells CulturedHumansDoxorubicinSulfhydryl CompoundsPhysical and Theoretical ChemistryCytotoxicityoxidative cell deathCell Proliferationprooxidative drugbiologyChemistryHEK 293 cellslipid peroxidationbiology.organism_classificationmedicine.diseaseCytostatic Agentschain-transfer agentIn vitroChemistry (miscellaneous)Cell cultureCancer researchMolecular MedicineNitrogen OxidesDrug Screening Assays Antitumormedicine.drugrate-limiting stepMolecules
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Cytotoxicity, anti-angiogenic, apoptotic effects and transcript profiling of a naturally occurring naphthyl butenone, guieranone A

2012

Abstract Background Malignant diseases are responsible of approximately 13% of all deaths each year in the world. Natural products represent a valuable source for the development of novel anticancer drugs. The present study was aimed at evaluating the cytotoxicity of a naphtyl butanone isolated from the leaves of Guiera senegalensis, guieranone A (GA). Results The results indicated that GA was active on 91.67% of the 12 tested cancer cell lines, the IC50 values below 4 μg/ml being recorded on 83.33% of them. In addition, the IC50 values obtained on human lymphoblastic leukemia CCRF-CEM (0.73 μg/ml) and its resistant subline CEM/ADR5000 (1.01 μg/ml) and on lung adenocarcinoma A549 (0.72 μg/m…

Cell cycle checkpointCytotoxicityApoptosisMicroarrayBiologyBioinformaticslcsh:RC254-282BiochemistryAngiogensismedicineCytotoxic T cellDoxorubicinlcsh:QH573-671CytotoxicityMolecular Biologylcsh:CytologyResearchCell BiologyCell cyclelcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogensMolecular biologyChorioallantoic membraneCell cultureApoptosisGuieranone APharmacogenomicsmedicine.drugCell Division
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Antitumoural properties of benzannelated seven-membered 5-fluorouracil derivatives and related open analogues. Molecular markers for apoptosis and ce…

2005

Attention is increasingly being focussed on the cell cycle and apoptosis as potential targets for therapeutic intervention in cancer. We prepared a series of bioisosteric benzannelated seven-membered 5-FU O,N-acetals to test them against the MCF-7 human breast cancer cell line. Benzo-fused seven-membered O,O-acetals or their acyclic analogues led to the expected 5-FU O,N-acetals (or aminals), in addition to six- and 14-membered aminal structures and acyclic compounds. All the cyclic aminals provoked a G0/G1-phase cell cycle arrest, whereas Ftorafur, a known prodrug of 5-FU, and 1-[2-(2-hydroxymethyl-4-nitrophenoxy)-1-methoxyethyl]-5-fluorouracil (11) induced an S-phase cell cycle arrest. Al…

Cell cycle checkpointPharmaceutical ScienceAntineoplastic AgentsApoptosisBreast NeoplasmsStructure-Activity RelationshipBreast cancerDrug DiscoverymedicineBenzene DerivativesTumor Cells CulturedHumansCytotoxicityChemistryCell CycleG1 PhaseCancerCell cycleProdrugmedicine.diseaseFluorouracilApoptosisDrug DesignImmunologyCancer researchFluorouracilHT29 Cellsmedicine.drugFarmaco (Societa chimica italiana : 1989)
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