Search results for "Centration"

showing 10 items of 1914 documents

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

2016

International audience; 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.

0301 basic medicine300323-Dihydrobenzofuran privileged structure; Cancer; Inflammation; Molecular docking; mPGES-1 inhibitors; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003Amino Acid MotifsClinical BiochemistryGene ExpressionPharmaceutical Science01 natural sciencesClinical biochemistryBiochemistry[ CHIM ] Chemical SciencesProtein Structure Secondary[ SDV.CAN ] Life Sciences [q-bio]/Cancerchemistry.chemical_compoundLow affinityDrug DiscoveryEnzyme Inhibitors23-Dihydrobenzofuran privileged structure; Molecular docking; mPGES-1 inhibitors; Cancer; InflammationProstaglandin-E SynthasesCancerAnti-Inflammatory Agents Non-SteroidalBiological activityProto-Oncogene Proteins c-metIntramolecular OxidoreductasesMolecular Docking SimulationMolecular dockingMolecular Medicinelipids (amino acids peptides and proteins)Cell SurvivalStereochemistryMolecular Sequence Data2Antineoplastic Agents[SDV.CAN]Life Sciences [q-bio]/Cancer3-Dihydrobenzofuran privileged structureInhibitory Concentration 50Structure-Activity Relationship03 medical and health sciencesCell Line TumorMicrosomesHumans[CHIM]Chemical SciencesMolecular BiologyBenzofuransInflammationNatural product010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryEpithelial CellsmPGES-1 inhibitorsCombinatorial chemistryCombined approach0104 chemical sciences030104 developmental biologychemistryDrug DesignDrug Screening Assays Antitumor
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Evaluation of different conditions to enhance the performances of Lactobacillus pentosus OM13 during industrial production of Spanish-style table oli…

2017

The main objective was to set up a methodology to improve the high volume production of green table olives, cv. Nocellara del Belice. Lactobaccillus pentosus OM13 was applied during three different industrial processes of table olives as follows: trial one (IOP1) was subjected to an addition of lactic acid until a brine level of pH 7.0 was reached; trial two (IOP2) subjected to same addition of lactic acid as in trial one plus nutrient adjuvant; and trial three (IOP3) subjected to same addition of lactic acid as in trial one, but with the strain L. pentosus OM13 acclimatized in brine for 12 h before inoculation. These trials were compared against two untreated controls (spontaneously fermen…

0301 basic medicineAcclimatizationLactic acid bacteria Yeasts Nocellara del Belice table olives Starter culture Lactobacillus pentosus OM13 Acclimatization Nutrient adjuvant Lactic acid030106 microbiologyLactobacillus pentosusMicrobiologyAcclimatization03 medical and health scienceschemistry.chemical_compoundIndustrial MicrobiologyBriningOleaYeastsFood scienceLactic AcidAromabiologybusiness.industryProbioticsfood and beveragesSettore AGR/15 - Scienze E Tecnologie AlimentariHydrogen-Ion Concentrationbiology.organism_classificationLactobacillus pentosusBiotechnologyLactic acidSettore AGR/03 - Arboricoltura Generale E Coltivazioni ArboreeLactobacilluschemistryTasteFermentationFood MicrobiologyFermentationPediococcusSaltsbusinessLactobacillus plantarumSettore AGR/16 - Microbiologia AgrariaFood ScienceFood microbiology
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Adequate Urinary Iodine Concentration among Infants in the Inland Area of Norway

2021

Considering the importance of iodine to support optimal growth and neurological development of the brain and central nervous system, this study aimed to assess and evaluate iodine status in Norwegian infants. We collected data on dietary intake of iodine, iodine knowledge in mothers, and assessed iodine concentration in mother’s breast milk and in infant’s urine in a cross-sectional study at two public healthcare clinics in the inland area of Norway. In the 130 mother–infant pairs, the estimated infant 24-h median iodine intake was 50 (IQR 31, 78) µg/day. The median infant urinary iodine concentration (UIC) was 146 (IQR 93, 250) µg/L and within the recommended median defined by the World He…

0301 basic medicineAdultMalePediatricsmedicine.medical_specialtyknowledgeIodine intakeschemistry.chemical_elementNutritional Status030209 endocrinology & metabolismUrineBreast milkIodinePublic healthcareWorld healthArticle03 medical and health sciences0302 clinical medicineUrinary iodine concentrationsMedicineHumansTX341-641Infant Nutritional Physiological PhenomenaInland areasIodine intake030109 nutrition & dieteticsNutrition and DieteticsUICMilk HumanNutrition. Foods and food supplybusiness.industryinfantsiodineNorwayDietary intakeInfant NewbornInfanturinary iodine concentrationiodine intakeinland areaBreast FeedingCross-Sectional StudiesVDP::Medisinske Fag: 700::Helsefag: 800chemistryFemaleUrinary iodinebusinessFood Science
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Anticancer, antioxidant, and antibacterial activities of low molecular weight bioactive subfractions isolated from cultures of wood degrading fungus …

2017

The aim of this study is to investigate in vitro the anticancer, antioxidant, and antibacterial activities of three low molecular weight subfractions I, II and III isolated from secondary metabolites produced by the wood degrading fungus Cerrena unicolor. The present study demonstrated that the low molecular weight subfractions III exhibited the strongest inhibitory activity towards breast carcinoma cells MDA-MB-231, prostatic carcinoma cells PC3, and breast cancer cells MCF7 with the half-maximal inhibitory concentration (IC50) value of 52,25 μg/mL, 60,66 μg/mL, and 54,92 μg/mL, respectively. The highest percentage of inhibition was noted at a concentration of 300 μg/mL in all the examined…

0301 basic medicineAntioxidantStaphylococcusmedicine.medical_treatmentlcsh:MedicineBacillusLaccasesBacillus subtilisPathology and Laboratory Medicinemedicine.disease_causeBiochemistryAntioxidantsNeoplasmsMedicine and Health SciencesCerrena unicolorStaphylococcus AureusFood sciencelcsh:ScienceMultidisciplinarybiologyAntimicrobialsChemistryDrugsEukaryota04 agricultural and veterinary sciencesWood040401 food scienceAnti-Bacterial AgentsBacterial PathogensEnzymesChemistryBacillus SubtilisExperimental Organism SystemsMedical MicrobiologyStaphylococcus aureusPhysical SciencesMCF-7 CellsProkaryotic ModelsPathogensAntibacterial activityResearch ArticleAntineoplastic AgentsResearch and Analysis MethodsMicrobiology03 medical and health sciencesMinimum inhibitory concentration0404 agricultural biotechnologyPhenolsMicrobial ControlmedicineHumansMicrobial PathogensIC50PharmacologyBacterialcsh:RChemical CompoundsOrganismsFungiBiology and Life SciencesProteinsbiology.organism_classificationIn vitro030104 developmental biologyEnzymologyAntibacterialslcsh:QPolyporalesPLOS ONE
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Biosynthesis of selenium-nanoparticles and -nanorods as a product of selenite bioconversion by the aerobic bacterium Rhodococcus aetherivorans BCP1

2018

The wide anthropogenic use of selenium compounds represents the major source of selenium pollution world- wide, causing environmental issues and health concerns. Microbe-based strategies for metal removal/recovery have received increasing interest thanks to the association of the microbial ability to detoxify toxic metal/ metalloid polluted environments with the production of nanomaterials. This study investigates the tolerance and the bioconversion of selenite (SeO32−) by the aerobically grown Actinomycete Rhodococcus aetherivorans BCP1 in association with its ability to produce selenium nanoparticles and nanorods (SeNPs and SeNRs). The BCP1 strain showed high tolerance towards SeO32− with…

0301 basic medicineBioconversionStatic Electricity030106 microbiologychemistry.chemical_elementBioengineeringSelenious AcidSettore BIO/19 - Microbiologia GeneraleSelenium pollutionSelenium03 medical and health sciencesMinimum inhibitory concentrationchemistry.chemical_compoundNanoparticleBiosynthesisRhodococcusParticle SizeSelenite Rhodococcus aetherivorans Selenium nanoparticles Selenium nanorods Biogenic nanostructuresSelenium nanorodMolecular BiologyNanotubesbiologyBiogenic nanostructureRhodococcus aetherivoranSpectrometry X-Ray EmissionGeneral Medicinebiology.organism_classificationDynamic Light ScatteringSelenium nanoparticleBacteria AerobicNanotube030104 developmental biologychemistryBiochemistry13. Climate actionSelenious AcidSeleniteNanoparticlesMetalloidRhodococcusSeleniumRhodococcuBiotechnologyNew Biotechnology
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Cytotoxic effects induced by patulin, deoxynivalenol and toxin T2 individually and in combination in hepatic cells (HepG2).

2018

Abstract Patulin (PAT), deoxynivalenol (DON) and toxin T-2 (T-2) are mycotoxins distributed worldwide in food and feed. Cytotoxicity of the three mycotoxins individually or in combination in human hepatocellular carcinoma (HepG2) cells was evaluated by MTT assay over 24, 48 and 72 h of exposure. The concentration ranges used were 0.625–15 μM for DON, 1.25–50 nM for T-2 and 0.45–7.5 μM for PAT. The IC 50 values obtained ranged from 9.30 to 2.53 μM, from 33.69 to 44.37 nM and from 2.66 to 1.17 μM for DON, T-2 and PAT, respectively. The most cytotoxic mycotoxin to HepG2 cells was T-2 followed by PAT and DON. The combination ratios used for the mixtures were 1:3 (DON: T-2), 1:5 (DON: PAT), 1:1.…

0301 basic medicineCell SurvivalComplex MixturesToxicologymedicine.disease_causePatulin03 medical and health scienceschemistry.chemical_compoundInhibitory Concentration 500404 agricultural biotechnologymedicineCytotoxic T cellHumansMTT assayDrug InteractionsCytotoxicityMycotoxinDose-Response Relationship DrugToxin04 agricultural and veterinary sciencesGeneral MedicineHep G2 CellsMycotoxinsmedicine.disease040401 food scienceMolecular biologyDrug CombinationsT-2 Toxin030104 developmental biologyPatulinchemistryLiverHepatocellular carcinomaHepatic stellate cellTrichothecenesFood ScienceFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association
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Chemical Composition, In Vitro Antitumor and Pro-Oxidant Activities of Glandora rosmarinifolia (Boraginaceae) Essential Oil

2018

The biological properties of essential oils have been demonstrated in the treatment of several diseases and to enhance the bioavailability of other drugs. In natural habitats the essential oils compounds may play important roles in the protection of the plants as antibacterials, antivirals, antifungals, insecticides and also against herbivores by reducing their appetite for such plants or by repelling undesirable others. We analyzed by gas-chromatography mass spectrometry the chemical composition of the essential oil of aerial parts of Glandora rosmarinifolia (Ten.) D.C. Thomas obtained by hydrodistillation and verified some biological activities on a panel of hepatocellular carcinoma cell …

0301 basic medicineChemical RadicalsAntioxidantmedicine.medical_treatmentMDA-MB-231Cancer Treatmentlcsh:MedicinenaphthoquinoneChemical CompositionBiochemistryPhysical ChemistryditerpeneAntioxidantslaw.invention0302 clinical medicinelawBreast TumorsSUM 149Medicine and Health SciencesBioassaySettore BIO/15 - Biologia FarmaceuticaCytotoxicitylcsh:ScienceMultidisciplinarybiologyTraditional medicineChemistryLiver DiseasesBoraginaceaeBoraginaceaeOxidantsHep3BLipidsChemistryOncology030220 oncology & carcinogenesisPhysical SciencesResearch ArticleHepG2Free RadicalsCell SurvivalGastroenterology and HepatologyCarcinomas03 medical and health sciencesInhibitory Concentration 50Cell Line TumorAromatic HydrocarbonsGastrointestinal TumorsBreast CancermedicineOils VolatileHumansPlant OilsEssential oilcytotoxic activityHA22T/VGH; HepG2; Hep3B; SUM 149; MDA-MB-231; cytotoxic activity; diterpenes; naphthoquinones; plant secondary metabolitesVolatile Organic CompoundsDose-Response Relationship DrugCell growthPlant ExtractsHA22T/VGHlcsh:RChemical CompoundsBiology and Life SciencesCancers and NeoplasmsEpithelial CellsHepatocellular CarcinomaSettore CHIM/06 - Chimica OrganicaPlant Components Aerialbiology.organism_classificationPro-oxidantplant secondary metabolitesAntineoplastic Agents PhytogenicHydrocarbonsBioavailability030104 developmental biologySettore BIO/03 - Botanica Ambientale E ApplicataHepatocytesSettore BIO/14 - Farmacologialcsh:QOils
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Hyperosmolarity and Benzalkonium Chloride Differently Stimulate Inflammatory Markers in Conjunctiva-Derived Epithelial Cells in vitro

2017

Tear hyperosmolarity is known to cause ocular surface inflammation in dry eye syndrome. Benzalkonium chloride (BAK), an eyedrop preservative, is known to induce dry eye in long-term-treated patients. Analyzing the modulation of the proinflammatory potential of hyperosmolarity in the presence of BAK on the conjunctiva could give new insights into the effect of this preservative on the disease. In a hyperosmolar model on a conjunctiva-derived cell line, and in the presence of BAK, we evaluated key inflammatory markers [CCL2, IL-8, IL-6, macrophage migration inhibitory factor (MIF) and intercellular adhesion molecule (ICAM)-1] as well as the osmoprotectant element nuclear factor of activated T…

0301 basic medicineConjunctivaCell Survival[SDV]Life Sciences [q-bio]Enzyme-Linked Immunosorbent AssayInflammationPharmacologyCell LineProinflammatory cytokine03 medical and health sciencesCellular and Molecular NeuroscienceBenzalkonium chloride0302 clinical medicineNFAT5medicineHumansChemokine CCL2ComputingMilieux_MISCELLANEOUSInterleukin-6ChemistryInterleukin-8Osmolar ConcentrationPreservatives PharmaceuticalEpithelial CellsNFATGeneral MedicineAnatomyConjunctivitisIntercellular Adhesion Molecule-1Intercellular adhesion moleculeSensory Systems[SDV] Life Sciences [q-bio]Ophthalmology030104 developmental biologymedicine.anatomical_structure030221 ophthalmology & optometryMacrophage migration inhibitory factorbiological phenomena cell phenomena and immunitymedicine.symptomBenzalkonium CompoundsConjunctivaBiomarkersmedicine.drug
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Identification of an optimized 2′-O-methylated trinucleotide RNA motif inhibiting Toll-like receptors 7 and 8

2017

Bacterial RNA serves an important function as activator of the innate immune system. In humans bacterial RNA is sensed by the endosomal receptors TLR7 and TLR8. Differences in the posttranscriptional modification profile of prokaryotic when compared with eukaryotic RNA allow innate immune cells to discriminate between “host” and “foreign” RNA. Ribose 2′-O-methylation is of particular importance and has been reported to antagonize TLR7/8 activation. Yet, the exact sequence context in which 2′-O-methylation has to occur to mediate its inhibitory activity remains largely undefined. On the basis of a naturally occurring 2′-O-methylated RNA sequence, we performed a systematic permutation of the …

0301 basic medicineCytidineBiologyBioinformaticsMethylationInhibitory Concentration 5003 medical and health scienceschemistry.chemical_compound0302 clinical medicineRNA TransferReportRiboseHumansNucleotideNucleotide MotifsMolecular Biologychemistry.chemical_classificationInnate immune systemNucleotides2'-O-methylationRNATLR7TLR8Cell biologyRNA Bacterial030104 developmental biologyToll-Like Receptor 7chemistryToll-Like Receptor 8MutationLeukocytes MononuclearNucleic acidRNA030215 immunologyRNA
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Bioequivalence decision for nanoparticular iron complex drugs for parenteral administration based on their disposition

2017

Although parenteral iron products have been established to medicinal use decades before, their structure and pharmacokinetic properties are not fully characterized yet. With its' second reflection paper on intravenous iron-based nano-colloidal products (EMA/CHMP/SWP/620008/2012) the European Medicine Agency provided an extensive catalogue of methods for quality, non-clinical and pharmacokinetic studies for the comparison of nano-sized iron products to an originator (EMA, 2015). For iron distribution studies, the reflection paper assumed the use of rodents. In our tests, we used a turkey fetus model to investigate time dependent tissue concentrations in pharmacological and toxicological rele…

0301 basic medicineEmbryo NonmammalianTissue concentrationsTurkeyAmylopectinDose dependenceBioequivalencePharmacologyKidneyToxicologyFerric CompoundsGlucaric Acid03 medical and health sciences0302 clinical medicinePharmacokineticsAnimalsDistribution (pharmacology)MedicineIron complexMaltoseFerric Oxide Saccharatedbusiness.industryMyocardiumGeneral MedicineDisposition030104 developmental biologyLiverTherapeutic Equivalency030220 oncology & carcinogenesisModels AnimalNanoparticlesIron-Dextran ComplexbusinessParenteral ironRegulatory Toxicology and Pharmacology
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