Search results for "CEI"

showing 10 items of 1294 documents

Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents

2016

Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage of a computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives, we identified a new lead compound (i.e., 4a), bearing a vinyl ketone warhead and endowed with a promising antitrypanosomal activity against Trypanosoma brucei brucei (IC50 = 5.29 µM), coupled with a lack of cytotoxicity towards mammalian cells (TC50>100 µM).

0301 basic medicineTrypanosomaKetonePeptidomimeticPeptidomimeticStereochemistryTrypanosoma brucei bruceiClinical BiochemistryPharmaceutical ScienceTrypanosoma brucei01 natural sciencesBiochemistryCell LineBenzodiazepinesMiceStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundparasitic diseasesDrug DiscoveryAnimalsStructure–activity relationshipMoietyCytotoxicityMolecular BiologyMicrowave irradiationchemistry.chemical_classificationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryMacrophagesOrganic Chemistrybiology.organism_classificationMichael acceptors Microwave irradiation Peptidomimetics Pharmacokinetic parameters TrypanosomaTrypanocidal Agents0104 chemical sciencesPharmacokinetic parameter030104 developmental biologychemistryMichael reactionMolecular MedicineMichael acceptorLead compoundBioorganic & Medicinal Chemistry Letters
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Iron-loaded transferrin (Tf) is detrimental whereas iron-free Tf confers protection against brain ischemia by modifying blood Tf saturation and subse…

2018

Despite transferrin being the main circulating carrier of iron in body fluids, and iron overload conditions being known to worsen stroke outcome through reactive oxygen species (ROS)-induced damage, the contribution of blood transferrin saturation (TSAT) to stroke brain damage is unknown. The objective of this study was to obtain evidence on whether TSAT determines the impact of experimental ischemic stroke on brain damage and whether iron-free transferrin (apotransferrin, ATf)-induced reduction of TSAT is neuroprotective. We found that experimental ischemic stroke promoted an early extravasation of circulating iron-loaded transferrin (holotransferrin, HTf) to the ischemic brain parenchyma.…

0301 basic medicineU-PAGE urea-polyacrylamide gel electrophoresisMaleClinical BiochemistryExperimental strokeBiochemistryBrain IschemiaBrain ischemia0302 clinical medicineADC apparent diffusion coefficientApotransferrinDWI diffusion-weighted imagingTANDEM-1 Thrombolysis and Deferoxamine in Middle Cerebral Artery Occlusion clinical trialrHTf rat HTfrATf rat ATflcsh:QH301-705.5chemistry.chemical_classificationNeuronslcsh:R5-920ChemistryTransferrinExtravasationNS21 a medium supplement to grow neuronspDAPK-1 phosphorylated anti-death-associated protein kinase 1NeuroprotectionStrokeWB Western blotFemalemedicine.symptomlcsh:Medicine (General)Research PaperhHTf human HTfPC12 cell line derived from a pheochromocytoma of the rat adrenal medullamedicine.medical_specialtyIron OverloadBBB blood-brain barrierNMDAR N-methyl-D-aspartate receptorDCF dihydrofluoresceinIronWGA wheat germ agglutininHTf holotransferrinTransferrin receptorBrain damageTfR transferrin receptorDeferoxamineNeuroprotectionPI propidium iodide03 medical and health sciencesBrain damageCM conditioned mediumROS reactive oxygen speciesInternal medicine4-HNE 4-hydroxynonenalTf transferrinReceptors TransferrinmedicineFeRhoNoxTM-1 probe to detect Fe2+AnimalsHumansATf apotransferrinCM-H2DCFDA 5-chloromethyl-27-dichlorodihydrofluorescein diacetateMCAO middle cerebral artery occlusionDMT-1 divalent metal transporterB-27 a medium supplement to grow neuronsReactive oxygen speciesNMDA N-methyl-D-aspartateTSAT blood transferrin saturationTransferrin saturationBlood transferrin saturation (TSAT)Organic ChemistryNIR near infraredReactive oxygen species (ROS)medicine.diseasepMCAO permanent middle cerebral artery occlusionRatsPWI perfusion-weighted imaging030104 developmental biologyEndocrinologylcsh:Biology (General)TransferrinDAPK-1 anti-death-associated protein kinaseOGD oxygen/glucose deprivationTTC 235-triphenyl-tetrazolium chlorideLipid PeroxidationMCA middle cerebral arteryApoproteinsReactive Oxygen SpeciesMRI magnetic resonance imagingtMCAO transient middle cerebral artery occlusion030217 neurology & neurosurgeryhATf human ATf
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Holistic Optimization of Bioinformatic Analysis Pipeline for Detection and Quantification of 2′-O-Methylations in RNA by RiboMethSeq

2020

International audience; A major trend in the epitranscriptomics field over the last 5 years has been the high-throughput analysis of RNA modifications by a combination of specific chemical treatment(s), followed by library preparation and deep sequencing. Multiple protocols have been described for several important RNA modifications, such as 5-methylcytosine (m5C), pseudouridine (ψ), 1-methyladenosine (m1A), and 2'-O-methylation (Nm). One commonly used method is the alkaline cleavage-based RiboMethSeq protocol, where positions of reads' 5'-ends are used to distinguish nucleotides protected by ribose methylation. This method was successfully applied to detect and quantify Nm residues in vari…

0301 basic medicinebioinformatic pipelinelcsh:QH426-470Computer scienceComputational biologyDeep sequencingPseudouridine03 medical and health scienceschemistry.chemical_compound0302 clinical medicine[SDV.BBM.GTP]Life Sciences [q-bio]/Biochemistry Molecular Biology/Genomics [q-bio.GN]ribose methylationEpitranscriptomicsGeneticsGenetics (clinical)receiver operating characteristic2'-O-methylation2′-O-methylationhigh-throughput sequencingRNA[SDV.BBM.BM]Life Sciences [q-bio]/Biochemistry Molecular Biology/Molecular biologyBrief Research Reportlcsh:Genetics030104 developmental biologychemistry030220 oncology & carcinogenesisTransfer RNARNAMolecular MedicineSmall nuclear RNAReference genomeFrontiers in Genetics
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Bistacrines as potential antitrypanosomal agents

2017

Human African Trypanosomiasis (HAT) is caused by two subspecies of the genus Trypanosoma, namely Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense. The disease is fatal if left untreated and therapy is limited due to only five non-adequate drugs currently available. In preliminary studies, dimeric tacrine derivatives were found to inhibit parasite growth with IC50-values in the nanomolar concentration range. This prompted the synthesis of a small, but smart library of monomeric and dimeric tacrine-type compounds and their evaluation of antiprotozoal activity. Rhodesain, a lysosomal cathepsin-L like cysteine protease of T. brucei rhodesiense is essential for parasite survival a…

0301 basic medicinemedicine.drug_classTrypanosoma brucei bruceiClinical BiochemistryPharmaceutical ScienceFlavoproteinBiochemistryCell LineMiceStructure-Activity Relationship03 medical and health sciencesParasitic Sensitivity TestsOxidoreductaseparasitic diseasesDrug DiscoverymedicineAnimalsAfrican trypanosomiasisMolecular BiologyCell Proliferationchemistry.chemical_classificationDose-Response Relationship DrugMolecular StructurebiologyChemistryOrganic ChemistryTrypanosoma brucei rhodesiensemedicine.diseasebiology.organism_classificationTrypanocidal AgentsCysteine proteaseTrypanosomiasis African030104 developmental biologyBiochemistryTacrineTacrineAntiprotozoalbiology.proteinMolecular MedicineProtozoamedicine.drugBioorganic & Medicinal Chemistry
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Machine learning–XGBoost analysis of language networks to classify patients with epilepsy

2017

Our goal was to apply a statistical approach to allow the identification of atypical language patterns and to differentiate patients with epilepsy from healthy subjects, based on their cerebral activity, as assessed by functional MRI (fMRI). Patients with focal epilepsy show reorganization or plasticity of brain networks involved in cognitive functions, inducing ‘atypical’ (compared to ‘typical’ in healthy people) brain profiles. Moreover, some of these patients suffer from drug-resistant epilepsy, and they undergo surgery to stop seizures. The neurosurgeon should only remove the zone generating seizures and must preserve cognitive functions to avoid deficits. To preserve functions, one sho…

0301 basic medicinemedicine.medical_specialtyCognitive Neuroscience[SCCO.COMP]Cognitive science/Computer scienceAudiologyExtreme Gradient Boostinglcsh:Computer applications to medicine. Medical informaticsArticle03 medical and health sciencesEpilepsy0302 clinical medicineText miningMachine learningmedicineLanguagelcsh:Computer softwareEpilepsyCognitive mapReceiver operating characteristicbusiness.industryCognitionNeurophysiologymedicine.diseaseMLComputer Science ApplicationsStatistical classificationlcsh:QA76.75-76.765030104 developmental biologyNeurologyBinary classification[ SCCO.COMP ] Cognitive science/Computer sciencelcsh:R858-859.7Artificial intelligencePsychologybusiness030217 neurology & neurosurgeryAtypicalXGBoost
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Impact of freeze-thaw cytoablation on aqueous outflow patterns in ex vivo anterior chamber perfusion cultures and whole eyes

2022

Background: Porcine eyes have been widely used as ex vivo models in glaucoma research, as they share similar features with human eyes. Freeze-thawing is a non-invasive technique that has been used to obliterate living cells in anterior segment ex vivo cultures, to prepare them for further research such as cellular repopulation. This technique has previously been shown to reduce the intraocular pressure (IOP) in porcine eyes. The aim of this study was to investigate whether freeze-thaw cytoablation causes corresponding canalogram outflow changes in perfused anterior segment cultures (AFT) and whole porcine eyes (WFT). We hypothesized that the known IOP drop in AFT after trabecular meshwork a…

0301 basic medicinemedicine.medical_specialtyIntraocular pressuregenetic structuresvirusesGlaucomaTexas RedGeneral Biochemistry Genetics and Molecular Biology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineOphthalmologymedicineFluoresceinGeneral Pharmacology Toxicology and PharmaceuticsGeneral Immunology and MicrobiologyChemistryvirus diseasesGeneral Medicinebiochemical phenomena metabolism and nutritionmedicine.diseasedigestive system diseases030104 developmental biologymedicine.anatomical_structure030221 ophthalmology & optometryOutflowTrabecular meshworksense organsPerfusionEx vivoF1000Research
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Automated Categorization of Parkinsonian Syndromes Using Magnetic Resonance Imaging in a Clinical Setting

2020

Background Machine learning algorithms using magnetic resonance imaging (MRI) data can accurately discriminate parkinsonian syndromes. Validation in patients recruited in routine clinical practice is missing. Objective The aim of this study was to assess the accuracy of a machine learning algorithm trained on a research cohort and tested on an independent clinical replication cohort for the categorization of parkinsonian syndromes. Methods Three hundred twenty-two subjects, including 94 healthy control subjects, 119 patients with Parkinson's disease (PD), 51 patients with progressive supranuclear palsy (PSP) with Richardson's syndrome, 35 with multiple system atrophy (MSA) of the parkinsoni…

0301 basic medicinemedicine.medical_specialtyParkinson's diseaseParkinson's diseasemultiple system atrophyProgressive supranuclear palsyDiagnosis Differential03 medical and health sciences0302 clinical medicinePhysical medicine and rehabilitationParkinsonian DisordersmedicineHumansmultimodal magnetic resonance imagingReceiver operating characteristicmedicine.diagnostic_testbusiness.industryParkinsonismMagnetic resonance imagingprogressive supranuclear palsymedicine.diseaseMagnetic Resonance Imaging3. Good healthnervous system diseasesmachine learning algorithm030104 developmental biologyDiffusion Tensor ImagingNeurologyCategorizationnervous systemCohort[SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]Neurology (clinical)Supranuclear Palsy Progressivebusiness030217 neurology & neurosurgeryDiffusion MRI
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Validation of the Sepsis MetaScore for Diagnosis of Neonatal Sepsis

2016

What’s known on this subject Neonates are at increased risk for developing sepsis, but this population often exhibits ambiguous clinical signs that complicate the diagnosis of infection. No biomarker has yet shown enough diagnostic accuracy to rule out sepsis at the time of clinical suspicion. What this study adds We show that a gene-expression-based signature is an accurate objective measure of the risk of sepsis in a neonate or preterm infant, and it substantially improves diagnostic accuracy over that of commonly used laboratory-based testing. Implementation might decrease inappropriate antibiotic use. Background Neonatal sepsis can have devastating consequences, but accurate diagnosis i…

0301 basic medicinemedicine.medical_specialtyPopulationSepsis03 medical and health sciences0302 clinical medicinePredictive Value of Tests030225 pediatricsDrug Resistance BacterialmedicineHumansIntensive care medicineeducationRetrospective Studieseducation.field_of_studyNeonatal sepsisReceiver operating characteristicClinical Laboratory Techniquesbusiness.industryRetrospective cohort studyOriginal ArticlesGeneral Medicinemedicine.diseaseAnti-Bacterial Agents030104 developmental biologyInfectious DiseasesROC CurvePredictive value of testsPediatrics Perinatology and Child HealthCohortBiomarker (medicine)Neonatal SepsisTranscriptomebusinessJournal of the Pediatric Infectious Diseases Society
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Neither Cathodal nor Anodal Transcranial Direct Current Stimulation on the Left Dorsolateral Prefrontal Cortex alone or Applied During Moderate Aerob…

2020

There is converging evidence that both aerobic exercise (AE) and transcranial direct current stimulation (tDCS) can acutely modulate executive functions (EF). In addition, recent studies have proposed the beneficial effects of applying tDCS during AE on physical performance. This study aimed to investigate whether tDCS applied during an AE session additionally or differently effects EF. Therefore, five experiments were conducted in a counterbalanced pre-post-retention crossover design to explore the acute effects of tDCS and AE on EF (inhibition and updating) once in isolation (i.e., either cathodal, anodal tDCS or AE alone as controls) and once in a combined application (i.e., anodal and c…

0301 basic medicinemedicine.medical_specialtyTranscranial direct-current stimulationbusiness.industryGeneral Neurosciencemedicine.medical_treatmentPrefrontal CortexPhysical exercisePerceived exertionAudiologyNeuropsychological TestsExecutive functionsTranscranial Direct Current StimulationCrossover study03 medical and health sciencesExecutive Function030104 developmental biology0302 clinical medicineHeart ratemedicineAerobic exerciseAnalysis of variancebusinessExercise030217 neurology & neurosurgeryNeuroscience
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Development and Validation of a New Clinical Prediction Model of Catheter-Related Thrombosis Based on Vascular Ultrasound Diagnosis in Cancer Patients

2020

Background: Central venous catheters are convenient for drug delivery and improved comfort for cancer patients, but they also cause serious complications. The most common complication is catheter-related thrombosis (CRT). Objectives: This study aimed to evaluate the incidence and risk factors for CRT in cancer patients and develop an effective prediction model for CRT in cancer patients. Methods: The development of our prediction model was based on a retrospective cohort (n = 3,131) from the National Cancer Center. Our prediction model was confirmed in a prospective cohort from the National Cancer Center (n = 685) and a retrospective cohort from the Hunan Cancer Hospital (n = 61). The predi…

0301 basic medicinemedicine.medical_specialtylcsh:Diseases of the circulatory (Cardiovascular) systemMultivariate analysis030204 cardiovascular system & hematologyCardiovascular Medicinecathetersnomogram03 medical and health sciences0302 clinical medicineInternal medicinemedicinecancerRisk factorProspective cohort studythrombosisOriginal ResearchReceiver operating characteristicbusiness.industryCancerRetrospective cohort studyNomogrammedicine.disease030104 developmental biologyrisk factorlcsh:RC666-701CohortCardiology and Cardiovascular MedicinebusinessFrontiers in Cardiovascular Medicine
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