Search results for "Niacin"

showing 10 items of 89 documents

Kinase Inhibitors in Multitargeted Cancer Therapy

2017

The old-fashioned anticancer approaches, aiming in arresting cancer cell proliferation interfering with non-specific targets (e.g. DNA), have been replaced, in the last decades, by more specific target oriented ones. Nonetheless, single-target approaches have not always led to optimal outcomes because, for its complexity, cancer needs to be tackled at various levels by modulation of several targets. Although at present, combinations of individual single-target drugs represent the most clinically practiced therapeutic approaches, the modulation of multiple proteins by a single drug, in accordance with the polypharmacological strategy, has become more and more appealing. In the perspective of…

0301 basic medicineDrugNiacinamideIndolesPyridinesmedia_common.quotation_subjectPharmacologyBioinformaticsBiochemistryReceptor tyrosine kinase03 medical and health sciencesCrizotinibPiperidinesMultitargeted drugs anticancer agents polypharmacology tyrosine kinase receptors oncogene addiction tumor microenvironment FDA-approved drugsNeoplasmsDrug DiscoverymedicineSunitinibHumansAnilidesPyrrolesProtein Kinase Inhibitorsmedia_commonPharmacologyTumor microenvironmentbiologybusiness.industryPhenylurea CompoundsOrganic ChemistryImidazolesCancerReceptor Protein-Tyrosine KinasesSorafenibmedicine.diseaseOncogene AddictionSettore CHIM/08 - Chimica FarmaceuticaClinical trialPyridazines030104 developmental biologyMechanism of actionbiology.proteinImatinib MesylateQuinazolinesMolecular MedicinePyrazolesmedicine.symptombusinessTyrosine kinase
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NUPR1, a new target in liver cancer: implication in controlling cell growth, migration, invasion and sorafenib resistance

2016

AbstractSorafenib, an oral multikinase inhibitor, is the only approved agent for the treatment of advanced hepatocellular carcinoma (HCC). However, its benefits are modest, and as its mechanisms of action remain elusive, a better understanding of its anticancer effects is needed. Based on our previous study results, we investigated here the implication of the nuclear protein 1 (NUPR1) in HCC and its role in sorafenib treatment. NUPR1 is a stress-inducible protein that is overexpressed in various malignancies, but its role in HCC is not yet fully understood. We found that NUPR1 expression was significantly higher in primary human HCC samples than in the normal liver. Knockdown of NUPR1 signi…

0301 basic medicineMaleCancer ResearchHepatocellular carcinomaCore Binding Factor Alpha 1 Subunit0302 clinical medicineCell MovementBasic Helix-Loop-Helix Transcription FactorsMolecular Targeted TherapyRNA Small InterferingRegulation of gene expressionAged 80 and overGene knockdownRELBLiver NeoplasmsMiddle AgedSorafenib3. Good healthNeoplasm ProteinsSorafenib.Gene Expression Regulation Neoplastic030220 oncology & carcinogenesisGene Knockdown TechniquesOriginal ArticleFemalemedicine.drugSorafenibNiacinamideCarcinoma HepatocellularRUNX2 GeneCell SurvivalIER3ImmunologyDown-RegulationBiology03 medical and health sciencesCellular and Molecular NeuroscienceYoung AdultmedicineGene silencingHumansNeoplasm InvasivenessGene SilencingneoplasmsAgedCell ProliferationCell growthGene Expression ProfilingPhenylurea CompoundsTranscription Factor RelBComputational BiologyMembrane ProteinsCell BiologyNuclear protein-1digestive system diseases030104 developmental biologyDrug Resistance NeoplasmCancer researchApoptosis Regulatory ProteinsTranscriptomeCell Death & Disease
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Effects of an Antimutagenic 1,4-Dihydropyridine AV-153 on Expression of Nitric Oxide Synthases and DNA Repair-related Enzymes and Genes in Kidneys of…

2016

Development of complications of diabetes mellitus (DM), including diabetic nephropathy, is a complex multi-stage process, dependent on many factors including the modification of nitric oxide (NO) production and an impaired DNA repair. The goal of this work was to study in vivo effects of 1,4-dihydropyridine AV-153, known as antimutagen and DNA binder, on the expression of several genes and proteins involved in NO metabolism and DNA repair in the kidneys of rats with a streptozotocin (STZ)-induced model of DM. Transcription intensity was monitored by means of real-time RT-PCR and the expression of proteins by immunohistochemistry. Development of DM significantly induced PARP1 protein express…

0301 basic medicineMalemedicine.medical_specialtyDihydropyridinesDNA RepairNitric Oxide Synthase Type IIIDNA repairPoly (ADP-Ribose) Polymerase-1Gene ExpressionNitric Oxide Synthase Type II030204 cardiovascular system & hematologyToxicologyKidneyNiacinStreptozocinNitric oxideDiabetes Mellitus ExperimentalDiabetic nephropathyHistones03 medical and health scienceschemistry.chemical_compound0302 clinical medicineEnosInternal medicineGene expressionmedicineAnimalsRNA MessengerRats WistarGenePharmacologybiologyReverse Transcriptase Polymerase Chain ReactionKidney metabolismAntimutagenic AgentsGeneral Medicinemedicine.diseaseStreptozotocinbiology.organism_classificationPhosphoproteinsMolecular biologyRats030104 developmental biologyEndocrinologychemistrymedicine.drugBasicclinical pharmacologytoxicology
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Fasting inhibits hepatic stellate cells activation and potentiates anti-cancer activity of Sorafenib in hepatocellular cancer cells

2017

BACKGROUND: Hepatocellular carcinoma (HCC) has a poor outcome. Most HCCs develop in the context of liver fibrosis and cirrhosis caused by chronic inflammation. Short-term fasting approaches enhance the activity of chemotherapy in preclinical cancer models, other than HCC. Multi-tyrosine kinase inhibitor Sorafenib is the mainstay of treatment in HCC. However, its benefit is frequently short-lived. Whether fasting can alleviate liver fibrosis and whether combining fasting with Sorafenib is beneficial remains unknown. METHODS: 24 hour fasting (2% serum, 0.1% glucose)-induced changes on human hepatic stellate cells (HSC) LX-2 proliferation/viability/cell cycle were assessed by MTT and flow cyto…

0301 basic medicineSorafenibLipopolysaccharidesNiacinamidemedicine.medical_specialtyCirrhosisCarcinoma HepatocellularTime FactorsPhysiologyGlucose uptakeClinical BiochemistryAntineoplastic AgentsLiver Cirrhosis Experimental03 medical and health sciencesFibrosisNon-alcoholic Fatty Liver DiseaseInternal medicineSorafenib fastingmedicineHepatic Stellate CellsAnimalsHumansneoplasmsCell Proliferationhepatic stellate cellDose-Response Relationship Drugbusiness.industryMedicine (all)Phenylurea CompoundsLiver NeoplasmsCancerCell BiologyFastingHep G2 Cellshepatocellular carcinomaSorafenibmedicine.diseasedigestive system diseasesGene Expression Regulation NeoplasticMice Inbred C57BL030104 developmental biologyEndocrinologyGlucoseHepatocellular carcinomaHepatic stellate cellCancer researchSteatohepatitisbusinessmedicine.drug
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Comparative validity of the ASSO - Food Frequency Questionnaire for the web-based assessment of food and nutrients intake in adolescents

2015

Background : A new web-based food frequency questionnaire (the ASSO–FFQ) was developed within the ASSO Project funded by the Italian Ministry of Health. Objective : The aim of the present study is to assess the validity of the ASSO–FFQ at food groups, energy, and nutrients level. Design and subjects : The validation study compared the ASSO–FFQ against a weighted food record (WFR) measuring foods, beverages and supplements intake, compiled during the week following the ASSO–FFQ administration. Ninety-two subjects aged 14–17, recruited from secondary schools in Palermo (Italy), completed the ASSO–FFQ and WFR. The intake of 24 food groups, energy, and 52 nutrients were taken as main outcomes. …

0301 basic medicinevalidityDried fruitfood frequency questionnaire030209 endocrinology & metabolismlcsh:TX341-641Food group03 medical and health scienceschemistry.chemical_compound0302 clinical medicineNutrientEnvironmental healthMedicineFood scienceadolescents adults children diet folic acid food composition food frequency questionnaire food intake food processing health claims human nutrition metabolism micronutrients nhanes nutrition nutrition epidemiology obesity overweight physical activity satiety vitaminsLactoseFood Related Nutritionfood frequency questionnaire; intake; nutrient; adolescent; validation; nutrition epidemiologyvalidationAnimal fat030109 nutrition & dieteticsNutrition and Dieteticsbusiness.industrynutrientdigestive oral and skin physiologyPublic Health Environmental and Occupational HealthFood frequency questionnairefood and beveragesFood recordchemistryadolescentOriginal Articlebusinessintakelcsh:Nutrition. Foods and food supplyNiacinFood Science
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Nicotinamide riboside improves muscle mitochondrial biogenesis, satellite cell differentiation, and gut microbiota in a twin study

2023

Nicotinamide adenine dinucleotide (NAD + ) precursor nicotinamide riboside (NR) has emerged as a promising compound to improve obesity-associated mitochondrial dysfunction and metabolic syndrome in mice. However, most short-term clinical trials conducted so far have not reported positive outcomes. Therefore, we aimed to determine whether long-term NR supplementation boosts mitochondrial biogenesis and metabolic health in humans. Twenty body mass index (BMI)–discordant monozygotic twin pairs were supplemented with an escalating dose of NR (250 to 1000 mg/day) for 5 months. NR improved systemic NAD + metabolism, muscle mitochondrial number, myoblast differentiation, and gut microbiota compos…

11832 Microbiology and virologyMultidisciplinaryDna methylationSkeletal-muscleSupplementationmitokondriotNad(+)ylipainoNiacinFaecalibacterium-prausnitziiaineenvaihduntahäiriötHigh-fat dietMetabolismsuolistoLiverAdipose-tissueterveysvaikutuksetlihavuus3111 BiomedicineaineenvaihduntaScience Advances
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Nanoparticles of a polyaspartamide-based brush copolymer for modified release of sorafenib: In vitro and in vivo evaluation.

2017

Abstract In this paper, we describe the preparation of polymeric nanoparticles (NPs) loaded with sorafenib for the treatment of hepatocellular carcinoma (HCC). A synthetic brush copolymer, named PHEA-BIB-ButMA (PBB), was synthesized by Atom Trasnfer Radical Polymerization (ATRP) starting from the α-poly( N -2-hydroxyethyl)- d , l -aspartamide (PHEA) and poly butyl methacrylate (ButMA). Empty and sorafenib loaded PBB NPs were, then, produced by using a dialysis method and showed spherical morphology, colloidal size, negative ζ potential and the ability to allow a sustained sorafenib release in physiological environment. Sorafenib loaded PBB NPs were tested in vitro on HCC cells in order to e…

3003MaleHepatocellular carcinomamedicine.medical_treatmentPharmaceutical Science02 engineering and technologyATRPPharmacology01 natural sciencesDrug Delivery SystemsCopolymerChemistryATRP; Hepatocellular carcinoma; Sorafenib; Tumor targeting; α-Poly(N-2-hydroxyethyl)-DL-aspartamide; 3003Liver NeoplasmsSorafenib021001 nanoscience & nanotechnologyDrug delivery0210 nano-technologymedicine.drugSorafenibNiacinamideCarcinoma HepatocellularCell SurvivalRadical polymerizationIntraperitoneal injectionL-aspartamideMice NudeAntineoplastic AgentsEnhanced permeability and retention effect010402 general chemistryPolymethacrylic AcidsIn vivoCell Line TumormedicineAnimalsHumansneoplasmsProtein Kinase InhibitorsPhenylurea Compoundstechnology industry and agriculturedigestive system diseasesIn vitro0104 chemical sciencesDrug LiberationTumor targetingDelayed-Action PreparationsBiophysicsα-Poly(N-2-hydroxyethyl)-DNanoparticlesα-Poly(N-2-hydroxyethyl)-DL-aspartamidePeptidesJournal of controlled release : official journal of the Controlled Release Society
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Effects of sorbinicate and nicotinic acid on blood viscosity, red cell deformation and platelet function

1982

Summary Nicotinic acid (NA) and a retard derivative, sorbinicate, were investigated for their effects on blood rheology and platelet function, after oral administration, in two groups of patients with lower limb atherosclerosis obliterans — the second group having diabetes also. Red cell deformation and blood plasma viscosity were studied in the nondiabetic group (single dose of NA, 100 mg, and sorbinicate, 400 mg); release of platelet malondialdehyde (MDA) (single dose of NA, 100 mg, and sorbinicate, 800 mg), and the platelet regeneration time (before and after sorbinicate 400 mg × 3/die for 7 days) were studied in the diabetic group. Both drugs induced a significant improvement in red cel…

AdultBlood PlateletsMalemedicine.medical_specialtyErythrocytesTime FactorsBlood viscosityNiacinchemistry.chemical_compoundNEFAOral administrationMalondialdehydeInternal medicineDiabetes mellitusBlood plasmamedicineHumansSorbitolPlateletTriglyceridesPharmacologyRed CellChemistryNicotinic AcidsFibrinogenMiddle AgedBlood Viscositymedicine.diseaseMalondialdehydeCholesterolEndocrinologyBiochemistryFemalePharmacological Research Communications
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Safety and Efficacy of Sorafenib in Patients With Advanced Hepatocellular Carcinoma in Consideration of Concomitant Stage of Liver Cirrhosis

2009

GOALS AND BACKGROUND: The multikinase inhibitor sorafenib provides survival benefit for patients with advanced hepatocellular carcinoma (HCC) and liver cirrhosis (LCI) Child-Pugh A. We report our experiences with sorafenib in advanced HCC, particularly in patients with LCI Child-Pugh B/C, where only limited data are available in regard to safety and efficacy of sorafenib. METHODS: Thirty-four patients with advanced HCC were treated with sorafenib regardless of liver function and prior anticancer therapy. Adverse events (AEs) were graded using Common Toxicity Criteria version 3.0, tumor response was assessed according to Response Evaluation Criteria in Solid Tumors. RESULTS: Fifteen patients…

AdultLiver CirrhosisMaleNiacinamideSorafenibmedicine.medical_specialtyCarcinoma HepatocellularTime FactorsCirrhosisPyridinesAntineoplastic AgentsKaplan-Meier EstimateRisk AssessmentSeverity of Illness IndexGastroenterologyInternal medicinemedicineCarcinomaHumansProspective StudiesProtein Kinase InhibitorsAgedAged 80 and overbusiness.industryPatient SelectionPhenylurea CompoundsBenzenesulfonatesLiver NeoplasmsGastroenterologyCancerMiddle AgedSorafenibmedicine.diseasedigestive system diseasesSurgeryTreatment OutcomeResponse Evaluation Criteria in Solid TumorsHepatocellular carcinomaConcomitantFemaleLiver functionbusinessmedicine.drugJournal of Clinical Gastroenterology
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Lipoprotein hydrophobic core lipids are partially extruded to surface in smaller HDL: "Herniated" HDL, a common feature in diabetes

2016

AbstractRecent studies have shown that pharmacological increases in HDL cholesterol concentrations do not necessarily translate into clinical benefits for patients, raising concerns about its predictive value for cardiovascular events. Here we hypothesize that the size-modulated lipid distribution within HDL particles is compromised in metabolic disorders that have abnormal HDL particle sizes, such as type 2 diabetes mellitus (DM2). By using NMR spectroscopy combined with a biochemical volumetric model we determined the size and spatial lipid distribution of HDL subclasses in a cohort of 26 controls and 29 DM2 patients before and after two drug treatments, one with niacin plus laropiprant a…

AdultMale0301 basic medicineSimvastatinmedicine.medical_specialtyIndolesMagnetic Resonance SpectroscopySurface Properties030204 cardiovascular system & hematologyMicroscopy Atomic ForceNiacinArticle03 medical and health scienceschemistry.chemical_compound0302 clinical medicineFenofibrateInternal medicinemedicineHumansTriglyceridesAgedFluorescent DyesMultidisciplinaryFenofibrateCholesterolCholesterol HDLType 2 Diabetes Mellitusnutritional and metabolic diseasesLipid metabolismMiddle AgedLipid MetabolismLipids030104 developmental biologyEndocrinologyDiabetes Mellitus Type 2chemistryBiochemistryCardiovascular DiseasesSimvastatinFemalelipids (amino acids peptides and proteins)LaropiprantNiacinLipoproteinmedicine.drug
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