Search results for "EROI"

showing 10 items of 1497 documents

COX-1/COX-2 inhibitors based on the methanone moiety

2002

This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl)sulphonamides and -amides were studied in detail, and to consolidate the data evaluated the corresponding 3- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.

Blood PlateletsStereochemistrymedicine.drug_classDrug Evaluation PreclinicalCarboxamideIsozymeChemical synthesisStructure-Activity RelationshipOxazinesDrug DiscoverymedicineAnimalsPotencyMoietyCyclooxygenase InhibitorsPharmacologychemistry.chemical_classificationCyclooxygenase 2 InhibitorsMolecular StructurebiologyChemistryAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryGeneral MedicineIn vitroIsoenzymesEnzymeCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesEnzyme inhibitorCyclooxygenase 1biology.proteinEuropean Journal of Medicinal Chemistry
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Griffonianone D, an isoflavone with anti-inflammatory activity from the root bark of Millettia griffoniana.

2003

A new isoflavone, griffonianone D (1), and the previously known compounds durmillone and odorantin were isolated from a chloroform extract of the root bark of Millettia griffoniana. The structure of 1 was established as (7E)-(6",7"-dihydroxy-3",7"-dimethyloct-2"-enyl)oxy-4'-methoxyisoflavone on the basis of its spectral data. The chloroform extract of the root bark of M. griffoniana and compound 1 showed anti-inflammatory effects in different experimental models of inflammation.

Blood Plateletsmedicine.drug_classFlavonoidPharmaceutical SciencePlant RootsAnti-inflammatoryMillettiaPhospholipases AAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryBotanymedicineLeukocytesAnimalsEdemaHumansCameroonSpectral dataNuclear Magnetic Resonance BiomolecularPharmacologychemistry.chemical_classificationFlavonoidsChloroformPlants MedicinalTraditional medicinebiologyMolecular StructureOrganic ChemistryAnti-Inflammatory Agents Non-SteroidalGriffonianone DEarStereoisomerismbiology.organism_classificationIsoflavonesMillettiaRatsPhospholipases AComplementary and alternative medicinechemistryProstaglandin-Endoperoxide Synthasesvisual_artvisual_art.visual_art_mediumPlant BarkMolecular MedicineBarkJournal of natural products
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Blood pressure control in treated hypertensive patients in daily practice of Latvian family physicians.

2011

Background and Objective. The aim of this study was to evaluate blood pressure (BP) control level in treated hypertensive patients in Latvia and to compare their characteristics according to the adequacy of BP control. Materials and Methods. Family physicians collected information on demographic and clinical characteristics, and current antihypertensive treatment of 455 18–80-year-old patients with essential arterial hypertension treated for 1 or more years. Target BP was defined as values of <140/90 mm Hg for patients with low or moderate cardiovascular risk and <135/85–125/75 mm Hg for patients with high or very high risk. BP was measured in the office setting after a 5-minute rest …

Blood pressure controlAdultMalemedicine.medical_specialtyAdolescentBlood Pressurearterial hypertension; blood pressure control; antihypertensive drugsSittingYoung AdultRisk groupsInternal medicineDaily practicemedicineAneroid sphygmomanometerHumansIn patientAntihypertensive AgentsAgedAged 80 and overControl levelbusiness.industryPhysicians FamilyBlood Pressure DeterminationGeneral MedicineMiddle AgedLatviaBlood pressureTreatment OutcomeHypertensionPhysical therapyFemalebusinessMedicina (Kaunas, Lithuania)
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Human Spheroids from Adipose-Derived Stem Cells Induce Calvarial Bone Production in a Xenogeneic Rabbit Model

2020

ABSTRACT: Calvarial defects can result from several causes. Tissue engineering hold the potential to restore native form and protective function. We have recently shown that stemness and differentiation ability of spheroids from adipose-derived stem cells (S-ASCs) promotes osteoblasts growth within Integra in a small vertebral lesion. In our study, we aimed to test osteogenic potential of S-ASCs in aiding regeneration of a calvarial defect. Groups containing Integra showed increased bone regeneration at the calvarial defect-Integra interface compared with the control group. In particular, S-ASC-derived osteoblasts group showed a superior calvarial remodeling than undifferentiated S-ASCs gro…

Bone RegenerationCellular differentiationAdipose tissueBone healing030230 surgerySettore MED/08 - Anatomia Patologica03 medical and health sciences0302 clinical medicineTissue engineeringOsteogenesisAdipocytesAnimalsHumansMedicinespheroids.Bone regenerationCells Culturedadipose-derived stem cellbusiness.industryOssificationStem CellsRegeneration (biology)SkullCell DifferentiationCell biologyAdipose Tissue030220 oncology & carcinogenesisSurgeryRabbitsmedicine.symptomStem cellbusiness
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Injectable xyloglucan hydrogels incorporating spheroids of adipose stem cells for bone and cartilage regeneration

2021

Abstract Cartilage or bone regeneration approaches based on the direct injection of mesenchymal stem cells (MSCs) at the lesion site encounter several challenges, related to uncontrolled cell spreading and differentiation, reduced cell viability and poor engrafting. This work presents a simple and versatile strategy based on the synergic combination of in-situ forming hydrogels and spheroids of adipose stem cells (SASCs) with great potential for minimally invasive regenerative interventions aimed to threat bone and cartilage defects. Aqueous dispersions of partially degalactosylated xyloglucan (dXG) are mixed with SASCs derived from liposuction and either a chondroinductive or an osteoinduc…

Bone RegenerationMaterials scienceChondroblastic differentiationBioengineeringInjectable hydrogelsBiomaterialschemistry.chemical_compoundOsteogenic differentiationmedicineViability assayXyloglucanBone regenerationGlucansStem CellsCartilageRegeneration (biology)Mesenchymal stem cellCell DifferentiationHydrogelsChondroblastic differentiation; Injectable hydrogels; Osteogenic differentiation; Spheroids of adipose stem cells; XyloglucanCell biologyXyloglucanCartilagemedicine.anatomical_structurechemistryMechanics of MaterialsSelf-healing hydrogelsSpheroids of adipose stem cellsXylansStem cellMaterials Science and Engineering: C
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IL-17A induces chromatin remodeling promoting IL-8 release in bronchial epithelial cells: Effect of Tiotropium

2016

Abstract Aims IL-17A plays a key role in the persistence of airway inflammation, oxidative stress, and reduction of steroid-sensitivity in COPD. We studied the effect of IL-17A on chromatin remodeling and IL-8 production. Main methods We measured the levels of IL-8 and IL-17A in induced sputum supernatants (ISS) from healthy controls (HCs), healthy smokers (HSs), and COPD patients by enzyme-linked immunosorbent assay (ELISA). A human bronchial epithelial cell line (16HBE) was stimulated with ISS from HCs, HSs, or COPD subjects. IL-8 was evaluated in 16HBE by Western blot and real-time polymerase chain reaction (PCR). Histone deacetylase 2 (HDAC2), acetyl histone H3 (Ac-His H3) (k9) and inhi…

Bronchial epithelial cell0301 basic medicineHistone Deacetylase 2BronchiBiologyGeneral Biochemistry Genetics and Molecular BiologyChromatin remodelingProinflammatory cytokineHistonesChromatin remodelingAndrologyPulmonary Disease Chronic Obstructive03 medical and health sciencesHistone H3Western blotIL-17AmedicineHumansInterleukin 8Tiotropium BromideGeneral Pharmacology Toxicology and PharmaceuticsCells CulturedCOPDBiochemistry Genetics and Molecular Biology (all)IL-8medicine.diagnostic_testHistone deacetylase 2Chronic obstructive pulmonary diseaseAnti-Inflammatory Agents Non-SteroidalInterleukin-17Interleukin-8SmokingSputumEpithelial CellsGeneral MedicineChromatin Assembly and Disassemblymedicine.diseaserespiratory tract diseases030104 developmental biologyPharmacology Toxicology and Pharmaceutics (all)ImmunologyInterleukin 17human activitiesLife Sciences
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Differences in the efficacy and safety among inhaled corticosteroids (ICS)/long-acting beta2-agonists (LABA) combinations in the treatment of chronic…

2015

Inhaled corticosteroids (ICS) are frequently recommended for the treatment of asthma and COPD, often in combination with long-acting beta2-agonists (LABA), depending on the severity of the disease and/or on the specific phenotype. Several ICS/LABA combinations are currently available that differ in their pharmacokinetic characteristics and dose of both components. Thus, this review assesses differences in the efficacy and the safety profiles of the ICS components in the two more frequently used ICS/LABA combinations (budesonide/formoterol and fluticasone/salmeterol) for the management of COPD. Whereas the basic mechanism of action is similar for all ICS (binding with the intracellular gluco…

BudesonideAdrenergic beta-2 Receptor AgonistPulmonary and Respiratory MedicineChronic Obstructivemedicine.medical_specialtymedicine.drug_classPopulationSettore MED/10 - Malattie Dell'Apparato RespiratorioBudesonide; COPD; Fluticasone; Pneumonia; Administration Inhalation; Adrenergic beta-2 Receptor Agonists; Drug Combinations; Glucocorticoids; Humans; Pulmonary Disease Chronic Obstructive; Quality of Life; Pulmonary and Respiratory Medicine; Biochemistry (medical); Pharmacology (medical)Pulmonary DiseasePulmonary Disease Chronic ObstructiveGlucocorticoidInternal medicineDrug CombinationAdministration InhalationmedicineBudesonide; COPD; Fluticasone; Pneumonia; Pulmonary and Respiratory Medicine; Pharmacology (medical); Biochemistry (medical)HumansCOPDPharmacology (medical)educationBudesonideAdrenergic beta-2 Receptor AgonistsGlucocorticoidsAsthmaFluticasoneeducation.field_of_studyCOPDbusiness.industryBiochemistry (medical)Pneumoniamedicine.diseaserespiratory tract diseasesDrug CombinationsInhalationAnesthesiaAdministrationQuality of LifeCorticosteroidFluticasoneFormoterolSalmeterolbusinesshormones hormone substitutes and hormone antagonistsmedicine.drugHuman
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Budesonide in previously untreated autoimmune hepatitis

2005

Background: Autoimmune hepatitis (AIH) is a chronic liver disease that is effectively treated with immunosuppressive therapy. Predniso(lo)ne, often in combination with azathioprine, is the basic therapeutic option to induce remission. However, this regimen can cause numerous side effects. The aim of the present study was to evaluate budesonide as a treatment option in the induction of remission in patients with previously untreated AIH. Methods: Between October 1998 and August 1999, 12 patients were treated with 3 mg budesonide thrice daily for 3 months in this open one-arm multicenter phase IIa study. Primary end point was induction of remission indicated by a drop of aspartate aminotransf…

BudesonideAdultMalemedicine.medical_specialtybudesonideAzathioprinePREDNISOLONEAutoimmune hepatitisChronic liver diseaseGastroenterologyInflammatory bowel diseaseLiver diseaseLIVER-DISEASEInternal medicinemedicineHumansAgedHepatologyautoimmune hepatitisbusiness.industryCHRONIC ACTIVE HEPATITISCORTICOSTEROID-THERAPYAlanine TransaminaseMiddle Agedmedicine.diseaseCROHNS-DISEASERegimenHepatitis AutoimmuneImmunologyPrednisoloneFemaleTRIALORAL BUDESONIDEbusinesstreatment optionsmedicine.drugINFLAMMATORY-BOWEL-DISEASELiver international
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Regular versus as-needed budesonide and formoterol combination treatment for moderate asthma: A non-inferiority, randomised, double-blind clinical tr…

2015

Summary Background Treatment guidelines for patients with moderate persistent asthma recommend regular therapy with a combination of an inhaled corticosteroid and a longacting β 2 agonist plus as-needed rapid-acting bronchodilators. We investigated whether symptom-driven budesonide and formoterol combination therapy administered as needed would be as effective as regular treatment with this combination plus as-needed symptom-driven terbutaline for patients with moderate asthma. Methods In this non-inferiority randomised clinical trial, we recruited adult patients (18–65 years of age) with stable moderate persistent asthma, according to 2006 Global Initiative for Asthma guidelines. Patients …

BudesonideMalePediatricsKaplan-Meier Estimatelaw.inventionRandomized controlled triallawMedicineOutpatient clinicBudesonide Formoterol Fumarate Drug CombinationAnti-Asthmatic AgentsTreatment Failureeducation.field_of_studyasthma; clinical trialMedicine (all)clinical trialMiddle AgedCombined Modality TherapyBronchodilator AgentsFemalemedicine.drugHumanAdultPulmonary and Respiratory Medicinemedicine.medical_specialtyAdolescentTerbutalinePopulationSettore MED/10 - Malattie Dell'Apparato RespiratorioPlaceboDrug Administration ScheduleNOYoung AdultDouble-Blind MethodAdministration InhalationTerbutalineinhaled corticosteroids LABA asthma clinical trialHumansAnti-Asthmatic AgenteducationBronchodilator AgentPulmonary and Respiratory Medicine; Medicine (all)AsthmaAgedPulmonary and Respiratory Medicine RCT asthmabusiness.industryComputerSystemsOrganization_COMPUTER-COMMUNICATIONNETWORKSmedicine.diseaseAsthmarespiratory tract diseasesFormoterolbusiness
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Low-dose budesonide treatment for prevention of postoperative recurrence of Crohnʼs disease

1999

Summary and ConclusionAlthough the effect of budesonide was altogether positive in almost all variables studied in this train (e.g. endoscopic and histopathological score, time-to-failure, CDAI, patients' global judgement and rate of side effects), this increase in efficacy was small and the power f

Budesonidemedicine.medical_specialtyCrohn's diseaseHepatologymedicine.diagnostic_testbusiness.industrymedicine.drug_classGastroenterologyPlacebo-controlled studyColonoscopymedicine.diseaseGastroenterologylaw.inventionSurgeryClinical trialRandomized controlled triallawInternal medicineChemoprophylaxismedicineCorticosteroidbusinessmedicine.drugEuropean Journal of Gastroenterology & Hepatology
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