Search results for "Mace"

showing 10 items of 4713 documents

Modified nonsink equation for permeability estimation in cell monolayers: comparison with standard methods.

2014

Cell culture permeability experiments are valuable tools in drug development and candidate selection, but the monolayer preparation protocols and the calculations procedures can affect the permeability estimation. Hence, standardization and method suitability demonstration are necessary steps for using permeability data for regulatory and in vivo prediction purposes. Much attention is usually paid to experimental procedure validation and less to the mathematical analysis of the results although the standard equations used imply several assumptions that many times do not hold. The aim of this study was to use a simulation strategy to explore the performance of a new proposed modified nonsink…

Apparent permeabilityAnalytical chemistryPharmaceutical ScienceRegression analysisPermeationStandard methodsModels TheoreticalPermeabilityPermeability (earth sciences)Drug DiscoveryLinear regressionModel simulationMolecular MedicineRegression AnalysisBiological systemMathematicsMolecular pharmaceutics
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Critical review: Grand challenges in assessing the adverse effects of contaminants of emerging concern on aquatic food webs

2019

Much progress has been made in the past few decades in understanding the sources, transport, fate, and biological effects of contaminants of emerging concern (CECs) in aquatic ecosystems. Despite these advancements, significant obstacles still prevent comprehensive assessments of the environmental risks associated with the presence of CECs. Many of these obstacles center around the extrapolation of effects of single chemicals observed in the laboratory or effects found in individual organisms or species in the field to impacts of multiple stressors on aquatic food webs. In the present review, we identify 5 challenges that must be addressed to promote studies of CECs from singular exposure e…

Aquatic OrganismsFood ChainAquatic toxicologyHealth Toxicology and MutagenesisOtras Ciencias Biológicas010501 environmental sciences01 natural sciencesAquatic organismsAquatic toxicologyCiencias Biológicas//purl.org/becyt/ford/1 [https]03 medical and health sciencesAquatic speciesSpecies Specificityaquatic food webEnvironmental ChemistrypharmaceuticaleffectsEcological risk assessment//purl.org/becyt/ford/1.6 [https]Endocrine disruptorsEnvironmental planning030304 developmental biology0105 earth and related environmental sciencesGrand ChallengesTrophic level0303 health sciencesAquatic ecosystemEnvironmental ExposureFood webPersonal care productsAquatic environmentMixturescardiovascular systemPharmaceuticalsEnvironmental sciencecontaminantsCIENCIAS NATURALES Y EXACTASWater Pollutants Chemical
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Insight into the Mechanism of Action of Marine Cytotoxic Thiazinoquinones

2017

The electrochemical response of four natural cytotoxic thiazinoquinones isolated from the Aplidium species was studied using conventional solution-phase and solid-state techniques, based on the voltammetry of immobilized particles methodology. The interaction with O-2 and electrochemically generated reactive oxygen species (ROS) was electrochemically monitored. At the same time, a molecular modeling study including density functional theory (DFT) calculations was performed in order to analyze the conformational and electronic properties of the natural thiazinoquinones, as well as those of their reduced intermediates. The obtained electrochemical and computational results were analyzed and c…

Aquatic OrganismsMolecular modelStereochemistryBioactive natural products; Cytotoxic activity; DFT calculations; Electrochemistry; Reactive radical species; Thiazinoquinones; Animals; Electrochemistry; Quinones; Reactive Oxygen Species; Aquatic Organisms; Urochordata; Drug Discovery3003 Pharmaceutical ScienceThiazinoquinoneDFT calculationPharmaceutical Science02 engineering and technologyDFT calculationsElectrochemistry01 natural sciencesArticleAplidiumbioactive natural products; thiazinoquinones; electrochemistry; DFT calculations; reactive radical species; cytotoxic activityComputational chemistryDrug DiscoverymedicineAnimalsCytotoxic T cellUrochordataBioactive natural productlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Voltammetrycytotoxic activitychemistry.chemical_classificationReactive oxygen speciesbiology010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceQuinonesReactive radical specie021001 nanoscience & nanotechnologybiology.organism_classification0104 chemical scienceslcsh:Biology (General)electrochemistryMechanism of actionchemistryreactive radical speciesbioactive natural productsthiazinoquinonesDensity functional theorymedicine.symptomReactive Oxygen Species0210 nano-technologyMarine Drugs
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Marine Pyrrole Alkaloids

2021

Nitrogen heterocycles are essential parts of the chemical machinery of life and often reveal intriguing structures. They are not only widespread in terrestrial habitats but can also frequently be found as natural products in the marine environment. This review highlights the important class of marine pyrrole alkaloids, well-known for their diverse biological activities. A broad overview of the marine pyrrole alkaloids with a focus on their isolation, biological activities, chemical synthesis, and derivatization covering the decade from 2010 to 2020 is provided. With relevant structural subclasses categorized, this review shall provide a clear and timely synopsis of this area.

Aquatic OrganismsQH301-705.5Ecologymarine natural productsPharmaceutical Sciencepyrrole-aminoimidazole alkaloidsReviewBiologyalkaloidsStructure-Activity Relationshipchemistry.chemical_compoundchemistrypyrrolesDrug DiscoveryAnimalspyrrole-imidazole alkaloidsnitrogen heterocyclesbromopyrrolesBiology (General)Pharmacology Toxicology and Pharmaceutics (miscellaneous)PyrroleMarine Drugs
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Morphogenetic (Mucin Expression) as Well as Potential Anti-Corona Viral Activity of the Marine Secondary Metabolite Polyphosphate on A549 Cells

2020

The mucus layer of the nasopharynx and bronchial epithelium has a barrier function against inhaled pathogens such as the coronavirus SARS-CoV-2. We recently found that inorganic polyphosphate (polyP), a physiological, metabolic energy (ATP)-providing polymer released from blood platelets, blocks the binding of the receptor binding domain (RBD) to the cellular ACE2 receptor in vitro. PolyP is a marine natural product and is abundantly present in marine bacteria. Now, we have approached the in vivo situation by studying the effect of polyP on the human alveolar basal epithelial A549 cells in a mucus-like mucin environment. These cells express mucins as well as the ectoenzymes alkaline phospha…

Aquatic OrganismsSecondary MetabolismVirus AttachmentPharmaceutical ScienceAdenylate kinaseRespiratory MucosaMucin 5ACdigestive systemArticle03 medical and health sciences0302 clinical medicinemucinPolyphosphatesDrug Discoveryotorhinolaryngologic diseasesExtracellularHumansReceptorlcsh:QH301-705.5neoplasmsinnate immunityPharmacology Toxicology and Pharmaceutics (miscellaneous)MUC1030304 developmental biologyA549 cellBiological Products0303 health sciencesBacteriaSARS-CoV-2ChemistryCell growthMucin-1MucinCOVID-19polyphosphaterespiratory systemImmunity Innatedigestive system diseasesSARS-CoV-2 spike proteinADKCell biologyATPlcsh:Biology (General)A549 Cells030220 oncology & carcinogenesishydrogelhuman alveolar cellsMarine Drugs
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Oxygenated Cembrene Diterpenes from Sarcophyton convolutum: Cytotoxic Sarcoconvolutum A–E

2021

The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (1–5) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton convolutum. Compounds were assemblies according to spectroscopic methods including FTIR, 1D- and 2D-NMR as well as HRMS. Metabolite cytotoxicity was tested against lung adenocarcinoma, cervical cancer, and oral-cavity carcinoma (A549, HeLa and HSC-2, respectively). The most cytotoxic compound, (4) was observed to be active against cell lines A549 and HSC-2 with IC50 values of 49.70 and 53.17 μM, respectively.

Aquatic Organismssarcoconvolutum A–EMagnetic Resonance Spectroscopy<i>Sarcophyton convolutum</i>StereochemistryQH301-705.5MetaboliteEthyl acetatePharmaceutical ScienceAntineoplastic AgentsArticleHeLaInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundCell Line TumorDrug DiscoveryIc50 valuesAnimalsCytotoxic T cellBiology (General)CytotoxicityIndian OceanPharmacology Toxicology and Pharmaceutics (miscellaneous)cembrenoidschemistry.chemical_classificationbiologyChemistrySarcophyton<i>Sarcophyton convolutum</i>; sarcoconvolutum A–E; cembrenoids; cytotoxicitySarcophyton convolutumAnthozoabiology.organism_classificationEnzymecytotoxicityDiterpenesDrug Screening Assays AntitumorMarine Drugs
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Voltammetric behavior of berenil.

1993

Abstract Berenil is reduced on mercury drops electrode in buffered aqueous media. The reduction of —N=N— group is controlled by diffusion. Polarographie waves are of analytical usefulness. The hydrogen discharge is favored by the basic centers of the molecule in Co(ll)/ammonia-buffered media.

Aqueous mediumHydrogenAnalytical chemistryPharmaceutical Sciencechemistry.chemical_elementHydrogen-Ion ConcentrationTrypanocidal AgentsMercury (element)chemistryElectrodeElectrochemistryMoleculeVoltammetryDiminazeneElectrodesOxidation-ReductionPolarographyJournal of pharmaceutical sciences
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Concurrent removal of Cr(III), Cu(II), and Pb(II) ions from water by multifunctional TiO2/Alg/FeNPs beads

2019

Abstract The use of multifunctional materials for water remediation is a modern approach where adsorption phenomena and heterogeneous photocatalysis can be applied for the removal of pollutants. Since the ideal remediation system should be able to remove both organic and inorganic pollutants, a crucial aspect to consider is the knowledge of operational parameters affecting the removal process, especially when heavy metal ions are present in concoction as in real systems. Given the proven efficiency of multifunctional TiO2/Alg/FeNPs magnetic beads for the removal of model organic pollutants, this study investigated the possibility to exploit such system also for the removal of mixed heavy me…

Aqueous solution010405 organic chemistryMetal ions in aqueous solutionInorganic chemistryGroundwater remediationMagnetic nanoparticleAdsorbentPharmaceutical Sciencechemistry.chemical_elementManagement Monitoring Policy and Law010402 general chemistry01 natural sciencesPollution0104 chemical sciencesCatalysisMetalChromiumAdsorptionHeavy metalchemistryvisual_artPhotocatalysisvisual_art.visual_art_mediumEnvironmental ChemistryPhotocatalysis
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FLUORINATED DERIVATIVES OF A POLYASPARTAMIDE BEARING POLYETHYLENE GLYCOL CHAINS AS OXYGEN CARRIERS

2008

Abstract In this paper the synthesis and characterization of new fluorinated polymers based on a polyaspartamide bearing polyethylene glycol (PEG) chains, are reported. The starting material was the α,β-poly(N-2-hydroxyethyl)- dl -aspartamide (PHEA), a water soluble and biocompatible polymer, that has been derivatized with both polyethylene glycol (with a molecular weight of 2000 Da) and 5-pentafluorophenyl-3-perfluoroheptyl-1,2,4-oxadiazole. By varying the amount of the fluorinated oxadiazole, three samples have been prepared and characterized by FT-IR, 1H NMR, 19F NMR and UV–VIS spectroscopy. Size exclusion chromatography analysis of these copolymers revealed the occurrence of a self-asso…

Aqueous solutionBiocompatibilityChemistryOrganic ChemistrySize-exclusion chromatographyOxadiazoleFluorine-19 NMRPolyethylene glycolHaemolysisBiochemistryInorganic Chemistrychemistry.chemical_compoundDynamic light scatteringARTIFICIAL OXYGEN CARRIER POLYASPARTAMIDE FLUORINATED POLYMERIC MICELLESSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoPolymer chemistryEnvironmental ChemistryPhysical and Theoretical Chemistry
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New hydrogel matrices based on chemical crosslinked α,β -polyas parthydrazide: Synthesis, characterization and in vivo biocompatibility studies

1996

New swellable micromatrices of α,β-polyasparthydrazide (PAHy) crosslinked with glutaraldehyde were prepared. The effect of crosslinking agent concentration was evaluated. In particular, crosslinking density affected aqueous dynamic swelling and glass-transition temperature of the material. The structure of prepared networks was also studied by scanning electron microscopy and X-ray analysis. Finally, biocompatibility of PAHy derivatives was investigated in vivo by subcutaneous implantation and in oral administration to laboratory animals.

Aqueous solutionBiocompatibilityChemistryScanning electron microscopetechnology industry and agriculturePharmaceutical Sciencemacromolecular substancesDosage formchemistry.chemical_compoundChemical engineeringIn vivoPolymer chemistrySelf-healing hydrogelsmedicineGlutaraldehydeSwellingmedicine.symptomInternational Journal of Pharmaceutics
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