Search results for "Screening"

showing 10 items of 1150 documents

In vivo phage display: identification of organ-specific peptides using deep sequencing and differential profiling across tissues.

2021

Abstract In vivo phage display is widely used for identification of organ- or disease-specific homing peptides. However, the current in vivo phage biopanning approaches fail to assess biodistribution of specific peptide phages across tissues during the screen, thus necessitating laborious and time-consuming post-screening validation studies on individual peptide phages. Here, we adopted bioinformatics tools used for RNA sequencing for analysis of high-throughput sequencing (HTS) data to estimate the representation of individual peptides during biopanning in vivo. The data from in vivo phage screen were analyzed using differential binding—relative representation of each peptide in the target…

Phage displayT7 phageAcademicSubjects/SCI00010virusesPeptideBiopanningComputational biologyDeep sequencing03 medical and health sciencesMiceIn vivoPeptide LibraryGeneticsAnimalsTissue DistributionMolecular Biology030304 developmental biologychemistry.chemical_classification0303 health sciencesMice Inbred BALB Cbiology030302 biochemistry & molecular biologyRNAHigh-Throughput Nucleotide Sequencingbiology.organism_classificationHigh-Throughput Screening AssayschemistryCell Surface Display TechniquesPeptidesHoming (hematopoietic)Nucleic acids research
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Euphosantianane E–G: Three New Premyrsinane Type Diterpenoids from Euphorbia sanctae-catharinae with Contribution to Chemotaxonomy

2019

Euphorbia species were widely used in traditional medicines for the treatment of several diseases. From the aerial parts of Egyptian endemic plant, Euphorbia sanctae-catharinae, three new premyrsinane diterpenoids, namely, euphosantianane E&ndash

Pharmaceutical ScienceAgglomerative hierarchical clustering01 natural sciencesArticlepremyrsinane diterpenoidsAnalytical Chemistrylcsh:QD241-441TerpeneType (biology)lcsh:Organic chemistryEuphorbiaDrug DiscoveryPhysical and Theoretical ChemistryEuphorbiaMolecular StructurebiologyTraditional medicinePlant Extracts010405 organic chemistryOrganic ChemistryeuphorbiaceaeEuphorbiaceaeEuphorbia sanctae-catharinaePlant Components Aerialendemic plantchemotaxonomic significancebiology.organism_classificationAntineoplastic Agents Phytogenic0104 chemical sciences010404 medicinal & biomolecular chemistryChemistry (miscellaneous)Chemotaxonomyeuphosantianane E–G<i>Euphorbia sanctae-catharinae</i>Molecular MedicineEgyptDiterpenesDrug Screening Assays AntitumorMolecules
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Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.

2014

Chemical investigation of the sponge Dactylospongia metachromia afforded five new sesquiterpene aminoquinones (1-5), two new sesquiterpene benzoxazoles (6 and 7), the known analogue 18-hydroxy-5-epi-hyrtiophenol (8), and a known glycerolipid. The structures of all compounds were unambiguously elucidated by one- and two-dimensional NMR and by MS analyses, as well as by comparison with the literature. Compounds 1-5 showed potent cytotoxicity against the mouse lymphoma cell line L5178Y with IC50 values ranging from 1.1 to 3.7 μM. When tested in vitro for their inhibitory potential against 16 different protein kinases, compounds 5, 6, and 8 exhibited the strongest inhibitory activity against AL…

Pharmaceutical ScienceAntineoplastic AgentsMarine BiologySesquiterpeneAnalytical Chemistrychemistry.chemical_compoundInhibitory Concentration 50MiceDrug DiscoveryAnimalsHumansProtein kinase ACytotoxicityIC50Nuclear Magnetic Resonance BiomolecularProtein Kinase InhibitorsPharmacologyBenzoxazolesMolecular StructureKinaseOrganic ChemistryQuinonesIn vitroPoriferaComplementary and alternative medicineBiochemistrychemistryCell cultureMolecular MedicineDrug Screening Assays AntitumorSesquiterpenesProto-oncogene tyrosine-protein kinase SrcJournal of natural products
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Activity of three cytotoxic isoflavonoids from Erythrina excelsa and Erythrina senegalensis (neobavaisoflavone, sigmoidin H and isoneorautenol) towar…

2013

Abstract Introduction Resistance of cancer cells to chemotherapy has become a worldwide concern. Naturally occuring isoflavonoids possess a variety of biological activities including anti-cancer effects. The present study was aimed at investigating the cytotoxicity and the modes of action of three naturally occuring isoflavonoids, neobavaisoflavone ( 1 ), sigmoidin H ( 2 ) and a pterocarpan that is a special type of isoflavonoid, isoneorautenol ( 3 ) against a panel of nine cancer cell lines, including various sensitive and drug-resistant phenotypes. Methods The cytotoxicity of the compounds was determined using a resazurin reduction assay, whereas the caspase-Glo assay was used to detect t…

Pharmaceutical ScienceApoptosisIsoflavonoidDrug DiscoveryHumansCytotoxic T cellBenzopyransCytotoxicityCaspaseBenzofuransErythrinaMembrane Potential MitochondrialPharmacologybiologyCell CyclePterocarpanHCT116 CellsAntineoplastic Agents PhytogenicIsoflavonesMolecular biologyComplementary and alternative medicineBiochemistryDrug Resistance NeoplasmCell cultureApoptosisCaspasesCancer cellbiology.proteinMolecular MedicineDrug Screening Assays AntitumorReactive Oxygen SpeciesPhytomedicine
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Cytotoxic Compounds from the Fruits of Uapaca togoensis towards Multifactorial Drug-Resistant Cancer Cells

2014

Cancer cells may rapidly acquire multidrug resistance, mainly due to the presence of adenosine triphosphate-binding cassette transporters, epidermal growth factor receptor, or mutations in the p53 tumor suppressor gene. This work was designed to assess the cytotoxicity of the methanol crude extracts and compounds from the fruits of Uapaca togoensis, namely, β-amyryl acetate (1), 11-oxo-α-amyryl acetate (2), lupeol (3), pomolic acid (4), futokadsurin B (5), arborinin (6), and 3-O-β-D-glucopyranosyl sitosterol (7) against nine drug sensitive and multidrug-resistant cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of the fruits of U. togoensis and compound…

Pharmaceutical ScienceBiologyLignansAnalytical ChemistryInhibitory Concentration 50chemistry.chemical_compoundCell Line TumorDrug DiscoveryHumansCytotoxic T cellOleanolic AcidCytotoxicityLupeolMembrane Potential MitochondrialPharmacologyMolecular StructurePlant ExtractsAlkaloidOrganic ChemistryEuphorbiaceaeCell cycleAntineoplastic Agents PhytogenicDrug Resistance MultipleTriterpenesComplementary and alternative medicinechemistryBiochemistryDoxorubicinDrug Resistance NeoplasmApoptosisCell cultureCancer cellAcridinesMolecular MedicineDrug Screening Assays AntitumorPentacyclic TriterpenesReactive Oxygen SpeciesPlanta Medica
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Antibacterial Activity and Anticancer Activity of Rosmarinus officinalis L. Essential Oil Compared to That of Its Main Components

2012

In this study, Rosmarinus officinalis L. essential oil and three of its main components 1,8-cineole (27.23%), α-pinene (19.43%) and β-pinene (6.71%) were evaluated for their in vitro antibacterial activities and toxicology properties. R. officinalis L. essential oil possessed similar antibacterial activities to α-pinene, and a little bit better than β-pinene, while 1,8-cineole possessed the lowest antibacterial activities. R. officinalis L. essential oil exhibited the strongest cytotoxicity towards three human cancer cells. Its inhibition concentration 50% (IC50) values on SK-OV-3, HO-8910 and Bel-7402 were 0.025‰, 0.076‰ and 0.13‰ (v/v), respectively. The cytotoxicity of all the test sampl…

Pharmaceutical ScienceRosmarinusAnalytical Chemistrylaw.inventionchemistry.chemical_compoundlawDrug DiscoveryFood scienceCytotoxicityBicyclic Monoterpenesbiologyantibacterial activities18-cineoleAnti-Bacterial AgentsChemistry (miscellaneous)α-pineneOfficinaliscytotoxicityMolecular MedicineAntibacterial activityCell SurvivalMicrobial Sensitivity TestsRosmarinus officinalis L.Articlelcsh:QD241-441Bridged Bicyclo CompoundsInhibitory Concentration 50lcsh:Organic chemistryCell Line TumorBotanyOils Volatile<em>Rosmarinus officinalis </em>L.; 18-cineole; α-pinene; β-pinene; antibacterial activities; cytotoxicityHumansPhysical and Theoretical ChemistryIC50Essential oilEucalyptolBacteriaPlant ExtractsOrganic ChemistryCyclohexanolsbiology.organism_classificationAntineoplastic Agents PhytogenicRosmarinusβ-pineneEucalyptolchemistryMonoterpenesDrug Screening Assays AntitumorHuman cancerMolecules; Volume 17; Issue 3; Pages: 2704-2713
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Sensitive screening of synthetic cannabinoids using liquid chromatography quadrupole time-of-flight mass spectrometry after solid phase extraction.

2021

Analysis of synthetic cannabinoids still poses a challenge for many institutions due to the number of available substances and the constantly changing drug market. Both new and well-known substances keep appearing and disappearing on the market, making it hard to adapt analytical methods in a timely manner. In this study, we developed a qualitative screening approach for synthetic cannabinoids and their metabolites by means of liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS). Samples were measured in data-dependent auto-MS/MS mode and identified by fragment spectra, retention time and accurate mass. Two established solid phase extractions were compared using fo…

Pharmaceutical ScienceUrineMass spectrometry01 natural sciencesMass SpectrometryAnalytical ChemistryDesigner Drugs03 medical and health sciencesForensic Toxicology0302 clinical medicineTandem Mass SpectrometryTriple quadrupole mass spectrometryGeneral screeningSynthetic cannabinoidsmedicineEnvironmental ChemistryHumans030216 legal & forensic medicineSolid phase extractionQuadrupole time of flightSpectroscopyChromatography High Pressure LiquidChromatographyChemistryCannabinoidsHydrolysis010401 analytical chemistryExtraction (chemistry)Solid Phase ExtractionReproducibility of ResultsReference Standards0104 chemical sciencesmedicine.drugDrug testing and analysisREFERENCES
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Poly(alkylidenimine) Dendrimers Functionalized with the Organometallic Moiety [Ru(η5-C5H5)(PPh3)2]+ as Promising Drugs Against Cisplatin-Resistant Ca…

2018

Here and for the first time, we show that the organometallic compound [Ru(&eta

Pharmaceutical Sciencecisplatin01 natural sciencesAnalytical ChemistrydendrimersCoordination ComplexesDrug DiscoveryMoietyplatinummetallitta116Molecular StructureChemistrymolekyylitnanomedicineNanomedicineChemistry (miscellaneous)MCF-7 CellsMolecular MedicineplatinaDendrimersEpithelial-Mesenchymal TransitionCell SurvivalAntineoplastic Agents.myrkyllisyys010402 general chemistryArticlecancer treatmentlcsh:QD241-441Faculdade de Ciências Exatas e da Engenharialcsh:Organic chemistryDendrimerCell Line TumorOrganometallic CompoundsHumansPhysical and Theoretical ChemistryrutheniumPlatinumCell ProliferationTumor microenvironmentCancer och onkologiToxicitynanocarrierssyöpähoidot010405 organic chemistryOrganic ChemistryMesenchymal stem celltoxicityMesenchymal Stem CellsCombinatorial chemistrykantasolutnanolääketiede0104 chemical scienceslääkkeetTumor progressionCell cultureDrug Resistance NeoplasmmetallodrugsCancer and OncologyCancer cellNanocarriersCaco-2 CellsDrug Screening Assays Antitumor<i>cisplatin</i>hMSCs
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Statistical inference in abstracts of 3 influential clinical pharmacology journals analysed using a text‐mining algorithm

2021

Aim To describe the trend in the prevalence of statistical inference in three influential clinical pharmacology journals METHODS: We applied a computer-based algorithm to abstracts of three clinical pharmacology journals published in 1976 to 2016 to identify statistical inference and its subtypes. Furthermore, we manually reviewed a random sample of 300 articles to access algorithm's performance in finding statistical inference in abstracts and as a screening tool for presence and absence of statistical inference in full text. Result The algorithm identified 59% (13,375/22,516 [mid p 95% CI, 59%-60%]) article abstracts with statistical inference. The percentage of abstracts with statistical…

PharmacologyClinical pharmacologybusiness.industryData interpretation030226 pharmacology & pharmacyPredictive valuelaw.invention03 medical and health sciences0302 clinical medicineText mininglawSignificance testingStatistical inferencePharmacology (medical)Screening tool030212 general & internal medicinebusinessAlgorithmMathematicsBritish Journal of Clinical Pharmacology
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Steroidal saponins from Dioscorea preussii.

2014

Abstract Three new steroidal saponins, named diospreussinosides A–C (1–3), along with two known ones (4, 5) were isolated from rhizomes of Dioscorea preussii. Their structures were elucidated mainly by 1D and 2D NMR spectroscopic analysis and mass spectrometry as (25S)-17α,25-dihydroxyspirost-5-en-3β-yl-O-α- l -rhamnopyranosyl-(1 → 4)-α- l -rhamnopyranosyl-(1 → 4)-β- d -glucopyranoside (1), (25S)-17α,25-dihydroxyspirost-5-en-3β-yl-O-α- l -rhamnopyranosyl-(1 → 4)-α- l -rhamnopyranosyl-(1 → 4)-[α- l -rhamnopyranosyl-(1 → 2)]-β- d -glucopyranoside (2), and (24S,25R)-17α,24,25-trihydroxyspirost-5-en-3β-yl-O-α- l -rhamnopyranosyl-(1 → 4)-α- l -rhamnopyranosyl-(1 → 4)-[α- l -rhamnopyranosyl-(1 → …

PharmacologyDioscorea preussiiMolecular StructureStereochemistryChemistryDioscoreaPhytosterolsGeneral MedicineSaponinsMass spectrometryHCT116 CellsRhizomeDihydroxylationCarcinoma CellDrug DiscoveryHumansDrug Screening Assays AntitumorCytotoxicityTwo-dimensional nuclear magnetic resonance spectroscopyHT29 CellsHuman colonFitoterapia
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