Search results for "DISCOVERY"

showing 10 items of 4119 documents

Configurations and conformations of torreyol (δ-cadinol), α-cadinol, T-muurolol and T-cadinol

1981

Abstract The configurations and conformations of torreyol (6; “δ-cadinol”,10α-hydroxy-4-muurolene), α-cadinol (7; 10α-hydroxy-4-cadinene), T-muurolol (8; 10β-hydroxy-4-muurolene), and T-cadinol (9; 10β-hydroxy-4-cadinene) have been determined by an extensive PMR study using lanthanide-induced shifts. Characteristic mass spectrometric fragmentation patterns of muurolols and cadinols are briefly discussed.

Cadinolchemistry.chemical_compoundFragmentation (mass spectrometry)ChemistryStereochemistryOrganic ChemistryDrug DiscoveryT-muurololBiochemistryMass spectrometricTetrahedron
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Conformationally regulated fluorescent sensors. Study of the selectivity in Zn 2+ versus Cd 2+ sensing

2004

Abstract The Zn 2+ and Cd 2+ complexing properties of four ligands containing a 4,4′-substituted biphenyl moiety are described. Ligands 1 and 3 , containing only one 1-aza-18-crown-6 cavity, lead to selective complexation of Cd 2+ versus Zn 2+ . Ligand 4 , with two crown cavities linked to a tetramethylbenzidine unit, is able to form 1:1 complexes with Zn 2+ and Cd 2+ , showing a higher complexing constant with Zn 2+ than with Cd 2+ , probably due to enthalpic factors. Several complementary experiments suggest that the 1:1 complexes formed by ligand 4 involve both crown cavities acting together to give rise to clamp structures. The formation of this type of zinc complex gives rise to red sh…

CadmiumQuenching (fluorescence)ChemistryStereochemistryLigandOrganic Chemistrychemistry.chemical_elementZincBiochemistryFluorescenceCrystallographyDrug DiscoveryNitroMoietySelectivityTetrahedron
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Zur direkten komplexometrischen Calciumbestimmung im Serum mit Calcein als Indicator

1958

Es wird eine einfache Methode zur direkten komplexometrischen Ca-Bestimmung im Serum ohne Fallung und Enteiweisung mit Calcein als Indicator angegeben. Nach ausreichender Verdunnung wird die Titration bei pH>13 ausgefuhrt, wobei Mg quantitativ als Hydroxyd ausfallt. Bei der Standardmethode wird 1 ml Serum mit 0,002 m Komplexon titriert, gegebenenfalls konnen auch 0,5 ml Serum mit 0,0005 m Komplexon titriert werden. Eine Doppelbestimmung nimmt kaum mehr als 2 min in Anspruch.

Calceinchemistry.chemical_compoundChromatographyChemistryDrug DiscoveryMolecular Medicinechemistry.chemical_elementGeneral MedicineCalciumGenetics (clinical)Klinische Wochenschrift
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The Understanding of the Metazoan Skeletal System, Based on the Initial Discoveries with Siliceous and Calcareous Sponges

2017

Initiated by studies on the mechanism of formation of the skeletons of the evolutionary oldest still extant multicellular animals, the sponges (phylum Porifera) have provided new insights into the mechanism of formation of the Ca-phosphate/hydroxyapatite skeleton of vertebrate bone. Studies on the formation of the biomineral skeleton of sponges revealed that both the formation of the inorganic siliceous skeletons (sponges of the class of Hexactinellida and Demospongiae) and of the calcareous skeletons (class of Calcarea) is mediated by enzymes (silicatein: polymerization of biosilica; and carbonic anhydrase: deposition of Ca-carbonate). Detailed studies of the initial mineralization steps i…

Calcium Phosphates0301 basic medicineenzyme-mediated biomineral formationPolymerscarbonic anhydrasePharmaceutical ScienceMineralogyReviewBiologyMineralization (biology)Calcium Carbonateamorphous nanoparticles03 medical and health scienceschemistry.chemical_compoundPolyphosphatesCarbonic anhydraseDrug DiscoveryAnimalsHumansbone-hydroxyapatitebiosilicaPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5SkeletonCarbonic Anhydraseschemistry.chemical_classificationInorganic polymerPhylum PoriferaPolyphosphatePhosphatePoriferaDurapatite030104 developmental biologyEnzymechemistryBiochemistrylcsh:Biology (General)calcium carbonate bio-seedsbiology.proteinCalcareousalkaline phosphataseinorganic polyphosphateMarine Drugs
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Application of integrative cloud point extraction and concentration for the analysis of polyphenols and alkaloids in mulberry leaves

2018

Abstract A simple and efficient method based on cloud point extraction and concentration combined with high performance liquid chromatography was developed for the simultaneous separation and determination of five target compounds (deoxynojirimycin, chlorogenic acid, rutin, isoquercitrin and astragalin) in mulberry leaves samples. Firstly, to obtain a high extraction rate, the ultrasound assisted extraction was developed on acid modified Triton X-114 system. Under the optimal conditions, the total maximum extraction yields of five target compounds reached 20.80 mg/g, which was superior to conventional solvent extraction. After the cloud point extraction and concentration, the HPLC analysis …

Calibration curveLiquid-Liquid ExtractionClinical BiochemistryPharmaceutical Science01 natural sciencesHigh-performance liquid chromatographyAnalytical ChemistrySurface-Active AgentsRutinchemistry.chemical_compoundAlkaloidsChlorogenic acidDrug DiscoveryChromatography High Pressure LiquidSpectroscopyDetection limitCloud pointChromatography010405 organic chemistryChemistry010401 analytical chemistryExtraction (chemistry)Polyphenols0104 chemical sciencesPlant LeavesUltrasonic WavesPolyphenolSolventsMorusJournal of Pharmaceutical and Biomedical Analysis
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Lower rim arylation of calix[n]arenes with extended perfluorinated domains

2006

Abstract Exhaustive O-arylation of p-tert -butylcalix[ n ]arenes 2 ( n  = 4–8) with an excess of 3-pentadecafluoroheptyl-5-pentafluorophenyl-1,2,4-oxadiazole 3 and K 2 CO 3 in refluxing acetonitrile provides an easy entry to a new family of perfluorinated calix[ n ]arenes 1 . The cyclic tetramer furnishes a mixture of cone , partial cone , and 1,2-alternate conformers, while the larger macrocycles afford single products. The structures of all new compounds are substantiated by NMR techniques and MALDI-TOF mass spectral data. Single-crystal X-ray diffraction studies on the pentamer derivative 1b reveal a distorted cone-in conformation of the calixarene cup.

Calixarenes; organofluorine derivativeChemistryPentamerOrganic ChemistryBiochemistryCrystallographychemistry.chemical_compoundTetramerDrug DiscoveryCalixareneCalixarenesSpectral dataAcetonitrileorganofluorine derivativeConformational isomerismDerivative (chemistry)
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Cytotoxicity of medicinal plants of the West-Canadian Gwich׳in Native Americans towards sensitive and multidrug-resistant cancer cells

2015

Abstract Ethnopharmacological relevance Traditional medicine of the Native Americans has a long tradition of medicinal plants, which also influenced modern oncology. For instance, podophyllotoxin the active ingredient of Podophyllum peltatum L. (Berberidaceae) used by Native Americans to treat warts led to the development of etoposide and teniposide. In the present investigation, we studied 10 medicinal plants used by the Gwich׳in First Nation of West-Canada, which have been used against diverse diseases including cancer. Material and methods Sensitive and multidrug-resistant (MDR) tumor cell lines expressing various ATP-binding cassette (ABC) transporters (P-glycoprotein/ ABCB1/MDR1 , MRP1…

CanadaCell SurvivalAntineoplastic AgentsDrug resistancePharmacologyBerberidaceaeCell Line TumorDrug DiscoveryLiliaceaemedicineAraceaeHumansMedicinal plantsEtoposidePharmacologyPlants MedicinalbiologyPlant Extractsbiology.organism_classificationDrug Resistance MultipleArctiumMultiple drug resistancePodophyllotoxinDrug Resistance NeoplasmIndians North AmericanATP-Binding Cassette TransportersArctiumPodophyllum peltatummedicine.drugJournal of Ethnopharmacology
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Biopiracy and the right to self-determination of indigenous peoples.

2018

Abstract Background: Since over thirty years, I work on the unclear legal situation of in which indigenous peoples find themselves today in the beginning mainly in the USA and later also in Canada, Australia and New Zealand. The status of indigenous people and native nations is characterized as a mixture of national and international law. Hypothesis/Purpose: To clarify the status of indigenous people it is necessary to analyze and interpret carefully hundreds of old treaties, international declarations and covenants, national statutes and jurisprudence, especially the old leading decisions of the US-Supreme Court. Such an analysis and interpretation should prove that indigenous people have …

CanadaUnited NationsPharmaceutical ScienceTheftIndigenousStatute03 medical and health sciences0302 clinical medicinePopulation GroupsPolitical scienceDrug DiscoveryComparative lawHumansTreaty030304 developmental biologyPharmacology0303 health sciencesAustraliaDeclaration on the Rights of Indigenous PeoplesBiodiversityInternational lawIndigenous rightsUnited StatesComplementary and alternative medicine030220 oncology & carcinogenesisLawPersonal AutonomyIndians North AmericanMolecular MedicineMinority rightsNew ZealandPhytomedicine : international journal of phytotherapy and phytopharmacology
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Application of patient-derived liver cancer cells for phenotypic characterization and therapeutic target identification.

2018

Primary liver cancer (PLC) ranks among the most lethal solid cancers worldwide due to lack of effective biomarkers for early detection and limited treatment options in advanced stages. Development of primary culture models that closely recapitulate phenotypic and molecular diversities of PLC is urgently needed to improve the patient outcome. Long-term cultures of 7 primary liver cancer cell lines of hepatocellular and cholangiocellular origin were established using defined culture conditions. Morphological and histological characteristics of obtained cell lines and xenograft tumors were analyzed and compared to original tumors. Time course analyses of transcriptomic and genomic changes were…

Cancer ResearchCarcinogenesisDNA Mutational AnalysisPrimary Cell CultureAntineoplastic AgentsDiseaseBiologymedicine.disease_causeTranscriptome03 medical and health sciencesMice0302 clinical medicineCell Line TumormedicineBiomarkers TumorAnimalsHumansPrecision MedicineDrug discoveryGene Expression ProfilingLiver NeoplasmsHigh-Throughput Nucleotide SequencingGenomicsPrecision medicinemedicine.diseasePhenotypeXenograft Model Antitumor AssaysOncologyCell culture030220 oncology & carcinogenesisMutationCancer researchKRASLiver cancerInternational journal of cancer
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Bortezomib: a new pro-apoptotic agent in cancer treatment.

2010

Bortezomib is a proteasome inhibitor. It targets the ubiquitin-proteasome pathway with subsequent inhibition of the degradation of proteins involved in cell cycle regulation and cancer cell survival. The best known molecular mechanism concerns the inhibition of IkappaB breakdown and the related stabilization of NFkappaB, thus preventing its translocation to the nucleus for the activation of downstream pathways. Bortezomib is the only drug in this class which has been approved for clinical use. It has shown an efficient antitumor effect in a phase III clinical trial (APEX) involving relapsed multiple myeloma patients. Response rate, time to progression and overall survival have been improved…

Cancer ResearchCell cycle checkpointSettore MED/06 - Oncologia MedicaAntineoplastic AgentsApoptosisPharmacologyDexamethasoneBortezomibMiceNeoplasmshemic and lymphatic diseasesAntineoplastic Combined Chemotherapy ProtocolsDrug DiscoverymedicineAnimalsHumansDexamethasoneMultiple myelomaPharmacologyproteasome inhibitionClinical Trials as TopicNeovascularization Pathologicbusiness.industryBortezomibCell CycleNF-kappa Bsolid tumorsmedicine.diseaseBoronic AcidsClinical trialBortezomib; solid tumors; proteasome inhibition.OncologyApoptosisPyrazinesCancer cellProteasome inhibitorCancer researchMultiple MyelomabusinessProteasome InhibitorsBortezomib solid tumors proteasome inhibitionmedicine.drug
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