Search results for "FALC"

showing 10 items of 200 documents

Joziknipholones A and B: The First Dimeric Phenylanthraquinones, from the Roots ofBulbine frutescens

2007

From the roots of the African plant Bulbine frutescens (Asphodelaceae), two unprecedented novel dimeric phenylanthraquinones, named joziknipholones A and B, possessing axial and centrochirality, were isolated, together with six known compounds. Structural elucidation of the new metabolites was achieved by spectroscopic and chiroptical methods, by reductive cleavage of the central bond between the monomeric phenylanthraquinone and -anthrone portions with sodium dithionite, and by quantum chemical CD calculations. Based on the recently revised absolute axial configuration of the parent phenylanthraquinones, knipholone and knipholone anthrone, the new dimers were attributed to possess the P-co…

StereochemistryPlasmodium falciparumDrug ResistanceAnthraquinonesStereoisomerismPlant RootsAnthroneAnthraquinoneCatalysisSodium dithioniteAntimalarialsMicechemistry.chemical_compoundCell Line TumorLiliaceaeAnimalsAsphodelaceaeLeukemia L5178Plants MedicinalMolecular StructurebiologySpectrum AnalysisOrganic ChemistryDithioniteChloroquineStereoisomerismPlasmodium falciparumGeneral Chemistrybiology.organism_classificationAntineoplastic Agents PhytogenicRatschemistryQuantum TheoryBulbine frutescensChirality (chemistry)DimerizationAlgorithmsChemistry - A European Journal
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Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.

2015

Five new compounds, 4-O-geranylisoliquiritigenin (1), 12-dihydrousararotenoid B (2), 12-dihydrousararotenoid C (3), 4'-O-geranyl-7-hydroxyflavanone (4), and 4'-O-geranyl-7-hydroxydihydroflavanol (5), along with 12 known natural products (6-17) were isolated from the CH2Cl2/MeOH (1:1) extract of the root bark of Millettia usaramensis ssp. usaramensis by chromatographic separation. The purified metabolites were identified by NMR spectroscopic and mass spectrometric analyses, whereas their absolute configurations were established on the basis of chiroptical data and in some cases also by X-ray crystallography. The crude extract was moderately active (IC50 = 11.63 μg/mL) against the ER-negative…

StereochemistryPlasmodium falciparumMolecular ConformationPharmaceutical Scienceroot barkCrystallography X-Ray01 natural sciencesMillettiaAnalytical ChemistryMillettia usaramensischemistry.chemical_compoundAntimalarialsChalconesDrug DiscoveryPlant BarkHumansta116IC50Nuclear Magnetic Resonance Biomolecularta317metabolitesPharmacologyFlavonoidsChromatographyNatural productbiologyMolecular Structure010405 organic chemistryChemistryPlant ExtractsOrganic ChemistryPlasmodium falciparumChloroquinebiology.organism_classification0104 chemical sciencesMillettia010404 medicinal & biomolecular chemistryChromatographic separationHEK293 CellsComplementary and alternative medicinevisual_artFlavanonesvisual_art.visual_art_mediumPlant BarkMolecular MedicineBarkrotenoidsJournal of natural products
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Naphthalene Derivatives from the Roots of Pentas parvifolia and Pentas bussei

2016

The phytochemical investigation of the CH2Cl2/MeOH (1:1) extract of the roots of Pentas parvifolia led to the isolation of three new naphthalenes, parvinaphthols A (1), B (2), and C (3), two known anthraquinones, and five known naphthalene derivatives. Similar investigation of the roots of Pentas bussei afforded a new polycyclic naphthalene, busseihydroquinone E (4), a new 2,2'-binaphthralenyl-1,1'-dione, busseihydroquinone F (5), and five known naphthalenes. All purified metabolites were characterized by NMR and MS data analyses, whereas the absolute configurations of 3 and 4 were determined by single-crystal X-ray diffraction studies. The E-geometry of compound 5 was supported by DFT-base…

StereochemistryPlasmodium falciparumPharmaceutical SciencePentasAnthraquinonesRubiaceaeCrystallography X-Ray010402 general chemistryPlant Roots01 natural sciencesAnalytical ChemistryAntimalarialsInhibitory Concentration 50chemistry.chemical_compoundBreast cancer cell lineDrug DiscoveryAnthraquinonesIc50 valuesHumansNuclear Magnetic Resonance Biomolecularta116naphthalene derivativesNaphthalenenaphthalenesPharmacologyPentasMolecular Structurebiology010405 organic chemistryOrganic Chemistryta1182Pentas parvifoliabiology.organism_classificationphytochemicals0104 chemical sciencesComplementary and alternative medicinechemistryPhytochemicalMolecular MedicineJournal of Natural Products
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Mbandakamine-Type Naphthylisoquinoline Dimers and Related Alkaloids from the Central African Liana Ancistrocladus ealaensis with Antiparasitic and An…

2018

Four new dimeric naphthylisoquinoline alkaloids, michellamine A5 (2) and mbandakamines C–E (4–6), were isolated from the Congolese plant Ancistrocladus ealaensis, along with the known dimer mbandakamine A (3). They represent constitutionally unsymmetric dimers, each consisting of two 5,8′-coupled naphthylisoquinoline monomers. While the molecular halves of michellamine A5 (2) are linked via C-6′ of both of the naphthalene moieties, i.e., via the least-hindered positions, so that the central biaryl axis is configurationally unstable and not an additional element of chirality, the mbandakamines 3–6 possess three consecutive stereogenic axes. Their monomeric units are linked through an unprece…

Steric effectsAntiparasiticmedicine.drug_classStereochemistryDimerPlasmodium falciparumPharmaceutical ScienceNaphthalenes010402 general chemistry01 natural sciencesAnalytical ChemistryStereocenterchemistry.chemical_compoundAntimalarialsAlkaloidsCell Line TumorDrug DiscoverymedicineHumansAfrica CentralAncistrocladus ealaensisPharmacologyMichellamineAntiparasitic Agents010405 organic chemistryOrganic ChemistryIsoquinolinesAntineoplastic Agents PhytogenicCaryophyllales0104 chemical sciencesMonomerComplementary and alternative medicinechemistryQuinolinesMolecular MedicineChirality (chemistry)Journal of natural products
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Tots som fills de Llorente. El llorentinisme de Carles Salvador

2016

Teodor Llorente i Olivares (1836-1911) és un dels escriptors valencians que més interés va suscitar durant la primera meitat del segle XX. Així, varen ser múltiples els autors que, durant aquell període de temps, li dedicaren poemes i articles d’opinió, anàlisi i/o crítica. Entre aquests autors destaca Carles Salvador i Gimeno (1893-1955), que podem qualificar com un dels més insignes llorentinistes de tots els temps. Així, la seua vinculació envers el patriarca de la Renaixença valenciana va des de l’admiració lírica i l’estudi pregon i detallat de diversos aspectes bibliogràfics, fins a la preparació d’una antologia poètica que veié la llum, de manera pòstuma, en 1958. Així mateix, ben si…

Teodor LlorenteCarles SalvadorTeodor Llorente Falcóvalencianisme culturalsegles XIX i XX
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Simplifying instructional texts in French and German Easy Language – Comparaison of Easy Language rules and analysis of their limits

2022

Contexte: Dans le contexte du développement d’une société plus inclusive, l’étude de la simplification du langage constitue un réel enjeu, aussi en termes scientifiques. Cette simplification a en effet pour ambition de profiter à différents types de publics, allant de l’éducation des élèves à l’accès à l’information pour des personnes présentant un handicap, des personnes vieillissantes, mais également pour des personnes allophones arrivant dans un pays donné. A l’échelle européenne, l'association Inclusion Europe, à travers son projet Easy-to-Read, a ainsi établi une liste de principes visant à standardiser la rédaction dans des variantes adaptées des langues nationales. Question de recher…

Text LinguisticsEasy languagesFALCAccessibility[SHS.LANGUE] Humanities and Social Sciences/LinguisticsCognitive Linguistics
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In Vitro and In Vivo Antimalarial Activity Assays of Seeds from Balanites aegyptiaca: Compounds of the Extract Show Growth Inhibition and Activity ag…

2011

Balanites aegyptiaca(Balanitaceae) is a widely grown desert plant with multiuse potential. In the present paper, a crude extract fromB. aegyptiacaseeds equivalent to a ratio of 1 : 2000 seeds to the extract was screened for antiplasmodial activity. The determined IC50value for the chloroquine-susceptiblePlasmodium falciparumNF54 strain was 68.26 . Analysis of the extract by gas chromatography-mass spectrometry detected 6-phenyl-2(H)-1,2,4-triazin-5-one oxime, an inhibitor of the parasitic M18 Aspartyl Aminopeptidase as one of the compounds which is responsible for thein vitroantiplasmodial activity. The crude plant extract had a of 2.35  and showed a dose-dependent response. After depletion…

Traditional medicineArticle SubjectPlasmodium falciparumParasitemiaBiologymedicine.diseasebiology.organism_classificationAminopeptidaseIn vitrolcsh:Infectious and parasitic diseaseschemistry.chemical_compoundInfectious DiseaseschemistryIn vivoddc:570BotanymedicineParasitologylcsh:RC109-216Growth inhibitionAspartyl aminopeptidaseBalanites aegyptiacaResearch ArticleJournal of Parasitology Research
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Antileukemic ancistrobenomine B and related 5,1′-coupled naphthylisoquinoline alkaloids from the Chinese liana Ancistrocladus tectorius

2017

A striking feature of the metabolite pattern of the Southeast Asian liana Ancistrocladus tectorius (Ancistrocladaceae) is the predominance of 5,1′-coupled naphthylisoquinoline alkaloids. About 20 alkaloids of this coupling type have so far been discovered in this plant species. Here, we report on the isolation of four new 5,1′-linked naphthylisoquinolines from the twigs and stems of A. tectorius. Two of them, the ancistrobenomines B (5) and C (6), belong to the very rare group of alkaloids with a fully dehydrogenated isoquinoline portion. Likewise unusual for naphthylisoquinoline alkaloids is the presence of a hydroxymethylene group at C-3. Within the large class of meanwhile ca. 180 such n…

Trypanosoma brucei rhodesienseCircular dichroismStereochemistryMetabolitePlasmodium falciparumNaphthalenesSoutheast asian01 natural sciencesAntimalarialsMagnoliopsidachemistry.chemical_compoundAlkaloidsCell Line TumorDrug DiscoveryHumansIsoquinolinePharmacologyMolecular StructurePlant Stemsbiology010405 organic chemistryTrypanosoma brucei rhodesiensePlasmodium falciparumGeneral MedicineIsoquinolinesbiology.organism_classificationAntineoplastic Agents Phytogenic0104 chemical sciences010404 medicinal & biomolecular chemistrychemistryAncistrocladaceaeTwo-dimensional nuclear magnetic resonance spectroscopyFitoterapia
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Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

2019

This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...

Trypanosoma brucei rhodesienseStrong inhibitorKetoneStereochemistryProtein ConformationPeptide01 natural sciences03 medical and health sciencesStructure-Activity RelationshipSUBSTRATEDrug DiscoverymedicineHumansAfrican trypanosomiasisSulfonesBIOLOGICAL EVALUATION030304 developmental biologyWARHEADchemistry.chemical_classification0303 health sciencesMolecular StructureChemistryDERIVATIVESTrypanosoma brucei rhodesienseCYSTEINE PROTEASES RHODESAIN BIOLOGICAL EVALUATION CATHEPSIN-L INHIBITORS BRUCEI PEPTIDOMIMETICS FALCIPAIN-2 DERIVATIVES SUBSTRATE WARHEADBRUCEImedicine.diseaseFALCIPAIN-2Trypanocidal Agents0104 chemical sciences010404 medicinal & biomolecular chemistryCysteine EndopeptidasesTrypanosomiasis AfricanCYSTEINE PROTEASES RHODESAINCATHEPSIN-LMolecular MedicineINHIBITORSPEPTIDOMIMETICS
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Biology of gama delta T Cells in Tuberculosis and Malaria

2002

Tuberculosis and malaria remain the leading causes of mortality among human infectious diseases in the world. It is estimated that 3 to 5 million people die from tuberculosis and malaria each year. Although it is traditionally believed that CD4 and CD8 alphabeta T lymphocytes are mandatory for protective immune responses against Mycobacterium tuberculosis and Plasmodium falciparum (the ethiologic agents of tuberculosis and the most severe form of malaria, respectively), there is still incomplete understanding of the mechanisms of immune protection and of the causes of its failure in the affected patients. Several studies in humans and animal models have suggested that Vgamma9/Vdelta2 T cell…

TuberculosisT cellPlasmodium falciparumBiochemistryMycobacterium tuberculosisMiceImmune systemAntigenT-Lymphocyte Subsetsparasitic diseasesmedicineAnimalsHumansTuberculosisMalaria FalciparumMolecular BiologybiologyReceptors Antigen T-Cell gamma-deltaPlasmodium falciparumMycobacterium tuberculosisGeneral Medicinemedicine.diseasebiology.organism_classificationVirologyDisease Models Animalmedicine.anatomical_structureImmunologyMolecular MedicineCD8MalariaCurrent Molecular Medicine
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