Search results for "Pori"

showing 10 items of 761 documents

Synthesis of Pyrrolidin-2-ones and of Staurosporine Aglycon (K-252c) by Intermolecular Michael Reaction

1999

Indolo[2,3-a]pyrrolo[3,4-c]carbazoles were isolated from nature, e.g., from low plants, especially fungi, as structurally rare natural substances. Responsible for naming and also the most important representative of this type is staurosporine (1), isolated from Streptomyces staurosporeus, and its aglycon (2), also known as staurosporinone or K-252c. 3,4-Disubstituted pyrrolidin-2-ones, a group of compounds with many interesting biological properties are related to staurosporinone. The most important property is the inhibition of protein kinase C (PKC), so that this antiproliferative agent can interfere with the cell cycle. The synthetic strategy, developed by us, allows the synthesis of pyr…

StaurosporinoneStereochemistryOrganic ChemistryIntermolecular forceEnantioselective synthesisCombinatorial chemistrychemistry.chemical_compoundchemistryNitroLactammedicineMichael reactionStaurosporineProtein kinase Cmedicine.drugThe Journal of Organic Chemistry
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Bioactive pyrrole alkaloids isolated from the Red Sea : marine sponge Stylissa carteri

2017

Abstract Fifteen pyrrole alkaloids were isolated from the Red Sea marine sponge Stylissa carteri and investigated for their biological activities. Four of them were dibrominated [(+) dibromophakelline, Z-3-bromohymenialdisine, (±) ageliferin and 3,4-dibromo-1H-pyrrole-2-carbamide], nine compounds were monobrominated [(−) clathramide C, agelongine, (+) manzacidin A, (−) 3-bromomanzacidin D, Z-spongiacidin D, Z-hymenialdisine, 2-debromostevensine, 2-bromoaldisine and 4-bromo-1H-pyrrole-2-carbamide)] and finally, two compounds were non-brominated derivatives viz., E-debromohymenialdisine and aldisine. The structure elucidations of isolated compounds were based on 1D & 2D NMR spectroscopic …

StereochemistryCell Survival01 natural sciencesGeneral Biochemistry Genetics and Molecular BiologyCell LineRSchemistry.chemical_compoundAlkaloidsAnimalsHumansPyrrolesProtein kinase ACytotoxicityIndian OceanAgeliferinPyrrolebiologyMolecular Structure010405 organic chemistryKinasebiology.organism_classificationHCT116 Cells0104 chemical sciencesPorifera010404 medicinal & biomolecular chemistrySpongechemistryStylissa carteriDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopy
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Putative identification of an amphipathic alpha-helical sequence in hemolysin of Escherichia coli (HlyA) involved in transmembrane pore formation.

2008

Abstract Escherichia coli hemolysin is a pore-forming protein belonging to the RTX toxin family. Cysteine scanning mutagenesis was performed to characterize the putative pore-forming domain of the molecule. A single cysteine residue was introduced at 48 positions within the sequence spanning residues 170–400 and labeled with the polarity-sensitive dye badan. Spectrofluorimetric analyses indicated that several amino acids in this domain are inserted into the lipid bilayer during pore formation. An amphipathic α-helix spanning residues 272–298 was identified that may line the aqueous pore. The importance of this sequence was highlighted by the introduction of two prolines at positions 284 and…

StereochemistryClinical BiochemistryAmino Acid MotifsPorinsmedicine.disease_causeBiochemistryProtein Structure SecondaryHemolysin ProteinsCell Line TumormedicineAnimalsHumansLipid bilayerMolecular BiologyEscherichia colichemistry.chemical_classificationEscherichia coli ProteinsRTX toxinMutagenesisErythrocyte MembraneHemolysinTransmembrane proteinAmino acidchemistryMutant ProteinsRabbitsCysteineBiological chemistry
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Trimeric Hemibastadin Congener from the Marine Sponge Ianthella basta

2012

The first naturally occurring trimeric hemibastadin congener, sesquibastadin 1 (1), and the previously reported bastadins 3, 6, 7, 11, and 16 (2-6) were isolated from the marine sponge Ianthella basta, collected in Indonesia. The structure of 1 was elucidated on the basis of 1D and 2D NMR measurements and by HRMS. Among all the isolated compounds, the linear sesquibastadin 1 (1) and bastadin 3 (2) showed the strongest inhibition rates for at least 22 protein kinases (IC(50) = 0.1-6.5 μM), while the macrocyclic bastadins (3-6) demonstrated a strong cytotoxic potential against the murine lymphoma cell line L5178Y (IC(50) = 1.5-5.3 μM).

StereochemistryPharmaceutical ScienceMarine BiologySesquibastadinAnalytical ChemistryMiceIanthella bastaDrug DiscoveryHalogenated Diphenyl EthersAnimalsNuclear Magnetic Resonance BiomolecularProtein Kinase InhibitorsPharmacologyMolecular StructurebiologyMurine lymphomaOrganic Chemistrybiology.organism_classificationPoriferaSpongeCongenerComplementary and alternative medicineIndonesiaMolecular MedicineDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopyJournal of Natural Products
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Cytotoxic Isomalabaricane Triterpenes from the Marine Sponge Rhabdastrella globostellata

2006

Fourteen isomalabaricane triterpenes were isolated from the marine sponge Rhabdastrella globostellata. In addition to the known compounds globostellatic acids A (1) and D (4) and stelliferin riboside (13), 11 of the compounds were new natural products, which included globostelletin (3), eight new globostellatic acid congeners, F to M (2, 5-11), and two new stelliferin ribosides (12 and 14). The isolated compounds were tested against three different cancer cell lines, L5178Y (mouse lymphoma), HeLa (human cervix carcinoma), and PC-12 (rat pheochromocytoma). The isomalabaricane derivatives were found to be selectively active toward the mouse lymphoma cell line L5178Y. The structures were deter…

StereochemistryRhabdastrella globostellataPharmaceutical ScienceAntineoplastic AgentsPharmacognosyPC12 CellsAnalytical ChemistryHeLaTerpeneMiceTriterpeneDrug DiscoveryTumor Cells CulturedAnimalsHumansPharmacologychemistry.chemical_classificationMolecular StructurebiologyOrganic ChemistryBiological activitybiology.organism_classificationTriterpenesTerpenoidPoriferaRatsSpongeComplementary and alternative medicinechemistryIndonesiaMolecular MedicineDrug Screening Assays AntitumorHeLa CellsJournal of Natural Products
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Microparticles derived from marine sponge collagen (SCMPs): preparation, characterization and suitability for dermal delivery of all-trans retinol.

2002

Abstract Collagen microparticles were prepared using marine sponge collagen. For this purpose a previous method by Rossler et al. (J. Microencapsul. 12 (1995) 49) of emulsification and cross-linking of native calf collagen was modified. The modified method for sponge collagen microparticles (SCMPs) achieved a yield of 10%. Scanning electromicroscopic photographs showed spherical particles with a diameter of 120–300 nm and photon correlation spectroscopic measurements indicated particle size range from 126 (±2.9) to 2179 (±342) nm. This broad size distribution was caused by some agglomerates that could not be destroyed by ultrasonication. The surface charge was measured as a function of pH. …

StereochemistrySonicationDrug CompoundingSkin AbsorptionPharmaceutical ScienceIn Vitro TechniquesAdministration CutaneousDosage formMiceDrug StabilityAnimalsAll trans retinolMicroparticleParticle SizeVitamin ADrug CarriersMice HairlessChromatographyChemistryGeneral MedicinePenetration (firestop)PoriferaSelf-healing hydrogelsFemaleParticle sizeCollagenDrug carrierBiotechnologyEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
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Methomyl analogues with increased biological activity towards F7T maize mitochondria

1987

Abstract Methomyl analogues were synthesized by substituting alkyl moieties (C 2 -C 21 ) in the place of the carbamic methyl. They were assayed on mitochondria isolated from male sterile (F 7 T) and male fertile (F 7 N) maize. They had no action on F 7 N mitochondria. The heptadecyl (C 17 ) and heneicosanyl (C 21 ) derivatives had no conspicuous effect on F 7 T mitochondria. By contrast, the ethyl, propyl, butyl, nonyl, tridecyl (C 13 ) and pentadecyl (C 15 ) derivatives had the same type of activity as Methomyl on F 7 T mitochondria, namely stimulation of NADH oxidation and inhibition of malate oxidation. Moreover, the concentration at which they were maximally effective decreased from 10 …

StereochemistryStimulationMethomylPlant ScienceHorticultureBiologyMitochondrionmedicine.disease_causeBiochemistry03 medical and health scienceschemistry.chemical_compoundmedicineHelminthosporium maydisMolecular Biology[SDV.BV.PEP] Life Sciences [q-bio]/Vegetal Biology/Phytopathology and phytopharmacyAlkylComputingMilieux_MISCELLANEOUS030304 developmental biologychemistry.chemical_classification0303 health sciencesToxinBiological activity04 agricultural and veterinary sciencesGeneral MedicineFungi imperfectibiology.organism_classification[SDV.BV.PEP]Life Sciences [q-bio]/Vegetal Biology/Phytopathology and phytopharmacyGRAMINEchemistryBiochemistry040103 agronomy & agriculture0401 agriculture forestry and fisheries
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Short-term response to waterlogging in Quercus petraea and Quercus robur: A study of the root hydraulic responses and the transcriptional pattern of …

2015

International audience; We characterized the short-term response to waterlogging in Quercus petraea (Matt.) Liebl. and Quercus robur L. as the initial response towards their known long-term differences in tolerance to waterlogging. One-month old seedlings were subjected to hypoxic stress and leaf gas exchange, shoot water potential (Psi(s)) and root hydraulic conductivity (Lp(r)) were measured. In parallel, the expression of nine aquaporins (AQPs) along the primary root was analysed by quantitative RT-PCR. Results showed a similar reduction in net assimilation (A) and stomatal conductance (g(s)) for the two species. Notably, the response of Lpr differed temporally between the two species. Q…

Stomatal conductanceTime FactorsTranscription GeneticPhysiology[SDE.MCG]Environmental Sciences/Global ChangesAquaporinPlant ScienceAquaporinsPlant RootsQuercus roburQuercusHydraulic conductivityGene Expression Regulation PlantBotanyGeneticsHypoxiaQuercus robur (pedunculate oak)Plant ProteinsQuercus petraea (sessile oak)Water transportbiologyWaterWater channelbiology.organism_classificationOxygenPlant Leaves[ SDE.MCG ] Environmental Sciences/Global ChangesShootQuercus petraeaStress conditionsRoot hydraulic conductivityPlant ShootsPlant Physiology and Biochemistry
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The Marine Sponge-Derived Inorganic Polymers, Biosilica and Polyphosphate, as Morphogenetically Active Matrices/Scaffolds for the Differentiation of …

2014

The two marine inorganic polymers, biosilica (BS), enzymatically synthesized from ortho-silicate, and polyphosphate (polyP), a likewise enzymatically synthesized polymer consisting of 10 to >100 phosphate residues linked by high-energy phosphoanhydride bonds, have previously been shown to display a morphogenetic effect on osteoblasts. In the present study, the effect of these polymers on the differential differentiation of human multipotent stromal cells (hMSC), mesenchymal stem cells, that had been encapsulated into beads of the biocompatible plant polymer alginate, was studied. The differentiation of the hMSCs in the alginate beads was directed either to the osteogenic cell lineage by …

Stromal cellAlginatesPolymersCellular differentiationOsteogenesis DistractionPharmaceutical ScienceBone Morphogenetic Protein 2biosilica; polyphosphate; multipotent stromal cells; mesenchymal stem cells; alkaline phosphatase; 3D cell/tissue printing; distraction osteogenesisBone morphogenetic protein 2ChondrocyteArticleCollagen Type IGlucuronic AcidPolyphosphatesDrug Discoverymedicinemultipotent stromal cellsAnimalsHumansbiosilicaPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Collagen Type IImesenchymal stem cells3D cell/tissue printingOsteoblastsTissue ScaffoldsChemistryHexuronic AcidsMesenchymal stem cellBiomaterialpolyphosphateCell DifferentiationAnatomyChondrogenesisAlkaline PhosphataseSilicon DioxideCell biologyPoriferamedicine.anatomical_structuredistraction osteogenesislcsh:Biology (General)Alkaline phosphataseMarine Drugs
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Molecular evolution of the metazoan protein kinase C multigene family

1996

Protein kinases C (PKCs) comprise closely related Ser/Thr kinases, ubiquitously present in animal tissues ; they respond to second messengers, e.g., Ca2+ and/or diacylglycerol, to express their activities. Two PKCs have been sequenced from Geodia cydonium, a member of the lowest multicellular animals, the sponges (Porifera). One sponge G. cydonium PKC, GCPKC1, belongs to the ''novel'' (Ca2+-independent) PKC (nPKC) subfamily while the second one, GCPKC2, has the hall-marks of the ''conventional'' (Ca2+-dependent) PKC (cPKC) subfamily. The alignment of the Ser/Thr catalytic kinase domains, of the predicted aa sequences for these cDNAs with respective segments from previously reported sequence…

SubfamilyMolecular Sequence DataProtein Serine-Threonine KinasesHomology (biology)CatalysisEvolution MolecularGeneticsAnimalssponges ; Geodia cydonium ; serine/threonine kinases ; phylogeny ; molecular systematics ; molecular evolutionAmino Acid SequenceMolecular BiologyEcology Evolution Behavior and SystematicsProtein kinase CPhylogenyProtein Kinase CGeneticsProtein-Serine-Threonine KinasesbiologyBase SequenceSequence Homology Amino AcidKinaseCyclin-dependent kinase 2PKCSCell biologyPoriferaenzymes and coenzymes (carbohydrates)Protein kinase domainMultigene Familybiology.proteinbiological phenomena cell phenomena and immunity
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