Search results for "Axinella"

showing 4 items of 4 documents

New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities

2011

Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteas…

Magnetic Resonance Spectroscopyanti-trypanosomalmedicine.medical_treatmentCathepsin LStreptomyces axinellaePharmaceutical ScienceCathepsin BCathepsin BCathepsin LCathepsin ODrug DiscoveryPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Coronavirus 3C ProteasesLeishmania major0303 health sciencesbiology030302 biochemistry & molecular biologytetromycin; anti-trypanosomal; protease inhibition; <em>Streptomyces axinellae</em>; marine spongeTrypanocidal AgentsStreptomycesCysteine EndopeptidasesBiochemistrySevere acute respiratory syndrome-related coronavirusStreptomyces axinellaetetromycinBiologiemarine spongeddc:547ProteasesTrypanosoma brucei bruceiAntiprotozoal AgentsTrypanosoma bruceiHeterocyclic Compounds 4 or More RingsArticle03 medical and health sciencesViral ProteinsAxinellaparasitic diseasesmedicineAnimalsProtease Inhibitorsddc:610protease inhibition ; anti-trypanosomal ; Streptomyces axinellae ; tetromycin ; marine sponge030304 developmental biologyCathepsinProteasebiology.organism_classificationprotease inhibitionlcsh:Biology (General)biology.protein
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Damipipecolin and damituricin, novel bioactive bromopyrrole alkaloids from the Mediterranean sponge Axinella damicornis

2007

Two new bromopyrrole alkaloids, damipipecolin (1) and damituricin (2), have been isolated from the Mediterranean sponge Axinella damicornis, and their structures established through spectroscopic methods. Compounds 1 and 2 extend the structural variety of the so far known pyrrole alkaloids; in these compounds, the 4-bromopyrrole 2-carboxylic acid is directly condensed with a non-protein cyclic alpha-amino acid, the (2R, 4R)-trans-4-hydroxypipecolic acid and (2R, 4R)-cis-N,N'-dimethyl-4-hydroxyproline (D-turicine) in 1 and 2, respectively. Compounds 1 and 2 were found to display a modulating effect of the serotonin receptor activity in vitro.

N-MethylaspartateCell SurvivalStereochemistryClinical BiochemistryGlutamic AcidPharmaceutical ScienceBiochemistryNatural productchemistry.chemical_compoundAlkaloidsAxinellaBromopyrrole alkaloidDrug DiscoverySerotonin receptor activityAnimalsHumansOrganic chemistryPyrrolesMolecular BiologyCells CulturedPyrroleMarine spongeNeuronsMolecular StructurebiologyMediterranean RegionAlkaloidOrganic ChemistryAxinellaBiological activityGlutamic acidBrominebiology.organism_classificationRatsAxinella damicorniSpongechemistryMolecular MedicineSerotonin receptor activity.CalciumSuberitesSuberitesBioorganic &amp; Medicinal Chemistry
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Cycloamphilectenes, a new type of potent marine diterpenes: inhibition of nitric oxide production in murine macrophages.

2003

The inhibitory effect of a series of 6 cycloamphilectenes, novel marine diterpenes based on amphilectene skeletons and isolated from the Vanuatu sponge Axinella sp., on NO, PGE(2) and TNFalpha production in murine peritoneal macrophages was studied. These compounds reduced potently nitric oxide production in a concentration-dependent manner with IC(50) values in the submicromolar range (0.1-4.3 microM). Studies on intact cells and Western blot analysis showed that the more potent cycloamphilectenes reduced the expression of inducible nitric oxide synthase without affecting cyclo-oxygenase-2 expression. Among them cycloamphilectene 2, the unique compound bearing an exocyclic methylene group,…

NeutrophilsBlotting WesternNitric Oxide Synthase Type IIElectrophoretic Mobility Shift AssayIn Vitro TechniquesNitric OxideGeneral Biochemistry Genetics and Molecular BiologyDinoprostoneNitric oxidechemistry.chemical_compoundMiceStructure-Activity RelationshipWestern blotmedicineAnimalsEdemaHumansGeneral Pharmacology Toxicology and PharmaceuticsMethylenebiologymedicine.diagnostic_testPancreatic ElastaseTumor Necrosis Factor-alphaMacrophagesZymosanAnti-Inflammatory Agents Non-SteroidalAxinellaNF-kappa BMembrane ProteinsGeneral Medicinebiology.organism_classificationPoriferaNitric oxide synthaseIsoenzymesSpongechemistryBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide Synthasesbiology.proteinMacrophages PeritonealTumor necrosis factor alphaFemaleMarine ToxinsDiterpenesNitric Oxide SynthaseLife sciences
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Novel bioactive bromopyrrole alkaloids from the Mediterranean sponge Axinella verrucosa

2005

The Mediterranean sponge Axinella verrucosa has been investigated for its alkaloid composition and has been found to produce a complex mixture of bromopyrrole alkaloids. Along with the previously isolated compounds 5-18, four novel alkaloids of this class, compounds 1-4, have been isolated, and their structures established through spectroscopic methods. Compounds 1-4 were found to display neuroprotective activity against the agonists serotonin and glutamate in vitro.

SerotoninSpectrometry Mass Electrospray Ionizationendocrine systemAxinella verrucosaMagnetic Resonance SpectroscopyStereochemistryClinical BiochemistryThin layerGlutamic AcidPharmaceutical ScienceSpectrometry Mass Fast Atom BombardmentPharmacognosycomplex mixturesBiochemistryAnimal originPyrrole derivativesNatural productCell LineAlkaloidsBromopyrrole alkaloidDrug DiscoveryAnimalsPyrrolesheterocyclic compoundsMolecular BiologyNeuronsMarine spongeMolecular StructurebiologyChemistryorganic chemicalsAlkaloidOrganic ChemistryQuisqualic AcidBiological activitybiology.organism_classificationPoriferaSpongeNeuroprotective activity.Axinella verrucosaMolecular MedicineCalciumChromatography Thin LayerSerotonin AntagonistsExcitatory Amino Acid Antagonists
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