0000000000093246

AUTHOR

Ute Hentschel

showing 6 related works from this author

Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Frac…

2014

In this paper, we report new protease inhibitory activity of plakortide E towards cathepsins and cathepsin-like parasitic proteases. We further report on its anti-parasitic activity against Trypanosoma brucei with an IC50 value of 5 mu M and without cytotoxic effects against J774.1 macrophages at 100 mu M concentration. Plakortide E was isolated from the sponge Plakortis halichondroides using enzyme assay-guided fractionation and identified by NMR spectroscopy and mass spectrometry. Furthermore, enzyme kinetic studies confirmed plakortide E as a non-competitive, slowly-binding, reversible inhibitor of rhodesain.

ProteasesStereochemistrymedicine.medical_treatmentTrypanosoma brucei bruceiPlakortis halichondroidesPharmaceutical ScienceTrypanosoma brucei01 natural sciences570 Life sciencesDioxanesprotease inhibitor03 medical and health sciencesddc:593Drug DiscoverymedicineAnimalsHumansProtease Inhibitorscathepsinlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)IC50030304 developmental biologyTrypanocidal agentrhodesainchemistry.chemical_classification0303 health sciencesProteaseAntiparasitic Agentsbiology010405 organic chemistryCommunicationplakortide Ebiology.organism_classificationCathepsinsTrypanocidal AgentsAntiparasitic agentProtease inhibitor (biology)Porifera0104 chemical sciencesCysteine Endopeptidasesslowly-binding reversible inhibitorEnzymelcsh:Biology (General)BiochemistrychemistryDrug Screening Assays Antitumor570 Biowissenschaftenmedicine.drug
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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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Antibacterial activity of the sponge Suberites domuncula and its primmorphs: potential basis for epibacterial chemical defense

2003

The epibacterial chemical defense of the marine sponge Suberites domuncula was explored by screening sponge extract, sponge primmorph (3-D aggregates containing proliferating cells) extract and sponge-associated as well as primmorph-associated bacteria for antibacterial activ- ity. 16S rDNA sequencing revealed that the antimicrobially active bacteria belonged to the α - and γ- subdivisions of Proteobacteria (α -Proteobacterium MBIC 3368, Idiomarina sp. and Pseudomonas sp., respectively). Moreover, a recombinant perforin-like protein was cloned from S. domuncula that dis- played strong antibacterial activity. Based on these observations, it is proposed that the sponge may be provided with a …

0303 health sciencesbiology030306 microbiologyPseudomonasAquatic Sciencebiology.organism_classificationMicrobiologySuberites domuncula03 medical and health sciencesSpongePseudomonadales14. Life underwaterProteobacteriaAntibacterial activityEcology Evolution Behavior and SystematicsBacteria030304 developmental biologyPseudomonadaceae
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Bioactive metabolites from the endophytic fungus Ampelomyces sp. isolated from the medicinal plant Urospermum picroides

2007

Extracts of cultures grown in liquid or on solid rice media of the fungal endophyte Ampelomyces sp. isolated from the medicinal plant Urospermum picroides exhibited considerable cytotoxic activity when tested in vitro against L5178Y cells. Chromatographic separation yielded 14 natural products that were unequivocally identified based on their 1H and 13C NMR as well as mass spectra and comparison with previously published data. Six compounds (2, 4, 5, 7, 9 and 11) were natural products. Both fungal extracts differed considerably in their secondary metabolites. The extract obtained from liquid cultures afforded a pyrone (2) and sulfated anthraquinones (7 and 9) along with the known compounds …

MetaboliteMicrobial Sensitivity TestsPlant ScienceAsteraceaeHorticultureBiochemistryEndophyteGas Chromatography-Mass SpectrometryEnterococcus faecalisPlant use of endophytic fungi in defenseMicrobiologyMicechemistry.chemical_compoundAnti-Infective AgentsAscomycotaCell Line TumorAnthraquinonesAnimalsFood scienceLeukemia L5178Urospermum picroidesMolecular BiologyPlants MedicinalBacteriaMolecular StructurebiologyCytotoxinsGeneral MedicineAntimicrobialbiology.organism_classificationPyronechemistryDrug Screening Assays AntitumorPhytochemistry
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Molecular response of the sponge Suberites domuncula to bacterial infection

2001

The aim of this study was the documentation of the molecular immune response of Suberites domuncula upon bacterial infection. Additionally, the bacteria that are naturally present in the sponge after prolonged aquarium maintenance were characterized. After 6 months of maintenance of S. domuncula in seawater aquaria, only one bacterial 16S rDNA sequence could be recovered, which belongs to the genus Pseudomonas. Concomitantly, morphologically uniform bacteria were found encapsulated in bacteriocytes. These findings indicate that certain bacteria, possibly of the genus Pseudomonas, are able to persist for long periods in host bacteriocytes. Subsequent to performing a previously established in…

EcologybiologyLipopolysaccharidep38 mitogen-activated protein kinasesPseudomonasAquatic Sciencebiology.organism_classificationVibrioMicrobiologySuberites domunculachemistry.chemical_compoundchemistryVibrionaceaeMitogen-activated protein kinasebiology.proteinEcology Evolution Behavior and SystematicsBacteriaMarine Biology
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From anti-fouling to biofilm inhibition: New cytotoxic secondary metabolites from two Indonesian Agelas sponges

2010

Chemical investigation of Indonesian marine sponges Agelas linnaei and A. nakamurai afforded 24 alkaloid derivatives representing either bromopyrrole or diterpene alkaloids. A. linnaei yielded 16 bromopyrrole alkaloids including 11 new natural products with the latter exhibiting unusual functionalities. The new compounds include the first iodinated tyramine-unit bearing pyrrole alkaloids, agelanesins A-D. These compounds exhibited cytotoxic activity against L5178Y mouse lymphoma cells with IC(50) values between 9.25 and 16.76 muM. Further new compounds include taurine acid substituted bromopyrrole alkaloids and a new dibromophakellin derivative. A. nakamurai yielded eight alkaloids among th…

Cell SurvivalStereochemistryMetaboliteClinical BiochemistryPharmaceutical ScienceAgelasineBiochemistryBromine CompoundsMicechemistry.chemical_compoundAlkaloidsCell Line TumorDrug DiscoveryStaphylococcus epidermidisAnimalsOrganic chemistryPyrrolesheterocyclic compoundsMolecular BiologybiologyCytotoxinsAlkaloidThoracicaOrganic ChemistryBiofilmBiological activitybiology.organism_classificationOximeAnti-Bacterial AgentsAgelaschemistryIndonesiaAgelasBiofilmsLarvaMolecular MedicineDiterpenesDiterpeneBioorganic & Medicinal Chemistry
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