1,721,016 research outputs found
One-pot syntheses of pseudopteroxazoles from pseudopterosins : a rapid route to non-natural congeners with improved antimicrobial activity
No full textRapid one-pot methodologies to prepare pseudopteroxazole (1) and novel congeners from abundant natural pseudopterosins have been devised. This is highlighted here with the first synthesis of the marine natural product homopseudopteroxazole (2) utilizing a novel, silver(I)-mediated catechol to benzoxazole transformation. Pseudopteroxazoles and isopseudopteroxazoles exhibit potent activity against a range of important Gram-positive pathogens including Mycobacterium spp. and vancomycin-resistant Enterococcus faecium. Several non-natural pseudopteroxazoles exhibited strong activity against methicillin-resistant Staphylococcus aureus, thereby displaying a broader spectrum of antibiotic activity compared to pseudopteroxazole
Elisabethamine: a new diterpene alkaloid from Pseudopterogorgia elisabethae
No full textPT: JSource type: Prin
Purification and characterization of the fatty acid synthase from Bugula neritina
No full textThe fatty acid synthase from Bugula neritina has been purified 100-fold using ammonium sulfate precipitation, ion-exchange and size exclusion chromatography. The purified enzyme has a molecular weight of approximately 382,000 Da, as judged by gel filtration. Polyacrylamide gel electrophoresis under denaturing conditions in the presence of SDS revealed one major protein band of approximately 190,000 Da suggesting that the enzyme is a homodimer. The size of the enzyme, together with the observation that the FAS activity is independent of the concentration of acyl carrier protein, indicate that the FAS from Bugula neritina is a type I. A detailed analysis of the products of the purified FAS indicated that palmitic acid is the primary product and longer chain fatty acids are not produced.LR: 20061115; PUBM: Print; JID: 9516061; 524-14-1 (Malonyl Coenzyme A); 53-59-8 (NADP); 53-84-9 (NAD); 72-89-9 (Acetyl Coenzyme A); EC 6.- (Fatty Acid Synthetase Complex); ppublishSource type: Prin
In vivo and in vitro biosynthesis of saponins in sea cucumbers
No full textThe triterpene precursor of saponins in sea cucumbers has been identified as parkeol [lanost-9(11)-en-3 beta-ol] [1]. Dissection of the sea cucumbers Holothuria floridea and Actinopyga agassize after incubations with radiolabeled parkeol demonstrated that saponin biosynthesis occurs exclusively in the Cuvier gland. This result was corroborated by incubating a cell-free extract of the Cuvier gland with labeled parkeol and observing transformation of the precursor to saponins.LR: 20061115; PUBM: Print; JID: 7906882; 0 (Saponins); 0 (Terpenes); 28032-52-2 (parkeol); 79-63-0 (Lanosterol); ppublishSource type: Electronic(1
12-acetoxypseudopterolide: a new diterpene from Pseudopterogorgia elisabethae
No full textPT: JSource type: Prin
New antiproliferative epoxysecosterols from Pseudopterogorgia americana
No full textPT: JSource type: Prin
Development of N,O‐carboxymethyl chitosan‐starch biomaterial inks for 3D printed wound dressing applications
No full textIn this paper, a novel hybrid biomaterial ink consisting of two water-soluble polymers is investigated: starch and N,O-carboxymethyl chitosan (NOCC). The biomaterial ink is used to fabricate controlled release biodegradable wound dressing scaffolds via a novel low-temperature solvent (organic)-free 3D printing technique. NOCC is a variant of chitosan with a high degradation rate that can lead to an immediate release of the drugs, and starch, on the other hand, is used to alter degradation and drug release characteristics of the biomaterial. Mupirocin, a topical anti-infective, is incorporated into the biomaterial inks. Different biomaterial inks in terms of NOCC to starch ratio are prepared and characterized. Printability and rheology of the samples are investigated, and the release of mupirocin over time is quantified. The efficacy of the developed 3D printed wound dressings against Staphylococcus aureus is examined through disk diffusion assays. Increasing NOCC accelerated the release of the drug from the scaffold and led to larger zones of inhibition in the early hours of the in vitro tests; this phenomenon is correlated to the enhanced hydrophilicity of NOCC-dominated scaffolds. The drug release and the zone of inhibition are controlled by altering starch to NOCC ratio in the biomaterial ink
Development of 3D printed drug-eluting scaffolds for preventing piercing infection
No full textHerein, novel drug-eluting, bio-absorbable scaffold intended to cover piercing studs is introduced. This “biopierce” will stay in human tissue following piercing, and will slowly release an antimicrobial agent to prevent infection while the wound heals. Nearly 20% of all piercings lead to local infection. Therefore, it is imperative to develop alternative methods of piercing aftercare to prevent infection. Biopierces were made using mupirocin loaded poly-lactic-co-glycolic acid (PLGA) biomaterial ink, and a low-temperature 3D printing technique was used to fabricate the biopierces. Proton nuclear magnetic resonance (1H NMR) spectroscopy was used to confirm the complete removal of the solvent, and liquid chromatography high-resolution mass spectrometry (LC-HRMS) was used to confirm the structural integrity of mupirocin and to quantify the amount of the released drug over time. The efficacy of the biopierces against Staphylococcus aureus, one of the most common piercing-site pathogens, was confirmed over two weeks using in vitro antimicrobial susceptibility testingNatural Sciences and Engineering Research Council of CanadaCanada Foundation for InnovationMitacsUniversity of Prince Edward Islan
Chemical dereplication of marine actinomycetes by liquid chromatography-high resolution mass spectrometry profiling and statistical analysis.
No full textDiscovery of novel bioactive metabolites from marine bacteria is becoming increasingly challenging, and the development of novel approaches to improve the efficiency of early steps in the microbial drug discovery process is therefore of interest. For example, current protocols for the taxonomic dereplication of microbial strains generally use molecular tools which do not take into consideration the ability of these selected bacteria to produce secondary metabolites. As the identification of novel chemical entities is one of the key elements driving drug discovery programs, this study reports a novel methodology to dereplicate microbial strains by a metabolomics approach using liquid chromatography-high resolution mass spectrometry (LC-HRMS). In order to process large and complex three dimensional LC-HRMS datasets, the reported method uses a bucketing and presence-absence standardization strategy in addition to statistical analysis tools including principal component analysis (PCA) and cluster analysis. From a closely related group of Streptomyces isolated from geographically varied environments, we demonstrated that grouping bacteria according to the chemical diversity of produced metabolites is reproducible and provides greatly improved resolution for the discrimination of microbial strains compared to current molecular dereplication techniques. Importantly, this method provides the ability to identify putative novel chemical entities as natural product discovery leads.journal articleresearch support, non-u.s. gov't2013 Dec 172013 10 21importe
Pseudopterosin biosynthesis in Symbiodinium sp., the dinoflagellate symbiont of Pseudopterogorgia elisabethae
No full textInvestigations are reported that identify the biosynthetic source and origins of the pseudopterosins, pharmacologically important diterpene glycosides, in the gorgonian coral Pseudopterogorgia elisabethae. We report here the isolation of physiologically significant levels of endogenous pseudopterosins A, B, C, and D from purified symbionts identified as the dinoflagellate Symbiodinium sp. Biosynthetic studies in photosynthesizing symbiont isolates utilizing 14C-labeled inorganic carbon and the tritiated intermediate geranylgeranyl diphosphate yielded radiochemically pure pseudopterosins A through D and the first committed intermediate, elisabethatriene. The 14CO(2) uptake into the pseudopterosin pathway occurred at low levels compared to the 14CO(2) uptake into total lipids, suggesting a large reserve pool of the compounds. These results reveal for the first time that pseudopterosin biosynthesis is occurring within the algal symbiont and suggests the physiological implications of this biosynthesis.LR: 20061115; PUBM: Print; JID: 9500160; 0 (Diterpenes); 0 (Glycosides); 0 (pseudopterosins); ppublishSource type: Prin
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