37 research outputs found

    A Double Payload Complex between Hypericin and All-trans Retinoic Acid in the β-Lactoglobulin Protein

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    Combined therapies are usually used to treat acne vulgaris since this approach can tackle various foci simultaneously. Using a combination of spectroscopic, computational, and microbiological techniques and methods, herein we report on the use of β-lactoglobulin as a double payload carrier of hypericin (an antimicrobial photodynamic agent) and all-trans retinoic acid (an anti-inflammatory drug) for S. aureus in vitro photodynamic inactivation. The addition of all-trans retinoic acid to hypericinβ-lactoglobulin complex renders a photochemically safe vehicle due to the photophysical quenching of hypericin, which recovers its photodynamic activity when in contact with bacteria. The ability of hypericin to photoinactivate S. aureus was not affected by retinoic acid. β-Lactoglobulin is a novel biocompatible and photochemically safe nanovehicle with strong potential for the treatment of acne

    The Interaction of Hypericin with SARS-CoV-2 Reveals a Multimodal Antiviral Activity

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    Hypericin is a photosensitizing drug that is active against membrane-enveloped viruses and therefore constitutes a promising candidate for the treatment of SARS-CoV-2 infections. The antiviral efficacy of hypericin is largely determined by its affinity toward viral components and by the number of active molecules loaded on single viruses. Here we use an experimental approach to follow the interaction of hypericin with SARS-CoV-2, and we evaluate its antiviral efficacy, both in the dark and upon photoactivation. Binding to viral particles is directly visualized with fluorescence microscopy, and a strong affinity for the viral particles, most likely for the viral envelope, is measured spectroscopically. The loading of a maximum of approximately 30 molecules per viral particle is estimated, despite with marked heterogeneity among particles. Because of this interaction, nanomolar concentrations of photoactivated hypericin substantially reduce virus infectivity on Vero E6 cells, but a partial effect is also observed in dark conditions, suggesting multiple mechanisms of action for this drug

    Nanoscale Mapping of Recombinant Viral Proteins: From Cells to Virus-Like Particles

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    Influenza recombinant proteins and virus-like particles (VLPs) play an important role in vaccine development (e.g., CadiFlu-S). However, their production from mammalian cells suffers from low yields and lack of control of the final VLPs. To improve these issues, characterization techniques able to visualize and quantify the different steps of the process are needed. Fluorescence microscopy represents a powerful tool able to image multiple protein targets; however, its limited resolution hinders the study of viral constructs. Here, we propose the use of super-resolution microscopy and in particular of DNA-point accumulation for imaging in nanoscale topography (DNA-PAINT) microscopy as a characterization method for recombinant viral proteins on both cells and VLPs. We were able to quantify the amount of the three main influenza proteins (hemagglutinin (HA), neuraminidase (NA), and ion channel matrix protein 2 (M2)) per cell and per VLP with nanometer resolution and single-molecule sensitivity, proving that DNA-PAINT is a powerful technique to characterize recombinant viral constructs

    Valutazione della qualità dell’olio extra vergine di oliva mediante naso elettronico a sensori MOS

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    Abstract: Electronic noses are becoming a valuable tool for the organoleptic evaluation of food freshness, seasoning, geographical origin and shelf-life. This article reports a series of experiments aimed to highlight potentials and limits of MOS electronic noses in detecting defects present in extra virgin olive oil. The instrument is also able to discriminate olive oils obtained from the same fruits using respectively milling of stoned olives and traditional milling. Riassunto: I nasi elettronici si stanno affermando come uno strumento analitico-sensoriale innovativo per la caratterizzazione organolettica comparata dei prodotti alimentari in termini di freschezza, determinazione del’origine geografica, stagionatura. Nel presente lavoro viene studiato l’impiego di tale strumentazione nella qualificazione dell’olio extra vergine di oliva, con particolare riferimento all’individuazione dei difetti, ed alla discriminazione di oli ottenuti con trattamenti tecnologici differenti

    Synthesis of naphtho[2,3-b]indolizine-6,11-dione derivatives by iodine oxidation of 2-alkyl-1,4-naphthoquinones in the presence of substituted pyridines

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    Iodine oxidation of 2-alkyl-1,4-naphthoquinones (1) in the presence of substituted pyridines (2) afforded naphtho[2,3-b]indolizine-6,11-dione derivatives (3). Other oxidant systems (MnO2/I- or Fe(ClO4)3/I2) can be used and 2-alkylbenzoquinones reacted in lower yield. Iodination of 3 by I2 and dibenzoyl peroxide occurred seelctively at position 1

    The Crystal Structure of the Inclusion Complex of the Sodium Salt of Piroxicam with beta-Cyclodextrin

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    The structural characterization by X-ray diffraction analysis of the title compound is reported. Crystallographic details are: C42H70O35°C15H12N3O4 SNa·8D2O, triclinic, space group P1, a = 14.767(3), b = 12.237(2), c = 11.537(2)Å, α = 79.49(1), β = 110.91-(1), c = 104.61(1)°, d calc = 1.460 g/cm3, Z = 1, R = 0.045 for 6635 observed reflections. The crystal structure consists of head-to-tail β-cyclodextrin molecules (β-CD) linked together by piroxicam anions in infinite polymeric chains running along the c axis. In a chain each β-CD molecule takes up simultaneously two guest molecules including on the secondary hydroxyl end the benzene ring and on the primary hydroxyl end the pyridine ring of two adjacent piroxicam anions. The piroxicam anion is located with its central hydrophilic moiety at the interface between two adjacent β-CD molecules, forming with them hydrogen bonds through the enolate and amide oxygen atoms. Conformation of piroxicam is different from those observed for its neutral and zwitterionic forms. It assumes the ZZE conformation expected for the enolate. The six-coordinated sodium cation acts as a bridge between adjacent polymeric chains linking them along the b axis. This results in the formation of hydrophilic channels filled by deuterium oxide molecules
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