bluuebunny/crossref_metadata_2025 huggingface dataset:
Toxic, Radical Scavenging, and Antifungal Activity of Rhododendron tomentosum H. Essential Oils
Authors: Judzentiene Asta , Budiene Jurga , Svediene Jurgita , Garjonyte Rasa
Published: April 2020

The chemical composition of eight (seven shoot and one inflorescence) essential oils (EOs) of Rh. tomentosum H. plants growing in Eastern Lithuania is reported. The plant material was collected during different phases of vegetation (from April to October). The oils were obtained by hydrodistillation from air-dried aerial parts (leaves and inflorescences). In total, up to 70 compounds were identified by GC−MS and GC (flame-ionization detector, FID); they comprised 91.0 ± 4.7%–96.2 ± 3.1% of the oil content. Sesquiterpene hydrocarbons (54.1 ± 1.5%–76.1 ± 4.5%) were found to be the main fraction. The major compounds were palustrol (24.6 ± 2.6%–33.5 ± 4.4%) and ledol (18.0 ± 2.9%–29.0 ± 5.0%). Ascaridol isomers (7.0 ± 2.4%–14.0 ± 2.4% in three oils), myrcene (7.2 ± 0.3% and 10.1 ± 1.3%), lepalol (3.3 ± 0.3% and 7.9 ± 3.0%), and cyclocolorenone isomers (4.1 ± 2.5%) were determined as the third main constituents. The toxic activity of marsh rosemary inflorescence and shoot oils samples was evaluated using a brine shrimp (Artemia sp.) bioassay. LC50 average values (11.23–20.50 µg/mL) obtained after 24 h of exposure revealed that the oils were notably toxic. The oil obtained from shoots gathered in September during the seed-ripening stage and containing appreciable amounts of palustrol (26.0 ± 2.5%), ledol (21.5 ± 4.0%), and ascaridol (7.0 ± 2.4%) showed the highest toxic activity. Radical scavenging activity of Rh. tomentosum EOs depended on the plant vegetation stage. The highest activities were obtained for EOs isolated from young shoots collected in June (48.19 ± 0.1 and 19.89 ± 0.3 mmol/L TROLOX (6-hydroxy-2,5,7,8-tetra-methylchromane-2-carboxylic acid) equivalent obtained by, respectively, ABTS•+ (2,2′-amino-bis(ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and DPPH•(2,2-diphenyl-1-picrylhydrazyl) assays). Agar disc diffusion assay against pathogenic yeast Candida parapsilosis revealed the potential antifungal activity of EOs. An alternative investigation of antifungal activity employed mediated amperometry at yeast Saccharomyces cerevisiae-modified electrodes. The subjection of yeast cells to vapors of EO resulted in a three to four-fold increase of electrode responses due to the disruption of yeast cell membranes.
A Peptide Nucleic Acid (PNA) Masking the miR-145-5p Binding Site of the 3′UTR of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) mRNA Enhances CFTR Expression in Calu-3 Cells
Authors: Sultan Shaiq , Rozzi Andrea , Gasparello Jessica , Manicardi Alex , Corradini Roberto , Papi Chiara , Finotti Alessia , Lampronti Ilaria , Reali Eva , Cabrini Giulio , Gambari Roberto , Borgatti Monica
Published: April 2020

Peptide nucleic acids (PNAs) have been demonstrated to be very useful tools for gene regulation at different levels and with different mechanisms of action. In the last few years the use of PNAs for targeting microRNAs (anti-miRNA PNAs) has provided impressive advancements. In particular, targeting of microRNAs involved in the repression of the expression of the cystic fibrosis transmembrane conductance regulator (CFTR) gene, which is defective in cystic fibrosis (CF), is a key step in the development of new types of treatment protocols. In addition to the anti-miRNA therapeutic strategy, inhibition of miRNA functions can be reached by masking the miRNA binding sites present within the 3′UTR region of the target mRNAs. The objective of this study was to design a PNA masking the binding site of the microRNA miR-145-5p present within the 3′UTR of the CFTR mRNA and to determine its activity in inhibiting miR-145-5p function, with particular focus on the expression of both CFTR mRNA and CFTR protein in Calu-3 cells. The results obtained support the concept that the PNA masking the miR-145-5p binding site of the CFTR mRNA is able to interfere with miR-145-5p biological functions, leading to both an increase of CFTR mRNA and CFTR protein content.
Photoprotective Effect of Dietary Galacto-Oligosaccharide (GOS) in Hairless Mice via Regulation of the MAPK Signaling Pathway
Authors: Suh Min Geun , Bae Gi Yeon , Jo Kyungae , Kim Jin Man , Hong Ki-Bae , Suh Hyung Joo
Published: April 2020

This study investigated the suppression of photoaging by galacto-oligosaccharide (GOS) ingestion following exposure to ultraviolet (UV) radiation. To investigate its photoprotective effects, GOS along with collagen tripeptide (CTP) as a positive control was orally administered to hairless mice under UVB exposure for 8 weeks. The water holding capacity, transepidermal water loss (TEWL), and wrinkle parameters were measured. Additionally, quantitative reverse-transcription polymerase chain reaction and Western blotting were used to determine mRNA expression and protein levels, respectively. The GOS or CTP orally-administered group showed a decreased water holding capacity and increased TEWL compared to those of the control group, which was exposed to UVB (CON) only. In addition, the wrinkle area and mean wrinkle length in the GOS and CTP groups significantly decreased. Skin aging-related genes, matrix metalloproteinase, had significantly different expression levels in the CTP and GOS groups. Additionally, the tissue inhibitor of metalloproteinases and collagen type I gene expression in the CTP and GOS groups significantly increased. Oral administration of GOS and CTP significantly lowered the tissue cytokine (interleukin-6 and -12, and tumor necrosis factor-α) levels. There was a significant difference in UVB-induced phosphorylation of JNK, p38, and ERK between the GOS group and the CON group. Our findings indicate that GOS intake can suppress skin damage caused by UV light and has a UV photoprotective effect.
Discovery of Novel Inhibitor for WNT/β-Catenin Pathway by Tankyrase 1/2 Structure-Based Virtual Screening
Authors: Li Bo , Liang Jinxia , Lu Feng , Zeng Guandi , Zhang Jindao , Ma Yinxing , Liu Peng , Wang Qin , Zhou Qian , Chen Liang
Published: April 2020

Aberrant activation of the WNT/β-catenin signaling pathway is implicated in various types of cancers. Inhibitors targeting the Wnt signaling pathway are intensively studied in the current cancer research field, the outcomes of which remain to be determined. In this study, we have attempted to discover novel potent WNT/β-catenin pathway inhibitors through tankyrase 1/2 structure-based virtual screening. After screening more than 13.4 million compounds through molecular docking, we experimentally verified one compound, LZZ-02, as the most potent inhibitor out of 11 structurally representative top hits. LiCl-induced HEK293 cells containing TOPFlash reporter showed that LZZ-02 inhibited the transcriptional activity of β-catenin with an IC50 of 10 ± 1.2 μM. Mechanistically, LZZ-02 degrades the expression of β-catenin by stabilizing axin 2, thereby diminishing downstream proteins levels, including c-Myc and cyclin D1. LZZ-02 also inhibits the growth of colonic carcinoma cell harboring constitutively active β-catenin. More importantly, LZZ-02 effectively shrinks tumor xenograft derived from colonic cell lines. Our study successfully identified a novel tankyrase 1/2 inhibitor and shed light on a novel strategy for developing inhibitors targeting the WNT/β-catenin signaling axis.
Influence of Carboxylate Anions on Phase Behavior of Choline Ionic Liquid Mixtures
Authors: Elhi Fred , Gantman Mikhail , Nurk Gunnar , Schulz Peter S. , Wasserscheid Peter , Aabloo Alvo , Põhako-Esko Kaija
Published: April 2020

Mixing ionic liquids is a suitable strategy to tailor properties, e.g., to reduce melting points. The present study aims to widen the application range of low-toxic choline-based ionic liquids by studying eight binary phase diagrams of six different choline carboxylates. Five of them show eutectic points with melting points dropping by 13 to 45 °C. The eutectic mixtures of choline acetate and choline 2-methylbutarate were found to melt at 45 °C, which represents a remarkable melting point depression compared to the pure compounds with melting points of 81 (choline acetate) and 90 °C (choline 2-methylbutarate), respectively. Besides melting points, the thermal stabilities of the choline salt mixtures were investigated to define the thermal operation range for potential practical applications of these mixtures. Typical decomposition temperatures were found between 165 and 207 °C, with choline lactate exhibiting the highest thermal stability.
Push–Pull Zinc Phthalocyanine Bearing Hexa-Tertiary Substituted Carbazolyl Donor Groups for Dye-Sensitized Solar Cells
Authors: Ghazal Basma , Azizi Kobra , Ewies Ewies F. , Youssef Ahmed S. A. , Mwalukuku Valid Mwatati , Demadrille Renaud , Torres Tomás , Makhseed Saad
Published: April 2020

An asymmetrical, push–pull phthalocyanine bearing bulky tert-butylcarbazolyl moieties as electron donor and carboxylic acid as anchoring group was synthetized and tested as a photosensitizer in dye-sensitized solar cells (DSSC). The new photosensitizer was characterized by 1H and 13C NMR, UV–Vis and mass spectrometry. The bulky tert-butylcarbazolyl moieties avoid the aggregation of the phthalocyanine dye. DFT studies indicate that the HOMO is delocalized throughout the -electron system of the substituted phthalocyanine and the LUMO is located on the core of the molecule with a sizable electron density distribution on carboxyl groups. The new dye has been used as a photosensitizer in transparent and opaque dye-sensitized solar cells, which exhibit poor efficiencies related to a low Jsc.
Optimization of ZnO Nanorods Growth on Polyetheresulfone Electrospun Mats to Promote Antibacterial Properties
Authors: Salmeri Mario , Ognibene Giulia , Saitta Lorena , Lombardo Cinzia , Genovese Carlo , Barcellona Matteo , D’Urso Alessandro , Spitaleri Luca , Blanco Ignazio , Cicala Gianluca , Gulino Antonino , Fragalà Maria Elena
Published: April 2020

Zinc oxide (ZnO) nanorods grown by chemical bath deposition (CBD) on the surface of polyetheresulfone (PES) electrospun fibers confer antimicrobial properties to the obtained hybrid inorganic–polymeric PES/ZnO mats. In particular, a decrement of bacteria colony forming units (CFU) is observed for both negative (Escherichia coli) and positive (Staphylococcus aureus and Staphylococcus epidermidis) Grams. Since antimicrobial action is strictly related to the quantity of ZnO present on surface, a CBD process optimization is performed to achieve the best results in terms of coverage uniformity and reproducibility. Scanning electron microscopy (SEM) and X-ray photoelectron spectroscopy (XPS) provide morphological and compositional analysis of PES/ZnO mats while thermogravimetric analysis (TGA) is useful to assess the best process conditions to guarantee the higher amount of ZnO with respect to PES scaffold. Biocidal action is associated to Zn2+ ion leaching in solution, easily indicated by UV–Vis measurement of metallation of free porphyrin layers deposited on glass.
New Insights into 4-Anilinoquinazolines as Inhibitors of Cardiac Troponin I–Interacting Kinase (TNNi3K)
Authors: Asquith Christopher R. M. , Laitinen Tuomo , Wells Carrow I. , Tizzard Graham J. , Zuercher William J.
Published: April 2020

We report the synthesis of several related 4-anilinoquinazolines as inhibitors of cardiac troponin I–interacting kinase (TNNi3K). These close structural analogs of 3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide (GSK114) provide new understanding of structure–activity relationships between the 4-anilinoquinazoline scaffold and TNNi3K inhibition. Through a small focused library of inhibitors, we observed that the N-methylbenzenesulfonamide was driving the potency in addition to the more traditional quinazoline hinge-binding motif. We also identified a compound devoid of TNNi3K kinase activity due to the addition of a methyl group in the hinge binding region. This compound could serve as a negative control in the study of TNNi3K biology. Small molecule crystal structures of several quinazolines have been solved, supporting observations made about overall conformation and TNNi3K inhibition.
Aggregation and Molecular Properties of β-Glucosidase Isoform II in Chayote (Sechium edule)
Authors: Cruz Rodríguez Alberto , Sánchez Esperanza Fabiola Anaid , Pérez-Campos Eduardo , Hernández-Huerta María Teresa , Pérez-Campos Mayoral Laura , Matias-Cervantes Carlos Alberto , Martínez Barras Alexis , Mayoral-Andrade Gabriel , Santos Pineda Luis Ángel , Díaz Barrita Aymara Judith , Zenteno Edgar , Romero Díaz Carlos , Martínez Cruz Ruth , Pérez-Campos Mayoral Eduardo , Bernabé Pérez Edith Alhelí , Pérez Santiago Alma Dolores , Pina-Canseco María del Socorro , Martínez Cruz Margarito
Published: April 2020

The presence of isoforms of β-glucosidase has been reported in some grasses such as sorghum, rice and maize. This work aims to extract and characterize isoform II in β-glucosidase from S. edule. A crude extract was prepared without buffer solution and adjusted to pH 4.6. Contaminating proteins were precipitated at 4 °C for 24 h. The supernatant was purified by chromatography on carboxymethyl cellulose (CMC) column, molecular exclusion on Sephacryl S-200HR, and exchange anionic on QFF column. Electrophoretic analyzes revealed a purified enzyme with aggregating molecular complex on SDS-PAGE, Native-PAGE, and AU-PAGE. Twelve peptides fragments were identified by nano liquid chromatography-tandem mass spectrometry (nano LC-ESI-MS/MS), which presented as 61% identical to Cucurbita moschata β-glucosidase and 55.74% identical to β-glucosidase from Cucumis sativus, another Cucurbitaceous member. The relative masses which contained 39% hydrophobic amino acids ranged from 982.49 to 2,781.26. The enzyme showed a specificity to β-d-glucose with a Km of 4.59 mM, a Vmax value of 104.3 μM∙min−1 and a kcat of 10,087 μM∙min−1 using p-nitrophenyl-β-D-glucopyranoside. The presence of molecular aggregates can be attributed to non-polar amino acids. This property is not mediated by a β-glucosidase aggregating factor (BGAF) as in grasses (maize and sorghum). The role of these aggregates is discussed.
Co-Microencapsulation of Anthocyanins from Black Currant Extract and Lactic Acid Bacteria in Biopolymeric Matrices
Authors: Enache Iuliana Maria , Vasile Aida Mihaela , Enachi Elena , Barbu Vasilica , Stănciuc Nicoleta , Vizireanu Camelia
Published: April 2020

Anthocyanins from black currant extract and lactic acid bacteria were co-microencapsulated using a gastro-intestinal-resistant biocomposite of whey protein isolate, inulin, and chitosan, with an encapsulation efficiency of 95.46% ± 1.30% and 87.38% ± 0.48%, respectively. The applied freeze-drying allowed a dark purple stable powder to be obtained, with a satisfactory content of phytochemicals and 11 log colony forming units (CFU)/g dry weight of powder (DW). Confocal laser microscopy displayed a complex system, with several large formations and smaller aggregates inside, consisting of biologically active compounds, lactic acid bacteria cells, and biopolymers. The powder showed good storage stability, with no significant changes in phytochemicals and viable cells over 3 months. An antioxidant activity of 63.64 ± 0.75 mMol Trolox/g DW and an inhibitory effect on α-amylase and α-glucosidase of 87.10% ± 2.08% and 36.96% ± 3.98%, respectively, highlighted the potential biological activities of the co-microencapsulated powder. Significantly, the in vitro digestibility profile showed remarkable protection in the gastric environment, with controlled release in the intestinal simulated environment. The powder was tested by addition into a complex food matrix (yogurt), and the results showed satisfactory stability of biologically active compounds when stored for 21 d at 4 °C. The obtained results confirm the important role of microencapsulation in ensuring a high degree of protection, thus allowing new approaches in developing food ingredients and nutraceuticals, with enhanced functionalities.
Interactions among Odorants, Phenolic Compounds, and Oral Components and Their Effects on Wine Aroma Volatility
Authors: Perez-Jiménez María , Esteban-Fernández Adelaida , Muñoz-González Carolina , Pozo-Bayón María Angeles
Published: April 2020

To determine the impact of oral physiology on the volatility of typical wine aroma compounds, mixtures of a synthetic wine with oral components (centrifuged human saliva (HS), artificial saliva with mucin (AS), and buccal epithelial cells (BC)) were prepared. Each wine type was independently spiked with four relevant wine odorants (guaiacol, β-phenyl ethanol, ethyl hexanoate, and β-ionone). Additionally, the impact of four types of phenolic compounds (gallic acid, catechin, grape seed extract, and a red wine extract) on aroma volatility in the HS, AS, and BC wines was also assessed. Static headspace was measured at equilibrium by solid phase microextraction–GC/MS analysis. Results showed a significant impact of oral components on the volatility of the four tested odorants. Independently of the type of aroma compound, aroma volatility was in general, higher in wines with BC. Moreover, while guaiacol and ethyl hexanoate volatility was significantly lower in wines with HS compared to wines with AS, β-ionone showed the opposite behavior, which might be related to metabolism and retention of mucin, respectively. Phenolic compounds also showed a different effect on aroma volatility depending on the type of compound and wine. Gallic acid had little effect on polar compounds but it enhanced the volatility of the most hydrophobic ones (ethyl hexanoate and β-ionone). In general, flavonoid type polyphenols significantly reduced the volatility of both polar (guaiacol and β-phenyl ethanol) and hydrophobic compounds (β-ionone in HS and BC wines), but through different mechanisms (e.g., π–π interactions and hydrophobic binding for polar and apolar odorants respectively). On the contrary, flavonoids enhanced the volatility of ethyl hexanoate, which might be due to the inhibition exerted on some salivary enzymes (e.g., carboxyl esterase) involved in the metabolism of this odorant molecule.
Hydroxycinnamoyl Amino Acids Conjugates: A Chiral Pool to Distinguish Commercially Exploited Coffea spp.
Authors: Berti Federico , Navarini Luciano , Colomban Silvia , Forzato Cristina
Published: April 2020

The synthesis of five hydroxycinnamoyl amides (HCAs) was accomplished and their identification and quantification in the green coffee bean samples of Coffea arabica, Coffea canephora, and Coffea liberica was performed. The HCAs p-coumaroyl-N-tyrosine 1b, caffeoyl-N-phenylalanine 2b, caffeoyl-N-tyrosine 3b, and p-coumaroyl-N-tryptophan 4b were characteristic of the C. canephora species while caffeoyl-N-tryptophan 5b was present in both C. canephora and C. arabica, but with higher content in C. canephora. The HCAs presence was also analyzed in C. liberica for the first time and none of the targeted compounds was found, indicating that this species is very similar to C. arabica species. Between C. canephora samples from various origins, significant differences were observed regarding the presence of all the HCAs, with C. canephora from Tanzania containing all five derivatives.
Plastics in Heritage Science: Analytical Pyrolysis Techniques Applied to Objects of Design
Authors: Nasa Jacopo La , Biale Greta , Ferriani Barbara , Trevisan Rafaela , Colombini Maria Perla , Modugno Francesca
Published: April 2020

The first synthetic polymers were introduced as constituents of everyday life, design objects, and artworks at the end of the 19th century. Since then, the history of design has been strictly connected with the 20th century evolution of plastic materials. Objects of design from the 20th century are today a precious part of the cultural heritage. They raise specific conservation issues due to the degradation processes affecting synthetic polymer-based plastics. Museums and collections dealing with the conservation of design objects and modern materials need to base their conservation strategies on compositional data that reveal the formulations of historical plastics and their decay processes. Specific and specifically optimized analytical tools are thus needed. We employed flash analytical pyrolysis coupled with gas chromatography and mass spectrometry (Py-GC/MS) and evolved gas analysis coupled with mass spectrometry (EGA-MS) to characterize “historic polymeric materials” (HIPOMS) and heritage plastics at the molecular level with high chemical detail. This approach complements non-invasive spectroscopic diagnosis whenever it fails to obtain significant or complete information on the nature and the state of preservation of the materials under study. We determined the composition of several 20th century design objects (1954–1994) from the Triennale Design Museum of Milan (Triennale Milano - Museo del Design Italiano), which for different morphological, chemical, or physical reasons were unsuitable for characterization by non-invasive spectroscopy. EGA-MS proved capable for the study of the different fractions constituting heterogeneous micro-samples and for gaining an insight into their degradation processes from the contextual interpretation of thermal and mass-spectrometric data.
Antibacterial Natural Halimanes: Potential Source of Novel Antibiofilm Agents
Authors: Tobal Ignacio E. , Roncero Alejandro M. , Moro Rosalina F. , Díez David , Marcos Isidro S.
Published: April 2020

The development of new agents against bacteria is an urgent necessity for human beings. The structured colony of bacterial cells, called the biofilm, is used to defend themselves from biocide attacks. For this reason, it is necessary to know their structures, develop new agents to eliminate them and to develop new procedures that allow an early diagnosis, by using biomarkers. Among natural products, some derivatives of diterpenes with halimane skeleton show antibacterial activity. Some halimanes have been isolated from marine organisms, structurally related with halimanes isolated from Mycobacterium tuberculosis. These halimanes are being evaluated as virulence factors and as tuberculosis biomarkers, this disease being one of the major causes of mortality and morbidity. In this work, the antibacterial halimanes will be reviewed, with their structural characteristics, activities, sources and the synthesis known until now.
Composite Polymers Development and Application for Polymer Electrolyte Membrane Technologies—A Review
Authors: Gagliardi Gabriele G. , Ibrahim Ahmed , Borello Domenico , El-Kharouf Ahmad
Published: April 2020

Nafion membranes are still the dominating material used in the polymer electrolyte membrane (PEM) technologies. They are widely used in several applications thanks to their excellent properties: high proton conductivity and high chemical stability in both oxidation and reduction environment. However, they have several technical challenges: reactants permeability, which results in reduced performance, dependence on water content to perform preventing the operation at higher temperatures or low humidity levels, and chemical degradation. This paper reviews novel composite membranes that have been developed for PEM applications, including direct methanol fuel cells (DMFCs), hydrogen PEM fuel cells (PEMFCs), and water electrolysers (PEMWEs), aiming at overcoming the drawbacks of the commercial Nafion membranes. It provides a broad overview of the Nafion-based membranes, with organic and inorganic fillers, and non-fluorinated membranes available in the literature for which various main properties (proton conductivity, crossover, maximum power density, and thermal stability) are reported. The studies on composite membranes demonstrate that they are suitable for PEM applications and can potentially compete with Nafion membranes in terms of performance and lifetime.
Main-Chain Phosphorus-Containing Polymers for Therapeutic Applications
Authors: Strasser Paul , Teasdale Ian
Published: April 2020

Polymers in which phosphorus is an integral part of the main chain, including polyphosphazenes and polyphosphoesters, have been widely investigated in recent years for their potential in a number of therapeutic applications. Phosphorus, as the central feature of these polymers, endears the chemical functionalization, and in some cases (bio)degradability, to facilitate their use in such therapeutic formulations. Recent advances in the synthetic polymer chemistry have allowed for controlled synthesis methods in order to prepare the complex macromolecular structures required, alongside the control and reproducibility desired for such medical applications. While the main polymer families described herein, polyphosphazenes and polyphosphoesters and their analogues, as well as phosphorus-based dendrimers, have hitherto predominantly been investigated in isolation from one another, this review aims to highlight and bring together some of this research. In doing so, the focus is placed on the essential, and often mutual, design features and structure–property relationships that allow the preparation of such functional materials. The first part of the review details the relevant features of phosphorus-containing polymers in respect to their use in therapeutic applications, while the second part highlights some recent and innovative applications, offering insights into the most state-of-the-art research on phosphorus-based polymers in a therapeutic context.
Preoperative and Intraoperative Methods of Parathyroid Gland Localization and the Diagnosis of Parathyroid Adenomas
Authors: Baj Jacek , Sitarz Robert , Łokaj Marek , Forma Alicja , Czeczelewski Marcin , Maani Amr , Garruti Gabriella
Published: April 2020

Accurate pre-operative determination of parathyroid glands localization is critical in the selection of minimally invasive parathyroidectomy as a surgical treatment approach in patients with primary hyperparathyroidism (PHPT). Its importance cannot be overemphasized as it helps to minimize the harmful side effects associated with damage to the parathyroid glands such as in hypocalcemia, severe hemorrhage or recurrent laryngeal nerve dysfunction. Preoperative and intraoperative methods decrease the incidence of mistakenly injuring the parathyroid glands and allow for the timely diagnosis of various abnormalities, including parathyroid adenomas. This article reviews 139 studies conducted between 1970 and 2020 (49 years). Studies that were reviewed focused on several techniques including application of carbon nanoparticles, carbon nanoparticles with technetium sestamibi (99m Tc-MIBI), Raman spectroscopy, near-infrared autofluorescence, dynamic optical contrast imaging, laser speckle contrast imaging, shear wave elastography, and indocyanine green to test their potential in providing proper parathyroid glands’ localization. Apart from reviewing the aforementioned techniques, this study focused on the applications that helped in the detection of parathyroid adenomas. Results suggest that applying all the reviewed techniques significantly improves the possibility of providing proper localization of parathyroid glands, and the application of indocyanine green has proven to be the ‘ideal’ approach for the diagnosis of parathyroid adenomas.
Theoretical Studies Aimed at Finding FLT3 Inhibitors and a Promising Compound and Molecular Pattern with Dual Aurora B/FLT3 Activity
Authors: Fernandes Ítalo Antônio , Braga Resende Déborah , Ramalho Teodorico Castro , Kuca Kamil , da Cunha Elaine Fontes Ferreira
Published: April 2020

FLT3 and dual Aurora B/FLT3 inhibitors have shown relevance in the search for promising new anticancer compounds, mainly for acute myeloid leukemia (AML). This study was designed to investigate the interactions between human FLT3 in the kinase domain with several indolin−2-one derivatives, structurally similar to Sunitinib. Molegro Virtual Docker (MVD) software was utilized in docking analyses. The predicted model of the training group, considering nineteen amino acid residues, performed in Chemoface, achieved an R2 of 0.82, suggesting that the binding conformations of the ligands with FLT3 are reasonable, and the data can be used to predict the interaction energy of other FLT3 inhibitors with similar molecular patterns. The MolDock Score for energy for compound 1 showed more stable interaction energy (–233.25 kcal mol−1) than the other inhibitors studied, while Sunitinib presented as one of the least stable (–160.94 kcal mol−1). Compounds IAF70, IAF72, IAF75, IAF80, IAF84, and IAF88 can be highlighted as promising derivatives for synthesis and biological evaluation against FLT3. Furthermore, IAF79 can be considered to be a promising dual Aurora B/FLT3 inhibitor, and its molecular pattern can be exploited synthetically to search for new indolin−2-one derivatives that may become drugs used in the treatment of cancers, including AML.
Applications of Near Infrared Photoacoustic Spectroscopy for Analysis of Human Respiration: A Review
Authors: Dumitras Dan C. , Petrus Mioara , Bratu Ana-Maria , Popa Cristina
Published: April 2020

In this review, applications of near-infrared photoacoustic spectroscopy are presented as an opportunity to evaluate human respiration because the measurement of breath is fast, intact and simple to implement. Recently, analytical methods for measuring biomarkers in exhaled air have been extensively developed. With laser-based photoacoustic spectroscopy, volatile organic compounds can be identified with high sensitivity, at a high rate, and with very good selectivity. The literature review has shown the applicability of near-infrared photoacoustic spectroscopy to one of the problems of the real world, i.e., human health. In addition, the review will consider and explore different breath sampling methods for human respiration analysis.
Spectroscopic Characterization of Emulsions Generated with a New Laser-Assisted Device
Authors: Dinache Andra , Tozar Tatiana , Smarandache Adriana , Andrei Ionut Relu , Nistorescu Simona , Nastasa Viorel , Staicu Angela , Pascu Mihail-Lucian , Romanitan Mihaela Oana
Published: April 2020

This paper presents a spectroscopic study of emulsions generated with a laser-assisted device. Fourier transform infrared (FTIR), Raman and UV–Vis–NIR reflectance spectra of emulsions, recorded before and after exposure to laser radiation were used to characterize the effect of laser irradiation. The paper also presents a comparison between the calculated IR spectra and the experimental FTIR spectra of an emulsion’s components. FTIR measurements allowed the identification of absorption bands specific to each of the emulsions’ components. Moreover, it enabled the observation of destabilization of the emulsion in real-time. Raman spectroscopy allowed the observation of the modifications at a molecular level, by identifying the vibrations of the representative functional groups and the polymerization of sodium tetradecyl sulfate (STS) molecules by analyzing the evolution of the carbonyl band. UV–Vis–NIR reflectance spectra of emulsions before and after exposure to laser radiation showed that the physical characteristics of the emulsions changed during irradiation—the dimensions of the droplets decreased, leading to an emulsion with a better time stability. These results proved that the employed spectroscopy techniques were powerful tools in emulsion analysis.
Synthesis and Evaluation of Artificial Nucleic Acid Bearing an Oxanorbornane Scaffold
Authors: Komine Hibiki , Mori Shohei , Morihiro Kunihiko , Ishida Kenta , Okuda Takumi , Kasahara Yuuya , Aoyama Hiroshi , Yamaguchi Takao , Obika Satoshi
Published: April 2020

Natural oligonucleotides have many rotatable single bonds, and thus their structures are inherently flexible. Structural flexibility leads to an entropic loss when unwound oligonucleotides form a duplex with single-stranded DNA or RNA. An effective approach to reduce such entropic loss in the duplex-formation is the conformational restriction of the flexible phosphodiester linkage and/or sugar moiety. We here report the synthesis and biophysical properties of a novel artificial nucleic acid bearing an oxanorbornane scaffold (OxNorNA), where the adamant oxanorbornane was expected to rigidify the structures of both the linkage and sugar parts of nucleic acid. OxNorNA phosphoramidite with a uracil (U) nucleobase was successfully synthesized over 15 steps from a known sugar-derived cyclopentene. Thereafter, the given phosphoramidite was incorporated into the designed oligonucleotides. Thermal denaturation experiments revealed that oligonucleotides modified with the conformationally restricted OxNorNA-U properly form a duplex with the complementally DNA or RNA strands, although the Tm values of OxNorNA-U-modified oligonucleotides were lower than those of the corresponding natural oligonucleotides. As we had designed, entropic loss during the duplex-formation was reduced by the OxNorNA modification. Moreover, the OxNorNA-U-modified oligonucleotide was confirmed to have extremely high stability against 3′-exonuclease activity, and its stability was even higher than those of the phosphorothioate-modified counterparts (Sp and Rp). With the overall biophysical properties of OxNorNA-U, we expect that OxNorNA could be used for specialized applications, such as conformational fixation and/or bio-stability enhancement of therapeutic oligonucleotides (e.g., aptamers).
Towards Building Blocks for Supramolecular Architectures Based on Azacryptates
Authors: Miljkovic Ana , La Cognata Sonia , Bergamaschi Greta , Freccero Mauro , Poggi Antonio , Amendola Valeria
Published: April 2020

In this work, we report the synthesis of a new bis(tris(2-aminoethyl)amine) azacryptand L with triphenyl spacers. The binding properties of its dicopper complex for aromatic dicarboxylate anions (as TBA salts) were investigated, with the aim to obtain potential building blocks for supramolecular structures like rotaxanes and pseudo-rotaxanes. As expected, UV-Vis and emission studies of [Cu2L]4+ in water/acetonitrile mixture (pH = 7) showed a high affinity for biphenyl-4,4′-dicarboxylate (dfc2−), with a binding constant of 5.46 log units, due to the best match of the anion bite with the Cu(II)-Cu(II) distance in the cage’s cavity. Compared to other similar bistren cages, the difference of the affinity of [Cu2L]4+ for the tested anions was not so pronounced: conformational changes of L seem to promote a good interaction with both long (e.g., dfc2−) and short anions (e.g., terephthalate). The good affinity of [Cu2L]4+ for these dicarboxylates, together with hydrophobic interactions within the cage’s cavity, may promote the self-assembly of a stable 1:1 complex in water mixture. These results represent a good starting point for the application of these molecular systems as building units for the design of new supramolecular architectures based on non-covalent interactions, which could be of interest in all fields related to supramolecular devices.
Analysis of Total Thiols in the Urine of a Cystathionine β-Synthase-Deficient Mouse Model of Homocystinuria Using Hydrophilic Interaction Chromatography
Authors: Chang Chun-Fang , Hamase Kenji , Tsunoda Makoto
Published: April 2020

Homocysteine and related thiols (cysteine, cysteinylglycine, and glutathione) in the urine of a cystathionine β-synthase (CBS)-deficient mouse model were quantified using hydrophilic interaction chromatography with fluorescence detection. Urine samples were incubated with tris(2-carboxyethyl) phosphine to reduce disulfide bonds into thiols. After deproteinization, thiols were fluorescently derivatized with ammonium 7-fluoro-2,1,3-benzoxadiazole-4-sulfonate (SBD-F). Homocysteine, cysteine, cysteinylglycine, and glutathione in mouse urine were analyzed using an amide-type column with a mobile phase of acetonitrile/120 mM ammonium formate buffer (pH 3.0) (81:19). The developed method was well-validated. Thiol concentrations in the urine of CBS-wild type (-WT), -heterozygous (-Hetero), and -knockout (-KO) mice were quantified using the developed method. As expected, total homocysteine concentration in CBS-KO mice was significantly higher than that in CBS-WT and CBS-Hetero mice. The developed method shows promise for diagnoses in preclinical and clinical studies.
Suppressive Effect of Arctium Lappa L. Leaves on Retinal Damage Against A2E-Induced ARPE-19 Cells and Mice
Authors: Kim Dong , Choi Yae , Shim Jaewon , Choi Yun-Sang , Kim Yun , Kim Mina , Kim Min
Published: April 2020

Age-related macular degeneration (AMD) is a major cause of irreversible loss of vision with 80–90% of patients demonstrating dry type AMD. Dry AMD could possibly be prevented by polyphenol-rich medicinal foods by the inhibition of N-retinylidene-N-retinylethanolamine (A2E)-induced oxidative stress and cell damage. Arctium lappa L. (AL) leaves are medicinal and have antioxidant activity. The purpose of this study was to elucidate the protective effects of the extract of AL leaves (ALE) on dry AMD models, including in vitro A2E-induced damage in ARPE-19 cells, a human retinal pigment epithelial cell line, and in vivo light-induced retinal damage in BALB/c mice. According to the total phenolic contents (TPCs), total flavonoid contents (TFCs) and antioxidant activities, ALE was rich in polyphenols and had antioxidant efficacies on 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and 2′,7′-dichlorofluorescin diacetate (DCFDA) assays. The effects of ALE on A2E accumulation and A2E-induced cell death were also monitored. Despite continued exposure to A2E (10 μM), ALE attenuated A2E accumulation in APRE-19 cells with levels similar to lutein. A2E-induced cell death at high concentration (25 μM) was also suppressed by ALE by inhibiting the apoptotic signaling pathway. Furthermore, ALE could protect the outer nuclear layer (ONL) in the retina from light-induced AMD in BALB/c mice. In conclusion, ALE could be considered a potentially valuable medicinal food for dry AMD.
Gold Clusters Attenuate Inflammation in Rat Mesangial Cells via Inhibiting the Activation of NF-κB Pathway
Authors: Yuan Jinling , Hou Kaixiao , Yao Yawen , Du Zhongying , Lu Cao , Yuan Qing , Gao Xueyun
Published: April 2020

Sepsis-induced acute kidney injury (AKI) with high incidence and mortality rates remains a great challenge in the clinic; thus, novel therapies need to be developed urgently. This complication is associated with an overwhelming systemic inflammatory response. The aim of this study was to evaluate the potential effects and possible mechanisms of gold clusters on septic AKI in vitro. Rat mesangial HBZY-1 cells were treated with peptide-templated gold clusters under lipopolysaccharide (LPS) stimulation. The LPS-induced expression of pro-inflammatory cytokines was measured, including tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β) and interleukin-6 (IL-6). Our data showed that the LPS-induced transcription and secretion of these cytokines were suppressed by pretreatment of gold clusters in a dose-dependent manner. Cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) also play key roles in septic AKI and both of them are induced upon LPS-stimulation in mesangial cells. Our results further showed that pretreatment with gold clusters dramatically inhibited the LPS-stimulated transcription and expression of COX2 and iNOS, and the subsequent prostaglandin E2 (PGE2) and nitric oxide (NO) production in HBZY-1 cells. Since these factors are involved in the NF-κB pathway upon LPS stimulation, the potential roles of gold clusters on the NF-κB pathway were further determined. We found that LPS-induced NF-κB activation was suppressed in gold clusters-pretreated HBZY-1 cells. These results demonstrated that gold clusters can attenuate LPS-induced inflammation in mesangial cells, probably via inhibiting the activation of the NF-κB pathway, suggesting a potential therapeutic approach for septic AKI.
Functional CdS-Au Nanocomposite for Efficient Photocatalytic, Photosensitizing, and Two-Photon Applications
Authors: Nawrot Katarzyna C. , Wawrzyńczyk Dominika , Bezkrovnyi Oleksii , Kępiński Leszek , Cichy Bartłomiej , Samoć Marek , Nyk Marcin
Published: April 2020

We demonstrate a low-temperature synthesis of hydrophilic, penicillamine-stabilized hybrid CdS-Au nanoparticles (NPs) utilizing different Au concentrations. The obtained hybrid nanomaterials exhibit photoluminescence quenching and emission lifetime reduction in comparison with their raw semiconductor CdS NPs counterparts. An increase of concentration of Au present at the surface of CdS leads to lower photoluminescence intensity and faster emission decays, suggesting more efficient charge separation when larger Au domains are present. For photocatalysis studies, we performed methylene blue (MB) absorption measurements under irradiation in the presence of CdS-Au NPs. After 1 h of light exposure, we observed the absorbance decrease to about 35% and 10% of the initial value for the CdS-5Au and CdS-7.5Au (the hybrid NPs obtained in a presence of 5.0 and 7.5 mM Au), respectively, which indicates MB reduction caused by electrons effectively separated from holes on metal surface. In further similar photocatalysis experiments, we measured bovine serum albumin (BSA) integrated photoluminescence intensity quenching in the presence of CdS-Au NPs, with a 50% decrease being obtained for CdS-2.5Au NPs and CdS-5Au NPs, with a faster response rate detected for the system prepared with a higher Au concentration. The results suggest hole-driven reactive oxygen species (ROS) production, causing BSA degeneration. Finally, we performed two-photon excited emission (TPEE) measurements for CdS-5Au NPs, obtaining their two-photon absorption (TPA) cross-section values up to 15.8 × 103 GM (Goeppert-Mayer units). We conclude that the obtained water-soluble CdS-Au NPs exhibit potential triple functionalities as photocatalysts for reduction and oxidation reactions as well as materials for two-photon absorption applications, so that they may be considered as future theranostics.
Neuroprotective Potential of Allium sativum against Monosodium Glutamate-Induced Excitotoxicity: Impact on Short-Term Memory, Gliosis, and Oxidative Stress
Authors: Hazzaa Suzan , Abdelaziz Seham , Abd Eldaim Mabrouk , Abdel-Daim Mohamed , Elgarawany Ghada
Published: April 2020

This study evaluated the neuroprotective potential of Allium sativum against monosodium glutamate (MSG)-induced neurotoxicity with respect to its impact on short-term memory in rats. Forty male Wistar albino rats were assigned into four groups. The control group received distilled water. The second group was administered Allium sativum powder (200 mg/kg of body weight) orally for 7 successive days, then was left without treatment until the 30th day. The third group was injected intraperitoneally with MSG (4 g/kg of body weight) for 7 successive days, then left without treatment until the 30th day. The fourth group was injected with MSG in the same manner as the third group and was treated with Allium sativum powder in the same manner as the second group, simultaneously. Phytochemical analysis of Allium sativum powder identified the presence of diallyl disulphide, carvone, diallyl trisulfide, and allyl tetrasulfide. MSG-induced excitotoxicity and cognitive deficit were represented by decreased distance moved and taking a long time to start moving from the center in the open field, as well as lack of curiosity in investigating the novel object and novel arm. Moreover, MSG altered hippocampus structure and increased MDA concentration and protein expression of glial fibrillary acidic protein (GFAP), calretinin, and caspase-3, whereas it decreased superoxide dismutase (SOD) activity and protein expression of Ki-67 in brain tissue. However, Allium sativum powder prevented MSG-induced neurotoxicity and improved short-term memory through enhancing antioxidant activity and reducing lipid peroxidation. In addition, it decreased protein expression of GFAP, calretinin, and caspase-3 and increased protein expression of Ki-67 in brain tissues and retained brain tissue architecture. This study indicated that Allium sativum powder ameliorated MSG-induced neurotoxicity through preventing oxidative stress-induced gliosis and apoptosis of brain tissue in rats.
The influence of Supreme Court of Cassation practice over legislation development in Bulgaria
Authors: Tsokeva Maria
Published: April 2020

The article discusses the influence of the Supreme Court of Cassation prac­tice over the Bulgarian legislation devel­opment. A subject of a detailed analysis is the jurisdiction of the Court, based on which the latter carries out its two main activities - judicial and interpretative. Further subject of analysis is the nature of judicial acts, laid down in this regard, as also their influence on our legislation from a theoretical point of view and via particular practice examples.
Case study: Automated recognition of wind farm sound using artificial neural networks
Authors: Iannace Gino , Trematerra Amelia , Ciaburro Giuseppe
Published: April 2020

Wind energy has been one of the most widely used forms of energy since ancient times, with it being a widespread type of clean energy, which is available in mechanical form and can be efficiently transformed into electricity. However, wind turbines can be associated with concerns around
noise pollution and visual impact. Modern turbines can generate more electrical power than older turbines even if they produce a comparable sound power level. Despite this, protests from citizens living in the vicinity of wind farms continue to be a problem for those institutions which issue
permits. In this article, acoustic measurements carried out inside a house were used to create a model based on artificial neural networks for the automatic recognition of the noise emitted by the operating conditions of a wind farm. The high accuracy of the models obtained suggests the adoption
of this tool for several applications. Some critical issues identified in a measurement session suggest the use of additional acoustic descriptors as well as specific control conditions.
Prevalence and incidence of type 1 diabetes in the world: a systematic review and meta-analysis
Authors: Mobasseri Majid , Shirmohammadi Masoud , Amiri Tarlan , Vahed Nafiseh , Hosseini Fard Hossein , Ghojazadeh Morteza
Published: April 2020

Background: Diabetes is referred to a group of diseases characterized by high glucose levels in blood. It is caused by a deficiency in the production or function of insulin or both, which can occur because of different reasons, resulting in protein and lipid metabolic disorders. The aim of this study was to systematically review the prevalence and incidence of type 1 diabetes in the world. Methods: A systematic search of resources was conducted to investigate the prevalence and incidence of type 1 diabetes in the world. The databases of Medline (via PubMed and Ovid),ProQuest, Scopus, and Web of Science from January 1980 to September 2019 were searched to locate English articles. The located articles were screened in multiple levels of title, abstract,and full-text and final studies that met the inclusion criteria were retrieved and included in the study. Results: From 1202 located articles, 193 studies were included in this systematic review. The results of meta-analysis showed that the incidence of type 1 diabetes was 15 per 100,000 people and the prevalence was 9.5% (95% CI: 0.07 to 0.12) in the world, which was statistically significant. Conclusion: According to the results, the incidence and prevalence of type 1 diabetes are increasing in the world. As a result, insulin will be difficult to access and afford, especially in underdeveloped and developing countries.