bluuebunny/crossref_metadata_2025 huggingface dataset:
Larvicidal Activities of 2-Aryl-2,3-Dihydroquinazolin -4-ones against Malaria Vector Anopheles arabiensis, In Silico ADMET Prediction and Molecular Target Investigation
Authors: Venugopala Katharigatta N. , Ramachandra Pushpalatha , Tratrat Christophe , Gleiser Raquel M. , Bhandary Subhrajyoti , Chopra Deepak , Morsy Mohamed A. , Aldhubiab Bandar E. , Attimarad Mahesh , Nair Anroop B. , Sreeharsha Nagaraja , Venugopala Rashmi , Deb Pran Kishore , Chandrashekharappa Sandeep , Khalil Hany Ezzat , Alwassil Osama I. , Abed Sara Nidal , Bataineh Yazan A. , Palenge Ramachandra , Haroun Michelyne , Pottathil Shinu , Girish Meravanige B. , Akrawi Sabah H. , Mohanlall Viresh
Published: March 2020

Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through the bites of infected Anopheles mosquitoes. Although insecticides are currently used to reduce malaria transmission, their safety concern for living systems, as well as the environment, is a growing problem. Therefore, the discovery of novel, less toxic, and environmentally safe molecules to effectively combat the control of these vectors is in high demand. In order to identify new potential larvicidal agents, a series of 2-aryl-1,2-dihydroquinazolin-4-one derivatives were synthesized and evaluated for their larvicidal activity against Anopheles arabiensis. The in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the compounds were also investigated and most of the derivatives possessed a favorable ADMET profile. Computational modeling studies of the title compounds demonstrated a favorable binding interaction against the acetylcholinesterase enzyme molecular target. Thus, 2-aryl-1,2-dihydroquinazolin-4-ones were identified as a novel class of Anopheles arabiensis insecticides which can be used as lead molecules for the further development of more potent and safer larvicidal agents for treating malaria.
Various Strategies in Post-Polymerization Functionalization of Organic Polymer-Based Monoliths Used in Liquid Phase Separation Techniques
Authors: Alharthi Sarah , El Rassi Ziad
Published: March 2020

This review article is aimed at summarizing the various strategies that have been developed so far for post-polymerization functionalization (PPF) of organic polymer-based monoliths used in liquid phase separation techniques, namely HPLC at all scales and capillary electrochromatography (CEC). The reader will find the organic reactions performed on monolithic columns for grafting the chromatographic ligands needed for solving the separation problems on hand. This process involves therefore the fabrication of template monoliths that carry reactive functional groups to which chromatographic ligands can be covalently attached in a post-polymerization kind of approach. That is, the template monolith that has been optimized in terms of pore structure and other morphology can be readily modified and tailor made on column to fit a particular separation. The review article will not only cover the various strategies developed so far but also describe their separation applications. To the best of our knowledge, this review article will be the first of its kind.
Pharmacological Update Properties of Aloe Vera and its Major Active Constituents
Authors: Sánchez Marta , González-Burgos Elena , Iglesias Irene , Gómez-Serranillos M. Pilar
Published: March 2020

Aloe vera has been traditionally used to treat skin injuries (burns, cuts, insect bites, and eczemas) and digestive problems because its anti-inflammatory, antimicrobial, and wound healing properties. Research on this medicinal plant has been aimed at validating traditional uses and deepening the mechanism of action, identifying the compounds responsible for these activities. The most investigated active compounds are aloe-emodin, aloin, aloesin, emodin, and acemannan. Likewise, new actions have been investigated for Aloe vera and its active compounds. This review provides an overview of current pharmacological studies (in vitro, in vivo, and clinical trials), written in English during the last six years (2014–2019). In particular, new pharmacological data research has shown that most studies refer to anti-cancer action, skin and digestive protective activity, and antimicrobial properties. Most recent works are in vitro and in vivo. Clinical trials have been conducted just with Aloe vera, but not with isolated compounds; therefore, it would be interesting to study the clinical effect of relevant metabolites in different human conditions and pathologies. The promising results of these studies in basic research encourage a greater number of clinical trials to test the clinical application of Aloe vera and its main compounds, particularly on bone protection, cancer, and diabetes.
Design, Synthesis and Biological Evaluation of New Antioxidant and Neuroprotective Multitarget Directed Ligands Able to Block Calcium Channels
Authors: Pachòn Angona Irene , Daniel Solene , Martin Helene , Bonet Alexandre , Wnorowski Artur , Maj Maciej , Jóźwiak Krzysztof , Silva Tiago Barros , Refouvelet Bernard , Borges Fernanda , Marco-Contelles José , Ismaili Lhassane
Published: March 2020

We report herein the design, synthesis and biological evaluation of new antioxidant and neuroprotective multitarget directed ligands (MTDLs) able to block Ca2+ channels. New dialkyl 2,6-dimethyl-4-(4-(prop-2-yn-1-yloxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate MTDLs 3a–t, resulting from the juxtaposition of nimodipine, a Ca2+ channel antagonist, and rasagiline, a known MAO inhibitor, have been obtained from appropriate and commercially available precursors using a Hantzsch reaction. Pertinent biological analysis has prompted us to identify the MTDL 3,5-dimethyl-2,6–dimethyl–4-[4-(prop–2–yn–1-yloxy)phenyl]-1,4-dihydro- pyridine- 3,5-dicarboxylate (3a), as an attractive antioxidant (1.75 TE), Ca2+ channel antagonist (46.95% at 10 μM), showing significant neuroprotection (38%) against H2O2 at 10 μM, being considered thus a hit-compound for further investigation in our search for anti-Alzheimer’s disease agents.
Synthesis of Samarium OxysulfateSm2O2SO4 in the High-Temperature Oxidation Reaction and Its Structural, Thermal and Luminescent Properties
Authors: Denisenko Yu. G. , Sal’nikova E. I. , Basova S. A. , Molokeev M. S. , Krylov A. S. , Aleksandrovsky A. S. , Oreshonkov A. S. , Atuchin V. V. , Volkova S. S. , Khritokhin N. A. , Andreev O. V.
Published: March 2020

The oxidation process of samariumoxysulfide was studied in the temperature range of 500–1000 °C. Our DTA investigation allowed for establishing the main thermodynamic (∆Hºexp = −654.6 kJ/mol) and kinetic characteristics of the process (Ea = 244 kJ/mol, A = 2 × 1010). The enthalpy value of samarium oxysulfate (ΔHºf (Sm2O2SO4(monocl)) = −2294.0 kJ/mol) formation was calculated. The calculated process enthalpy value coincides with the value determined in the experiment. It was established that samarium oxysulfate crystallizes in the monoclinic symmetry class and its crystal structure belongs to space group C2/c with unit cell parameters a = 13.7442 (2), b = 4.20178 (4) and c = 8.16711 (8)Å, β = 107.224 (1)°, V = 450.498 (9)Å3, Z = 4. The main elements of the crystalline structure are obtained and the cation coordination environment is analyzed in detail. Vibrational spectroscopy methods confirmed the structural model adequacy. The Sm2O2SO4luminescence spectra exhibit three main bands easily assignable to the transitions from 4G5/2 state to 6H5/2, 6H7/2, and 6H9/2 multiplets.
Anticatabolic and Anti-Inflammatory Effects of Myricetin 3-O-β-d-Galactopyranoside in UVA-Irradiated Dermal Cells via Repression of MAPK/AP-1 and Activation of TGFβ/Smad
Authors: Oh Jung Hwan , Karadeniz Fatih , Lee Jung Im , Park So Young , Seo Youngwan , Kong Chang-Suk
Published: March 2020

UV irradiation is one of the main causes of extrinsic skin aging. UV-mediated skin aging, also known as photoaging, causes excessive breakdown of extracellular matrix which leads skin to lose its elasticity and strength. Several phytochemicals are known to exert anti-photoaging effects via different mechanisms, partly due to their antioxidant properties. The current study has been carried out to determine the potential anti-photoaging properties of myricetin 3-O-β-d-galacto-pyranoside (M3G), a flavonol glycoside isolated from L. tetragonum, in UVA-irradiated in vitro models; HaCaT keratinocytes and human dermal fibroblasts (HDFs). UVA-induced changes in MMP-1 and collagen production have been observed in HaCaT keratinocytes and HDFs. Further, UVA-induced activation of MAPK signaling, and pro-inflammatory cytokine production have been investigated. TGFβ/Smad pathway has also been analyzed in UVA-irradiated HDFs. Treatment with M3G reversed the UVA-induced changes in MMP-1 and collagen production both in HaCaT keratinocytes and HDFs. UVA-mediated activation of p38, ERK and JNK MAPK activation was also inhibited by M3G treatment in HaCaT keratinocytes. In HDFs, M3G was able to upregulate the TGFβ/Smad pathway activation. In addition, M3G downregulated the UVA-induced pro-inflammatory cytokines in keratinocytes and HDFs. It has been suggested that the M3G has exerted potential antiphotoaging properties in vitro, by attenuating UVA-induced changes in MMP-1 and collagen production in keratinocytes and dermal fibroblasts.
Effects of Inclusion of Fresh Forage in the Diet for Lactating Buffaloes on Volatile Organic Compounds of Milk and Mozzarella Cheese
Authors: Sacchi Raffaele , Marrazzo Andrea , Masucci Felicia , Di Francia Antonio , Serrapica Francesco , Genovese Alessandro
Published: March 2020

This paper aimed to assess the effects of feeding fresh forage on volatile organic compounds (VOCs) of buffalo milk and mozzarella cheese. Sixteen lactating buffaloes were equally allotted into two groups fed diets containing (experimental (Exp) group) or not (control (Ctl) group) 20 kg/d of fresh sorghum. Milk from the groups was separately collected and transformed in the traditional ‘Mozzarella di Bufala Campana’ Protected Denomination of Origin (PDO). Three batches of mozzarella were produced for each diet and they were analyzed, along with the two bulks of milk, for VOC composition, by using solid phase micro-extraction (SPME) coupled with gas-chromatography/mass spectrometry (GC/MS). The use of fresh forage increased the levels of long chain fatty acids along with the contents of aldehydes, and this could be responsible for an increase in green notes of milk. The use of the Ctl diet, containing a higher proportion of silage, increased the ketones, acids, and esters, which are compounds that could raise the cheese and fruity notes of milk. The mozzarella was less affected by the dietary treatment than milk. The use of fresh forage (sorghum) enhanced the green notes of milk and induced a few changes in the VOC profile of the typical PDO Mozzarella di Bufala Campana cheese, that were nonetheless detectable by sensory analysis. The low level found for butanoic acid, 2,3-pentanedione, and propyl acetate in mozzarella cheese obtained with fresh forage diet can lead to perceive less the olfactory notes of cheese, cream, and fruit.
Polyphenols from Salix tetrasperma Impair Virulence and Inhibit Quorum Sensing of Pseudomonas aeruginosa
Authors: Mostafa Islam , Abbas Hisham A. , Ashour Mohamed L. , Yasri Abdelaziz , El-Shazly Assem M. , Wink Michael , Sobeh Mansour
Published: March 2020

Bacterial resistance represents one of the emerging obstacles in plants, animals, and humans that impairs treatment with antibacterial agents. Targeting of the bacterial quorum sensing system is one of the strategies to overcome this problem. Recently, research has been focused on natural and food components which can function as quorum sensing inhibitors. In this study, a methanol extract from Salix tetrasperma stem bark was phytochemically profiled by LC-MS analysis. This resulted in the identification of 38 secondary metabolites with (epi)catechin-(epi)catechin, epicatechin, tremulacin, salicortin, and trichocarposide as the major constituents. The extracts of both stem bark and the previously profiled flower of S. tetrasperma were tested for anti-quorum sensing activity in a common and widely distributed pathogen Pseudomonas aeruginosa. The natural products inhibited swimming and swarming motilities, as well as proteolytic and hemolytic activities in a dose-dependent manner. Molecular docking of the constituents from both extracts against the quorum sensing controlling systems Lasl/LasR, rhll/rhlR, and PQS/MvfR showed that epicatechin, (epi)catechin-(epi)catechin, p-hydroxy benzoyl galloyl glucose, p-hydroxy benzoyl protocatechuic acid glucose, and caffeoylmalic acid could be the main active components. This study supports the importance of secondary metabolites, especially polyphenols, as quorum sensing inhibitors.
Improving Dissolution and Cytotoxicity by Forming Multidrug Crystals
Authors: Bian Xufei , Jiang Lan , Zhou Jing , Guan Xiaoshu , Wang Jingyu , Xiang Peng , Pan Junyi , Hu Xiangnan
Published: March 2020

Both rosiglitazone and metformin have effects on blood glucose regulation and the proliferation of liver cancer cells. Combination therapy with these two drugs is common and effective for the treatment of diabetes in the clinic, however, the application of these two drugs is influenced by the poor dissolution of rosiglitazone and the gastrointestinal side-effect of metformin resulting from a high solubility. The formation of a multidrug crystal form (Rsg-Met) by a solvent evaporation method can solve the solubility issue. Crystal structure data and intramolecular hydrogen bonds were detected by X-ray diffraction and infrared spectroscopy. Surprisingly, Rsg-Met shortens the time spent in solubility equilibrium and multiplies the dissolution rate of Rsg. Finally, we found that a low concentration of Rsg-Met enhanced the proliferation inhibition effect on liver cancer cells (HepG2, SK-hep1) compared with rosiglitazone, without affecting the human normal cell line LO2.
The Evolution of Pleconaril: Modified O-Alkyl Linker Analogs Have Biological Activity towards Coxsackievirus B3 Nancy
Authors: Volobueva Alexandrina , Egorova Anna , Galochkina Anastasia , Ekins Sean , Zarubaev Vladimir , Makarov Vadim
Published: March 2020

Coxsackieviruses type B are one of the most common causes of mild upper respiratory and gastrointestinal illnesses. At the time of writing, there are no approved drugs for effective antiviral treatment for Coxsackieviruses type B. We used the core-structure of pleconaril, a well-known antienteroviral drug candidate, for the synthesis of novel compounds with O-propyl linker modifications. Some original compounds with 4 different linker patterns, such as sulfur atom, ester, amide, and piperazine, were synthesized according to five synthetic schemes. The cytotoxicity and bioactivity of 14 target compounds towards Coxsackievirus B3 Nancy were examined. Based on the results, the values of 50% cytotoxic dose (CC50), 50% virus-inhibiting dose (IC50), and selectivity index (SI) were calculated for each compound. Several of the novel synthesized derivatives exhibited a strong anti-CVB3 activity (SI > 20 to > 200). These results open up new possibilities for synthesis of further new selective anticoxsackievirus compounds.
Electrical and Optical Properties of Silicon Oxide Lignin Polylactide (SiO2-L-PLA)
Authors: Fal Jacek , Bulanda Katarzyna , Traciak Julian , Sobczak Jolanta , Kuzioła Rafał , Grąz Katarzyna Maria , Budzik Grzegorz , Oleksy Mariusz , Żyła Gaweł
Published: March 2020

This paper presents a study on the electrical properties of new polylactide-based nanocomposites with the addition of silicon-dioxide–lignin nanoparticles and glycerine as a plasticizer. Four samples were prepared with nanoparticle mass fractions ranging between 0.01 to 0.15 (0.01, 0.05, 0.10, and 0.15), and three samples were prepared without nanoparticle filler—unfilled and unprocessed polylactide, unfilled and processed polylactide, and polylactide with Fusabond and glycerine. All samples were manufactured using the melt mixing extrusion technique and injection molding. Only the unfilled and unprocessed PLA sample was directly prepared by injection molding. Dielectric properties were studied with broadband spectroscopy in a frequency range from 0.1 Hz to 1 MHz in 55 steps designed on a logarithmic scale and a temperature range from 293.15 to 333.15 K with a 5 K step. Optical properties of nanocomposites were measured with UV-VIS spectroscopy at wavelengths from 190 to 1100 nm. The experimental data show that the addition of silicon-dioxide–lignin and glycerine significantly affected the electrical properties of the studied nanocomposites based on polylactide. Permittivity and electrical conductivity show a significant increase with an increasing concentration of nanoparticle filler. The optical properties are also affected by nanofiller and cause an increase in absorbance as the number of silicon-dioxide–lignin nanoparticles increase.
Engineered ZnO and CuO Nanoparticles Ameliorate Morphological and Biochemical Response in Tissue Culture Regenerants of Candyleaf (Stevia rebaudiana)
Authors: Ahmad Muhammad Arslan , Javed Rabia , Adeel Muhammad , Rizwan Muhammad , Ao Qiang , Yang Yuesuo
Published: March 2020

Sustainable production of secondary metabolites in medicinal plants by artificial culturing on the industrial scale has gained worldwide importance. Engineered nanoparticles (ENPs) play a pivotal role in the elicitation of compounds of medicinal value. This investigation explores the influence of ZnO and CuO ENPs on in vitro roots formation, non-enzymatic antioxidant activities, and production of steviol glycosides (SGs) in regenerants of Candyleaf, Stevia rebaudiana. ENPs were applied in 0, 2, 20, 200, and 2000 mg/L of concentration in the MS medium containing plant shoots. The percentage of rooting induced was 91% and 94% by applying ZnO ENPs (2 mg/L) and CuO ENPs (20 mg/L), respectively. Moreover, at 2 mg/L of ZnO and 20 mg/L of CuO ENPs, the high performance liquid chromatography studies determined the significantly greatest content of SGs; rebaudioside A (4.42 and 4.44) and stevioside (1.28 and 1.96). Phytochemical studies including total flavonoid content, total phenolic content, and 2,2-diphenyl-1-picryl hydrazyl-free radical scavenging activity were calculated highest by the regenerants grown in 2 mg/L of ZnO and 20 mg/L of CuO ENPs dosage. Both ZnO and CuO ENPs at 200 mg/L and 2000 mg/L of concentration induced adverse effects on plant biomass, antioxidant activities, and SGs content up to 1.22 and 1.77 for rebaudioside A and 0.21 and 0.25 for stevioside. Hence, the biochemical and morphophysiological responses of Candyleaf were elicited as a defense against ZnO and CuO ENPs applied under threshold limit. This artificial biotechnological technique holds great promise for continued production of natural antioxidants on commercial scale and our study has further strengthened this impact.
Effect of Coffee Cascara Dietary Fiber on the Physicochemical, Nutritional and Sensory Properties of a Gluten-Free Bread Formulation
Authors: Rios Maria Belen , Iriondo-DeHond Amaia , Iriondo-DeHond Maite , Herrera Teresa , Velasco Diego , Gómez-Alonso Sergio , Callejo María Jesús , del Castillo Maria Dolores
Published: March 2020

This study aimed to assess the physicochemical, nutritional and sensory properties of gluten-free breads containing isolated coffee cascara dietary fiber (ICCDF) as a food ingredient. ICCDF was obtained by aqueous extraction. The oil and water holding capacity and the nutritional profile of the novel ingredient were determined. Its safety was certificated by analysis of ochratoxin A, caffeine and gluten. Gluten-free bread formulations were prepared enriching a commercial bakery premix in rice protein (8%) and ICCDF (3% and 4.5%). Nutritional profile of the novel gluten-free breads (dietary fiber, protein, amino acids, lipids, fatty acid profile and resistant starch), as well as bread volume, crumb density, moisture, firmness, elasticity and color intensity were determined. A sensory quantitative descriptive analysis of the breads was conducted using eight trained panelists. New breads showed significantly higher (p < 0.05) content of dietary fiber and protein than the control bread. The addition of ICCDF allowed increasing dough yield, a less crumb firmness and a higher crumb elasticity. The nutrition claims “source of protein and high in dietary fiber” were assigned to the new formulations. In conclusion, a certificated gluten-free bread with improved nutritional and physicochemical properties and good sensorial profile was obtained.
Antibacterial and Antioxidant Activity of Extracts from Rose Fruits (Rosa rugosa)
Authors: Cendrowski Andrzej , Kraśniewska Karolina , Przybył Jarosław L. , Zielińska Agnieszka , Kalisz Stanisław
Published: March 2020

The aim of the present study was to determine the antioxidant and antimicrobial properties in freeze-dried extracts of rose fruits (Rosa rugosa) obtained using various extraction techniques and to determine the effect of a selected extract on bacterial survival in model fluids imitating protein food. Ethanolic extracts from rose fruits showed higher antioxidant activity compared to other tested extracts. The rose fruits aqueous extract showed the highest inhibitory activity against most of the 10 bacterial strains tested. From the group of Gram-positive bacteria, the Bacillus cereus strain proved to be the most sensitive to the action of the rose extract. From the Gram-negative bacteria: Escherichia coli and Klebsiella pneumoniae were the most sensitive. The reduction in the number of bacterial cells in matrices imitating protein food depended on the concentration of the aqueous extract used. However, at none of the concentrations used was a complete inhibition of bacterial growth observed. We have confirmed that the traditional extraction and freeze-drying of rose fruits is still suitable for the food industry due to obtaining extracts with good antibacterial and antioxidant properties and the use of bio-solvents, such as water or ethanol, which are easily available in high purity and completely biodegradable.
Steady-State Kinetics of Enzyme-Catalyzed Hydrolysis of Echothiophate, a P–S Bonded Organophosphorus as Monitored by Spectrofluorimetry
Authors: Zueva Irina V. , Lushchekina Sofya V. , Daudé David , Chabrière Eric , Masson Patrick
Published: March 2020

Enzyme-catalyzed hydrolysis of echothiophate, a P–S bonded organophosphorus (OP) model, was spectrofluorimetrically monitored, using Calbiochem Probe IV as the thiol reagent. OP hydrolases were: the G117H mutant of human butyrylcholinesterase capable of hydrolyzing OPs, and a multiple mutant of Brevundimonas diminuta phosphotriesterase, GG1, designed to hydrolyze a large spectrum of OPs at high rate, including V agents. Molecular modeling of interaction between Probe IV and OP hydrolases (G117H butyrylcholinesterase, GG1, wild types of Brevundimonas diminuta and Sulfolobus solfataricus phosphotriesterases, and human paraoxonase-1) was performed. The high sensitivity of the method allowed steady-state kinetic analysis of echothiophate hydrolysis by highly purified G117H butyrylcholinesterase concentration as low as 0.85 nM. Hydrolysis was michaelian with Km = 0.20 ± 0.03 mM and kcat = 5.4 ± 1.6 min−1. The GG1 phosphotriesterase hydrolyzed echothiophate with a high efficiency (Km = 2.6 ± 0.2 mM; kcat = 53400 min−1). With a kcat/Km = (2.6 ± 1.6) × 107 M−1min−1, GG1 fulfills the required condition of potential catalytic bioscavengers. quantum mechanics/molecular mechanics (QM/MM) and molecular docking indicate that Probe IV does not interact significantly with the selected phosphotriesterases. Moreover, results on G117H mutant show that Probe IV does not inhibit butyrylcholinesterase. Therefore, Probe IV can be recommended for monitoring hydrolysis of P–S bonded OPs by thiol-free OP hydrolases.
Effect of Terpenoids and Flavonoids Isolated from Baccharis conferta Kunth on TPA-Induced Ear Edema in Mice
Authors: Ana Silvia Gutiérrez-Román , Gabriela Trejo-Tapia , Maribel Herrera-Ruiz , Nayeli Monterrosas-Brisson , José Luis Trejo-Espino , Alejandro Zamilpa , Manasés González-Cortazar
Published: March 2020

In this study, we isolated from the aerial parts of Baccharis conferta Kunth (i) a new neoclerodane, denominated “bacchofertone”; (ii) four known terpenes: schensianol A, bacchofertin, kingidiol and oleanolic acid; and (iii) two flavonoids: cirsimaritin and hispidulin. All structures were identified by an exhaustive analysis of nuclear magnetic resonance (NMR) and mass spectroscopy (MS). Extracts from aerial parts were screened for anti-inflammatory activity in the mice ear edema model of 12-O-tetradecanoylforbol-13-acetate mice. Dichloromethane extract (BcD) exhibited 78.5 ± 0.72% inhibition of edema, followed by the BcD2 and BcD3 fractions of 71.4% and 82.9% respectively, at a dose of 1 mg/ear. Kingidiol and cirsimaritin were the most potent compounds identified, with a median effective dose of 0.12 and 0.16 mg/ear, respectively. A histological analysis showed that the topical application of TPA promoted intense cell infiltration, and this inflammatory parameter was reduced with the topical application of isolated compounds.
State-of-the-Art Production Chains for Peas, Beans and Chickpeas—Valorization of Agro-Industrial Residues and Applications of Derived Extracts
Authors: Tassoni Annalisa , Tedeschi Tullia , Zurlini Chiara , Cigognini Ilaria Maria , Petrusan Janos-Istvan , Rodríguez Óscar , Neri Simona , Celli Annamaria , Sisti Laura , Cinelli Patrizia , Signori Francesca , Tsatsos Georgios , Bondi Marika , Verstringe Stefanie , Bruggerman Geert , Corvini Philippe F. X.
Published: March 2020

The world is confronted with the depletion of natural resources due to their unsustainable use and the increasing size of populations. In this context, the efficient use of by-products, residues and wastes generated from agro-industrial and food processing opens the perspective for a wide range of benefits. In particular, legume residues are produced yearly in very large amounts and may represent an interesting source of plant proteins that contribute to satisfying the steadily increasing global protein demand. Innovative biorefinery extraction cascades may also enable the recovery of further bioactive molecules and fibers from these insufficiently tapped biomass streams. This review article gives a summary of the potential for the valorization of legume residual streams resulting from agro-industrial processing and more particularly for pea, green bean and chickpea by-products/wastes. Valuable information on the annual production volumes, geographical origin and state-of-the-art technologies for the extraction of proteins, fibers and other bioactive molecules from this source of biomass, is exhaustively listed and discussed. Finally, promising applications, already using the recovered fractions from pea, bean and chickpea residues for the formulation of feed, food, cosmetic and packaging products, are listed and discussed.
Protective Effect of Astaxanthin on Ochratoxin A-Induced Kidney Injury to Mice by Regulating Oxidative Stress-Related NRF2/KEAP1 Pathway
Authors: Li Lin , Chen Yueli , Jiao Danyang , Yang Shuhua , Li Lin , Li Peng
Published: March 2020

The present study aimed to investigate the effects of astaxanthin (ASX) on ochratoxin A (OTA)-induced renal oxidative stress and its mechanism of action. Serum kidney markers, histomorphology, ultrastructural observation, and oxidative stress indicators were assessed. Meanwhile, quantitative real-time reverse transcription PCR and western blotting detection of NRF2 (encoding nuclear factor, erythroid 2 like) and members of the NRF2/KEAP1 signaling pathway (KEAP1 (encoding Kelch-like ECH-associated protein), NQO1 (encoding NAD(P)H quinone dehydrogenase), HO-1 (encoding heme oxygenase 1), γ-GCS (gamma-glutamylcysteine synthetase), and GSH-Px (glutathione peroxidase 1)) were performed. Compared with the control group, the OTA-treated group showed significantly increased levels of serum UA (uric acid) and BUN (blood urea nitrogen), tubular epithelial cells were swollen and degenerated, and the levels of antioxidant enzymes decreased significantly, and the expression of NRF2 (cytoplasm), NQO1, HO-1, γ-GCS, and GSH-Px decreased significantly. More importantly, after ASX pretreatment, compared with the OTA group, serum markers were decreased, epithelial cells appeared normal; the expression of antioxidant enzymes increased significantly, NQO1, HO-1, γ-GCS and GSH-Px levels increased significantly, and ASX promoted the transfer of NRF2 from the cytoplasm to the nucleus. These results highlight the protective ability of ASX in renal injury caused by OTA exposure, and provide theoretical support for ASX’s role in other mycotoxin-induced damage.
Synthesis and Antimicrobial Properties of a Ciprofloxacin and PAMAM-dendrimer Conjugate
Authors: Svenningsen Søren Wedel , Frederiksen Rikki Franklin , Counil Claire , Ficker Mario , Leisner Jørgen J. , Christensen Jørn Bolstad
Published: March 2020

Infections caused by bacteria resistant to antibiotics are an increasing problem. Multivalent antibiotics could be a solution. In the present study, a covalent conjugate between Ciprofloxacin and a G0-PAMAM dendrimer has been synthesized and tested against clinically relevant Gram-positive and Gram-negative bacteria. The conjugate has antimicrobial activity and there is a positive dendritic effect compared to Ciprofloxacin itself.
Influence of a Commercial Biological Fungicide containing Trichoderma harzianum Rifai T-22 on Dissipation Kinetics and Degradation of Five Herbicides in Two Types of Soil
Authors: Szpyrka Ewa , Podbielska Magdalena , Zwolak Aneta , Piechowicz Bartosz , Siebielec Grzegorz , Słowik-Borowiec Magdalena
Published: March 2020

Biological crop protection is recommended to be applied alternately or together with chemical one, to protect human health from the excessive use of toxic pesticides. Presence of microorganisms can influence the concentration of chemical pollutants in soil. The aim of this study is to estimate the influence of a commercial biological fungicide containing Trichoderma harzianum Rifai T-22 on dissipation kinetics and degradation of five herbicides belonging to different chemical classes: clomazone, fluazifop-P-butyl, metribuzin, pendimethalin, and propyzamide, in two types of soil. Results of the study revealed that T. harzianum T-22 influences pesticide degradation and dissipation kinetics of the non-persistent herbicides: clomazone, fluazifop-P-butyl, and metribuzin. In soil with a higher content of nitrogen, phosphorus, and organic matter, degradation increased by up to 24.2%, 24.8%, and 23.5% for clomazone, fluazifop-P-butyl, and metribuzin, respectively. In soil with lower organic content, degradation was on a low level, of 16.1%, 17.7%, and 16.3% for clomazone, fluazifop-P-butyl, and metribuzin, respectively. In our study, the addition of the biological preparation shortened herbicide dissipation half-lives, from 0.3 days (2.9%) for fluazifop-P-butyl, to 18.4 days (25.1%) for clomazone. During the degradation study, no significant differences were noticed for pendimethalin, belonging to persistent substances. Biological protection of crops can modify pesticide concentrations and dissipation rates. On one hand, this may result in the reduced effectiveness of herbicide treatments, while on the other, it can become a tool for achieving cleaner environment.
Cerebrosides and Steroids from the Edible Mushroom Meripilus giganteus with Antioxidant Potential
Authors: Sárközy András , Béni Zoltán , Dékány Miklós , Zomborszki Zoltán Péter , Rudolf Kinga , Papp Viktor , Hohmann Judit , Ványolós Attila
Published: March 2020

The detailed chemical analysis of the methanol extract of Meripilus giganteus (Pers.) P. Karst. led to the isolation of two new cerebrosides, mericeramides A (1) and B (2) together with cerebroside B (3), ergosterol (4), 3β-hydroxyergosta-7,22-diene (5), cerevisterol (6), 3β-hydroxyergosta-6,8(14),22-triene (7), 3β-O-glucopyranosyl-5,8-epidioxyergosta-6,22-diene (8) and (11E,13E)-9,10-dihydroxy-11,13-octadecadienoic acid (9). The structures of the compounds were determined on the basis of NMR and MS spectroscopic analysis. Mericeramide A (1) is the first representative of halogenated natural cerebrosides. The isolated fungal metabolites 1–9 were evaluated for their antioxidant activity using the oxygen radical absorbance capacity (ORAC) assay. Compounds 2, 5 and 9 proved to possess considerable antioxidant effects, with 2.50 ± 0.29, 4.94 ± 0.37 and 4.27 ± 0.05 mmol TE/g values, respectively. The result obtained gives a notable addition to the chemical and bioactivity profile of M. giganteus, highlighting the possible contribution of this species to a versatile and balanced diet.
Mass Spectrometry Advances and Perspectives for the Characterization of Emerging Adoptive Cell Therapies
Authors: Lombard-Banek Camille , Schiel John E.
Published: March 2020

Adoptive cell therapy is an emerging anti-cancer modality, whereby the patient’s own immune cells are engineered to express T-cell receptor (TCR) or chimeric antigen receptor (CAR). CAR-T cell therapies have advanced the furthest, with recent approvals of two treatments by the Food and Drug Administration of Kymriah (trisagenlecleucel) and Yescarta (axicabtagene ciloleucel). Recent developments in proteomic analysis by mass spectrometry (MS) make this technology uniquely suited to enable the comprehensive identification and quantification of the relevant biochemical architecture of CAR-T cell therapies and fulfill current unmet needs for CAR-T product knowledge. These advances include improved sample preparation methods, enhanced separation technologies, and extension of MS-based proteomic to single cells. Innovative technologies such as proteomic analysis of raw material quality attributes (MQA) and final product quality attributes (PQA) may provide insights that could ultimately fuel development strategies and lead to broad implementation.
Highly Bioavailable Forms of Curcumin and Promising Avenues for Curcumin-Based Research and Application: A Review
Authors: Stohs Sidney J. , Chen Oliver , Ray Sidhartha D. , Ji Jin , Bucci Luke R. , Preuss Harry G.
Published: March 2020

Curcumin exerts a wide range of beneficial physiological and pharmacological activities, including antioxidant, anti-amyloid, anti-inflammatory, anti-microbial, anti-neoplastic, immune-modulating, metabolism regulating, anti-depressant, neuroprotective and tissue protective effects. However, its poor solubility and poor absorption in the free form in the gastrointestinal tract and its rapid biotransformation to inactive metabolites greatly limit its utility as a health-promoting agent and dietary supplement. Recent advances in micro- and nano-formulations of curcumin with greatly enhanced absorption resulting in desirable blood levels of the active forms of curcumin now make it possible to address a wide range of potential applications, including pain management, and as tissue protective. Using these forms of highly bioavailable curcumin now enable a broad spectrum of appropriate studies to be conducted. This review discusses the formulations designed to enhance bioavailability, metabolism of curcumin, relationships between solubility and particle size relative to bioavailability, human pharmacokinetic studies involving formulated curcumin products, the widely used but inappropriate practice of hydrolyzing plasma samples for quantification of blood curcumin, current applications of curcumin and its metabolites and promising directions for health maintenance and applications.
Briarenols I—K, New Anti-inflammatory 8,17-Epoxybriaranes from the Octocoral Briareum excavatum (Briareidae)
Authors: Huynh Thanh-Hao , Fang Lee-Shing , Chen Yu-Hsin , Peng Bo-Rong , Chen You-Ying , Zheng Li-Guo , Wu Yu-Jen , Wen Zhi-Hong , Chen Jih-Jung , Lin Tzu-Chi , Sung Ping-Jyun
Published: March 2020

Five 8,17-epoxybriaranes, including three new compounds—briarenols I–K (1–3), along with two known analogues, briaexcavatolide P (4) and briaexcavatin P (5), were isolated from the octocoral Briareum excavatum. The structures of briaranes 1–3 were elucidated by spectroscopic methods, including 1D and 2D NMR studies and (+)-HRESIMS. Briarane 4 exerted inhibition effects on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) release from RAW 264.7.
Phosphine Oxides as Spectroscopic Halogen Bond Descriptors: IR and NMR Correlations with Interatomic Distances and Complexation Energy
Authors: Ostras’ Alexei S. , Ivanov Daniil M. , Novikov Alexander S. , Tolstoy Peter M.
Published: March 2020

An extensive series of 128 halogen-bonded complexes formed by trimethylphosphine oxide and various F-, Cl-, Br-, I- and At-containing molecules, ranging in energy from 0 to 124 kJ/mol, is studied by DFT calculations in vacuum. The results reveal correlations between R–X⋅⋅⋅O=PMe3 halogen bond energy ΔE, X⋅⋅⋅O distance r, halogen’s σ-hole size, QTAIM parameters at halogen bond critical point and changes of spectroscopic parameters of phosphine oxide upon complexation, such as 31P NMR chemical shift, ΔδP, and P=O stretching frequency, Δν. Some of the correlations are halogen-specific, i.e., different for F, Cl, Br, I and At, such as ΔE(r), while others are general, i.e., fulfilled for the whole set of complexes at once, such as ΔE(ΔδP). The proposed correlations could be used to estimate the halogen bond properties in disordered media (liquids, solutions, polymers, glasses) from the corresponding NMR and IR spectra.
Antiviral Effects of Novel 2-Benzoxyl-Phenylpyridine Derivatives
Authors: Wei Yanhong , Wang Haijie , Xi Caili , Li Ni , Li Dong , Yao Chenguang , Sun Ge , Ge Hongmei , Hu Kanghong , Zhang Qian
Published: March 2020

Coxsackievirus B3 (CVB3) is the most common cause of acute and chronic viral myocarditis, primarily in children, while human adenovirus infections represent a significant cause of morbidity and mortality worldwide, in people of all ages. A series of novel 2-benzoxyl-phenylpyridine derivatives were evaluated for their potential antiviral activities against CVB3 and adenovirus type 7 (ADV7). Preliminary assays indicated that some of these compounds exhibited excellent antiviral effects on both CVB3 and ADV7 viruses; they could effectively inhibit virus-induced cytopathic effects, reduce viral progeny yields, and had similar or superior antiviral activities compared with the control drug, ribavirin. Further, these compounds targeted the early stages of CVB3 replication in cells, including viral RNA replication and protein synthesis, rather than inactivating the virus directly, inhibiting virus adsorption/entry, or affecting viral release from cells. Our data demonstrate that the tested 2-benzoxyl-phenylpyridine derivatives are effective inhibitors of CVB3 and ADV7, raising the possibility that these compounds might be feasible candidates for anti-viral agents.
Enhanced Antibacterial Property of Sulfate-Doped Ag3PO4 Nanoparticles Supported on PAN Electrospun Nanofibers
Authors: Panthi Gopal , Hassan Md. Mehedi , Kuk Yun-Su , Kim Ji Yeon , Chung Hea-Jong , Hong Seong-Tshool , Park Mira
Published: March 2020

Heterojunction nanofibers of PAN decorated with sulfate doped Ag3PO4 nanoparticles (SO42−-Ag3PO4/PAN electrospun nanofibers) were successfully fabricated by combining simple and versatile electrospinning technique with ion exchange reaction. The novel material possessing good flexibility could exhibit superior antibacterial property over sulfate undoped species (Ag3PO4/PAN electrospun nanofibers). FESEM, XRD, FTIR, XPS and DRS were applied to characterize the morphology, phase structure, bonding configuration, elemental composition, and optical properties of the as fabricated samples. FESEM characterization confirmed the successful incorporation of SO42−-Ag3PO4 nanoparticles on PAN electrospun nanofibers. The doping of SO42− ions into Ag3PO4 crystal lattice by replacing PO43− ions can provide sufficient electron-hole separation capability to the SO42−-Ag3PO4/PAN heterojunction to generate reactive oxygen species (ROS) under visible light irradiation and enhances its antibacterial performance. Finally, we hope this work may offer a new paradigm to design and fabricate other types of flexible self-supporting negative-ions-doped heterojunction nanofibers using electrospinning technique for bactericidal applications.
Resveratrol and Its Nanoformulation Attenuate Growth and the Angiogenesis of Xenograft and Orthotopic Colon Cancer Models
Authors: Sudha Thangirala , El-Far Ali H. , Mousa Deena S. , Mousa Shaker A.
Published: March 2020

Cancer is a multifactorial disorder that induces mortality worldwide, and the colorectal type is the third most common cancer globally. Resveratrol (RSV) is a natural compound with an effective anticancer effect, especially against colorectal cancer, and therefore numerous studies recommended its use in colorectal cancer prevention and treatment. The current study investigated the effect of either RSV or its nanoformulation (NP-RSV) on the growth and vascularity of xenograft and orthotopic mice models in colon cancer (COLO205-luc). Both RSV and NP-RSV induced significant reductions in tumor growth and the hemoglobin percentages of the tumor mass, but NP-RSV showed greater bioavailability and efficacy than RSV. Generally, we recommend using NP-RSV as a therapeutic to control colon cancer.
Phytochemical Screening and Acanthamoebic Activity of Shoots from in Vitro Cultures and in Vivo Plants of Eryngium alpinum L.—The Endangered and Protected Species
Authors: Kikowska Małgorzata , Kruszka Dariusz , Derda Monika , Hadaś Edward , Thiem Barbara
Published: March 2020

Genetically uniform shoots of Eryngium alpinum L. cultured in vitro were subjected to the qualitative analysis applying the UPLC-HESI-HRMS technique. In vitro cultures give the opportunity to perform the phytochemical studies on the protected species without harvesting the plant material from the natural environment. The phytochemical screening of the crude methanolic extracts of shoots, both from in vitro cultures and in vivo plants, revealed the presence of phenolic acids, coumarins, flavonoids, triterpenoid saponins, amino acids, or dipeptides. Active compounds detected are known to have medicinal importance, and for this reason, the present study represents a preliminary investigation of the extracts against pathogenic and opportunistic amoeba. Among the extracts tested, the extract of shoots from in vitro cultures exhibited remarkable amoebicidal action against trophozoites. On the second day of treatment, the extract at the concentrations of 5 mg/mL, 2.5 mg/mL, and 0.5 mg/mL showed the highest antiamoebicidal effect: the inhibition of trophozoites reached 81.14%, 66.38%, and 54.99%, respectively. To our best knowledge, the present report is the first to show the phytochemical screening and to discuss the antiamoebic activity of Eryngium alpinum L. shoots, both from in vitro cultures and in vivo plants.
Straw in Clay Bricks and Plasters—Can We Use Its Molecular Decay for Dating Purposes?
Authors: Tintner Johannes , Roth Kimberly , Ottner Franz , Syrová-Anýžová Zuzana , Žabičková Ivana , Wriessnig Karin , Meingast Roland , Feiglstorfer Hubert
Published: March 2020

Dating of clay bricks (adobe) and plasters is a relevant topic not only for building historians in the Pannonian region. Especially in vernacular architecture in this region, clay with straw amendments is a dominant construction material. The paper presents the potential of the molecular decay of these amendments to establish prediction tools for age based on infrared spectroscopic measurements. Preliminary results revealed spectral differences between the different plant parts, especially culms, nodes, and ear spindles. Based on these results, a first prediction model is presented including 14 historic samples. The coefficient of determination for the validation reached 62.2%, the (RMSE) root mean squared error amounted to 93 years. Taking the limited sample amount and the high material heterogeneity into account, this result can be seen as a promising output. Accordingly, sample size should be increased to a minimum of 100 objects and separate models for the different plant parts should be established.
Antimicrobial and Antioxidant Properties of Four Lycopus Taxa and an Interaction Study of Their Major Compounds
Authors: Trajčíková Eva , Kurin Elena , Slobodníková Lívia , Straka Marek , Lichváriková Aneta , Dokupilová Svetlana , Čičová Iveta , Nagy Milan , Mučaji Pavel , Bittner Fialová Silvia
Published: March 2020

The compositions of leaf infusions of three genotypes of Lycopus europaeus L. with origins in central Europe, namely L. europaeus A (LeuA), L. europaeus B (LeuB), and L. europaeus C (LeuC), and one genotype of L. exaltatus (Lex), were examined by LC-MS-DAD (Liquid Chromatography Mass Spectrometry and Diode Array Detection) analysis. This revealed the presence of thirteen compounds belonging to the groups of phenolic acids and flavonoids, with a predominance of rosmarinic acid (RA) and luteolin-7-O-glucuronide (LGlr). The antimicrobial activity of leaf infusions was tested on the collection strains of Gram-positive and Gram-negative bacteria, and on the clinical Staphylococcus aureus strains. We detected higher activity against Gram-positive bacteria, of which the most susceptible strains were those of Staphylococcus aureus, including methicillin-resistant and poly-resistant strains. Furthermore, we examined the antioxidant activity of leaf infusions using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) methods, and on NIH/3T3 cell lines using dichlorodihydrofluorescein diacetate (DCFH-DA). We also studied the mutual interactions between selected infusions, namely RA and/or LGlr. In the mixtures of leaf infusion and RA or LGlr, we observed slight synergism and a high dose reduction index in most cases. This leads to the beneficial dose reduction at a given antioxidant effect level in mixtures compared to the doses of the parts used alone. Therefore, our study draws attention to further applications of the Lycopus leaves as a valuable alternative source of natural antioxidants and as a promising topical antibacterial agent for medicinal use.
Biomemristic Behavior for Water-Soluble Chitosan Blended with Graphene Quantum Dot Nanocomposite
Authors: Li Lei
Published: March 2020

Bionanocomposite has promising biomemristic behaviors for data storage inspired by a natural biomaterial matrix. Carboxylated chitosan (CCS), a water-soluble derivative of chitosan avoiding the acidic salt removal, has better biodegradability and bioactivity, and is able to absorb graphene quantum dots (GQDs) employed as charge-trapping centers. In this investigation, biomemristic devices based on water-soluble CCS:GQDs nanocomposites were successfully achieved with the aid of the spin-casting method. The promotion of binary biomemristic behaviors for Ni/CCS:GQDs/indium-tin-oxide (ITO) was evaluated for distinct weight ratios of the chemical components. Fourier transform infrared spectroscopy, Raman spectroscopy (temperature dependence), thermogravimetric analyses and scanning electron microscopy were performed to assess the nature of the CCS:GQDs nanocomposites. The fitting curves on the experimental data further confirmed that the conduction mechanism might be attributed to charge trapping–detrapping in the CCS:GQDs nanocomposite film. Advances in water-soluble CCS-based electronic devices would open new avenues in the biocompatibility and integration of high-performance biointegrated electronics.
The Emerging Role of ncRNAs and RNA-Binding Proteins in Mitotic Apparatus Formation
Authors: Ito Kei K. , Watanabe Koki , Kitagawa Daiju
Published: March 2020

Mounting experimental evidence shows that non-coding RNAs (ncRNAs) serve a wide variety of biological functions. Recent studies suggest that a part of ncRNAs are critically important for supporting the structure of subcellular architectures. Here, we summarize the current literature demonstrating the role of ncRNAs and RNA-binding proteins in regulating the assembly of mitotic apparatus, especially focusing on centrosomes, kinetochores, and mitotic spindles.