bluuebunny/crossref_metadata_2025 huggingface dataset:
Acid–Base Equilibrium and Self-Association in Relation to High Antitumor Activity of Selected Unsymmetrical Bisacridines Established by Extensive Chemometric Analysis
Authors: Kosno Michał , Laskowski Tomasz , Frackowiak Joanna E. , Potęga Agnieszka , Kurdyn Agnieszka , Andrałojć Witold , Borzyszkowska-Bukowska Julia , Szwarc-Karabyka Katarzyna , Mazerska Zofia
Published: June 2022

Unsymmetrical bisacridines (UAs) represent a novel class of anticancer agents previously synthesized by our group. Our recent studies have demonstrated their high antitumor potential against multiple cancer cell lines and human tumor xenografts in nude mice. At the cellular level, these compounds affected 3D cancer spheroid growth and their cellular uptake was selectively modulated by quantum dots. UAs were shown to undergo metabolic transformations in vitro and in tumor cells. However, the physicochemical properties of UAs, which could possibly affect their interactions with molecular targets, remain unknown. Therefore, we selected four highly active UAs for the assessment of physicochemical parameters under various pH conditions. We determined the compounds’ pKa dissociation constants as well as their potential to self-associate. Both parameters were determined by detailed and complex chemometric analysis of UV-Vis spectra supported by nuclear magnetic resonance (NMR) spectroscopy. The obtained results indicate that general molecular properties of UAs in aqueous media, including their protonation state, self-association ratio, and solubility, are strongly pH-dependent, particularly in the physiological pH range of 6 to 8. In conclusion, we describe the detailed physicochemical characteristics of UAs, which might contribute to their selectivity towards tumour cells as opposed to their effect on normal cells.
Issues with the European Pharmacopoeia Quality Control Method for 99mTc-Labelled Macroaggregated Albumin
Authors: Jensen Svend Borup , Meyer Lotte Studsgaard , Nielsen Nikolaj Schandorph , Nielsen Søren Steen
Published: June 2022

Technetium-99m macroaggregated albumin ([99mTc]Tc-MAA) is an injectable radiopharmaceutical used in nuclear medicine for lung perfusion scintigraphy. After changing to a new batch of macroaggregated albumin (MAA), we saw unwanted uptake in the liver and spleen. The batch was therefore tested by both the supplier and us and we found it to comply with the requirements of the European Pharmacopoeia (Ph. Eur.). However, a simple comparison between the problematic batch and a batch supplied by another manufacturer showed that there was a significant difference. The quality testing showed a higher number of small particles in the problem encumbered MAA batch with unwanted in vivo uptake. In this article we present a simple method of testing for particle size of [99mTc]Tc-MAA, which gives a good indication of how the radioactive drug performs in vivo. We argue that the quality control method described in the Ph. Eur. should be changed. The changes will improve concordance between the laboratory analyzes and what is seen in vivo in human lung perfusion scintigraphy. Furthermore, we hope that the MAA suppliers without delay will replace their release procedure to be in accordance with the method described in this article.
Potent Activity of a High Concentration of Chemical Ozone against Antibiotic-Resistant Bacteria
Authors: Rangel Karyne , Cabral Fellipe O. , Lechuga Guilherme C. , Carvalho João P. R. S. , Villas-Bôas Maria H. S. , Midlej Victor , De-Simone Salvatore G.
Published: June 2022

Background: Health care-associated infections (HAIs) are a significant public health problem worldwide, favoring multidrug-resistant (MDR) microorganisms. The SARS-CoV-2 infection was negatively associated with the increase in antimicrobial resistance, and the ESKAPE group had the most significant impact on HAIs. The study evaluated the bactericidal effect of a high concentration of O3 gas on some reference and ESKAPE bacteria. Material and Methods: Four standard strains and four clinical or environmental MDR strains were exposed to elevated ozone doses at different concentrations and times. Bacterial inactivation (growth and cultivability) was investigated using colony counts and resazurin as metabolic indicators. Scanning electron microscopy (SEM) was performed. Results: The culture exposure to a high level of O3 inhibited the growth of all bacterial strains tested with a statistically significant reduction in colony count compared to the control group. The cell viability of S. aureus (MRSA) (99.6%) and P. aeruginosa (XDR) (29.2%) was reduced considerably, and SEM showed damage to bacteria after O3 treatment Conclusion: The impact of HAIs can be easily dampened by the widespread use of ozone in ICUs. This product usually degrades into molecular oxygen and has a low toxicity compared to other sanitization products. However, high doses of ozone were able to interfere with the growth of all strains studied, evidencing that ozone-based decontamination approaches may represent the future of hospital cleaning methods.
Highly Sensitive, Stretchable Pressure Sensor Using Blue Laser Annealed CNTs
Authors: Park Chanju , Choi Munsu , Lee Suhui , Kim Hyunho , Lee Taeheon , Billah Mohammad Masum , Jung Byunglib , Jang Jin
Published: June 2022

A piezoresistive sensor is an essential component of wearable electronics that can detect resistance changes when pressure is applied. In general, microstructures of sensing layers have been adopted as an effective approach to enhance piezoresistive performance. However, the mold-casted microstructures typically have quite a thick layer with dozens of microscales. In this paper, a carbon microstructure is formed by blue laser annealing (BLA) on a carbon nanotube (CNT) layer, which changes the surface morphology of CNTs into carbonaceous protrusions and increases its thickness more than four times compared to the as-deposited layer. Then, the pressure sensor is fabricated using a spin-coating of styrene–ethylene–butylene–styrene (SEBS) elastomer on the BLA CNTs layer. A 1.32 µm-thick pressure sensor exhibits a high sensitivity of 6.87 × 105 kPa−1, a wide sensing range of 278 Pa~40 kPa and a fast response/recovery time of 20 ms, respectively. The stability of the pressure sensor is demonstrated by the repeated loading and unloading of 20 kPa for 4000 cycles. The stretchable pressure sensor was also demonstrated using lateral CNT electrodes on SEBS surface, exhibiting stable pressure performance, with up to 20% stretching.
Multi-Level Resistive Switching in SnSe/SrTiO3 Heterostructure Based Memristor Device
Authors: Ho Tsz-Lung , Ding Keda , Lyapunov Nikolay , Suen Chun-Hung , Wong Lok-Wing , Zhao Jiong , Yang Ming , Zhou Xiaoyuan , Dai Ji-Yan
Published: June 2022

Multilevel resistive switching in memristive devices is vital for applications in non-volatile memory and neuromorphic computing. In this study, we report on the multilevel resistive switching characteristics in SnSe/SrTiO3(STO) heterojunction-based memory devices with silver (Ag) and copper (Cu) top electrodes. The SnSe/STO-based memory devices present bipolar resistive switching (RS) with two orders of magnitude on/off ratio, which is reliable and stable. Moreover, multilevel state switching is achieved in the devices by sweeping voltage with current compliance to SET the device from high resistance state (HRS) to low resistance state (LRS) and RESET from LRS to HRS by voltage pulses without compliance current. With Ag and Cu top electrodes, respectively, eight and six levels of resistance switching were demonstrated in the SnSe/SrTiO3 heterostructures with a Pt bottom electrode. These results suggest that a SnSe/STO heterojunction-based memristor is promising for applications in neuromorphic computing as a synaptic device.
Development of Molecularly Imprinted Polymers for Fenthion Detection in Food and Soil Samples
Authors: Farooq Saqib , Chen Bochang , Gao Fukun , Muhammad Ihsan , Ahmad Shakeel , Wu Haiyan
Published: June 2022

Modern agricultural production is greatly dependent on pesticide usage, which results in severe environmental pollution, health risks and degraded food quality and safety. Molecularly imprinted polymers are one of the most prominent approaches for the detection of pesticide residues in food and environmental samples. In this research, we prepared molecularly imprinted polymers for fenthion detection by using beta-cyclodextrin as a functional monomer and a room-temperature ionic liquid as a cosolvent. The characterization of the developed polymers was carried out. The polymers synthesized by using the room-temperature ionic liquid as the cosolvent had a good adsorption efficiency of 26.85 mg g−1, with a short adsorption equilibrium time of 20 min, and the results fitted well with the Langmuir isotherm model and pseudo-second-order kinetic model. The polymer showed cross-selectivity for methyl-parathion, but it had a higher selectivity as compared to acetamiprid and abamectin. A recovery of 87.44–101.25% with a limit of detection of 0.04 mg L−1 and a relative standard deviation of below 3% was achieved from soil, lettuce and grape samples, within the linear range of 0.02–3.0 mg L−1, using high-performance liquid chromatography with an ultraviolet detector. Based on the results, we propose a new, convenient and practical analytical method for fenthion detection in real samples using improved imprinted polymers with room-temperature ionic liquid.
Recent Progress in Lanthanide-Doped Inorganic Perovskite Nanocrystals and Nanoheterostructures: A Future Vision of Bioimaging
Authors: Arumugam Gowri Manohari , Karunakaran Santhosh Kumar , Galian Raquel E. , Pérez-Prieto Julia
Published: June 2022

All-inorganic lead halide perovskite nanocrystals have great potential in optoelectronics and photovoltaics. However, their biological applications have not been explored much owing to their poor stability and shallow penetration depth of ultraviolet (UV) excitation light into tissues. Interestingly, the combination of all-inorganic halide perovskite nanocrystals (IHP NCs) with nanoparticles consisting of lanthanide-doped matrix (Ln NPs, such as NaYF4:Yb,Er NPs) is stable, near-infrared (NIR) excitable and emission tuneable (up-shifting emission), all of them desirable properties for biological applications. In addition, luminescence in inorganic perovskite nanomaterials has recently been sensitized via lanthanide doping. In this review, we discuss the progress of various Ln-doped all-inorganic halide perovskites (LnIHP). The unique properties of nanoheterostructures based on the interaction between IHP NCs and Ln NPs as well as those of LnIHP NCs are also detailed. Moreover, a systematic discussion of basic principles and mechanisms as well as of the recent advancements in bio-imaging based on these materials are presented. Finally, the challenges and future perspectives of bio-imaging based on NIR-triggered sensitized luminescence of IHP NCs are discussed.
Facile Hydrothermal Synthesis of SnO2 Nanoflowers for Low-Concentration Formaldehyde Detection
Authors: Xiang Chao , Chen Tingting , Zhao Yan , Sun Jianhai , Jiang Kaisheng , Li Yongzhen , Zhu Xiaofeng , Zhang Xinxiao , Zhang Ning , Guo Ruihua
Published: June 2022

In this work, SnO2 nanoflowers were prepared by a simple one-step hydrothermal process. The morphology and structure of SnO2 nanoflowers were characterized by SEM, TEM, Raman spectroscopy, and XRD, which demonstrated the good crystallinity of the SnO2 tetrahedron structure of the as-synthesized materials. In addition, the sensing properties of SnO2 nanoflowers were studied in detail. It was found that the SnO2 nanoflower-based gas sensor exhibits excellent gas response (9.2 to 120 ppm), fast response and recovery (2/15 s to 6 ppm), good linearity of correlation between response (S) vs. concentration (C) (lgS = 0.505 lgC − 0.147, R2 = 0.9863), superb repeatability, and selectivity at 300 °C. The outstanding performance can also be attributed to the high specific surface area ratio and size of SnO2 nanoflowers close to the thickness of the electron depletion layer that can provide abundant active sites, promote the rate of interaction, and make it easier for gas molecules to diffuse into the interior of the material. Therefore, SnO2 nanoflowers can be an ideal sensing material for real-time monitoring of low-concentration HCHO.
Molecular Fingerprinting of the Omicron Variant Genome of SARS-CoV-2 by SERS Spectroscopy
Authors: Leonardi Antonio Alessio , Sciuto Emanuele Luigi , Lo Faro Maria Josè , Morganti Dario , Midiri Angelina , Spinella Corrado , Conoci Sabrina , Irrera Alessia , Fazio Barbara
Published: June 2022

The continuing accumulation of mutations in the RNA genome of the SARS-CoV-2 virus generates an endless succession of highly contagious variants that cause concern around the world due to their antibody resistance and the failure of current diagnostic techniques to detect them in a timely manner. Raman spectroscopy represents a promising alternative to variants detection and recognition techniques, thanks to its ability to provide a characteristic spectral fingerprint of the biological samples examined under all circumstances. In this work we exploit the surface-enhanced Raman scattering (SERS) properties of a silver dendrite layer to explore, for the first time to our knowledge, the distinctive features of the Omicron variant genome. We obtain a complex spectral signal of the Omicron variant genome where the fingerprints of nucleobases in nucleosides are clearly unveiled and assigned in detail. Furthermore, the fractal SERS layer offers the presence of confined spatial regions in which the analyte remains trapped under hydration conditions. This opens up the prospects for a prompt spectral identification of the genome in its physiological habitat and for a study on its activity and variability.
Artificial Gastrointestinal Models for Nutraceuticals Research—Achievements and Challenges: A Practical Review
Authors: Gościniak Anna , Eder Piotr , Walkowiak Jarosław , Cielecka-Piontek Judyta
Published: June 2022

Imitating the human digestive system as closely as possible is the goal of modern science. The main reason is to find an alternative to expensive, risky and time-consuming clinical trials. Of particular interest are models that simulate the gut microbiome. This paper aims to characterize the human gut microbiome, highlight the importance of its contribution to disease, and present in vitro models that allow studying the microbiome outside the human body but under near-natural conditions. A review of studies using models SHIME, SIMGI, TIM-2, ECSIM, EnteroMix, and PolyfermS will provide an overview of the options available and the choice of a model that suits the researcher’s expectations with advantages and disadvantages.
Effects of Blueberry Consumption on Cardiovascular Health in Healthy Adults: A Cross-Over Randomised Controlled Trial
Authors: Wang Yueyue , Gallegos Jose Lara , Haskell-Ramsay Crystal , Lodge John K.
Published: June 2022

Blueberries are rich in polyphenols, and their effect on cardiovascular health, including risk factors for endothelial dysfunction and hypertension, has been investigated in interventional studies. However, the difference between blueberry treatments in varied forms for their cardiovascular-protective effect remains poorly understood. The current study assessed the effects of whole blueberry and freeze-dried blueberry powder compared to a control on cardiovascular health in young adults. A cross-over randomised controlled trial (RCT) was implemented with 1 week of treatment for three treatment groups, each followed by 1 week of wash out period. Systolic (SBP) and diastolic blood pressure (DBP), pulse wave velocity (PWV), plasma cholesterol (low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), and total cholesterol) and triglyceride levels (TAG), and glucose and nitrite (NO2-) concentrations were compared following fresh blueberry, freeze-dried blueberry powder, and control treatments. Thirty-seven participants with a mean age of 25.86 ± 6.81 completed the study. No significant difference was observed among fresh blueberry, blueberry powder, and the control arm. Plasma NO2- levels were improved by 68.66% and 4.34% separately following whole blueberry and blueberry powder supplementations compared to the baseline, whereas the control supplementation reported a decrease (−9.10%), although it was not statistically significant. There were no other effects shown for SBP, DBP, total cholesterol, HDL-C, LDL-C, TAG, or glucose. No difference was shown between whole blueberry and freeze-dried blueberry powder consumption for improving cardiovascular health.
Effect of Novel Gastro-Duodenal Flow Restrictor on Relative Weight Loss and Glucose Levels in a Porcine Model: A Pilot Randomized Study
Authors: Huh Gunn , Kwon Jinhee , Kim So Hee , Lim Ha Jong , Min Se Hee , Park Do Hyun
Published: June 2022

Endoscopic bariatric and metabolic therapies are promising for obesity. We developed a novel gastro-duodenal flow restrictor (G-DFR) device for relative weight loss and lowering of glucose level and evaluated its safety and efficacy in a porcine model. The G-DFR comprised self-expandable gastro-duodenal partially covered polytetrafluoroethylene (PTFE) metal stent distally attached to a PTFE skirt. Eleven juvenile pigs were randomized into the evaluation of migration (n = 3), mid-term efficacy (n = 5), and control (n = 3) groups. Five pigs showed G-DFR migration at 2, 4, 7, and 10 weeks after placement in the migration and mid-term efficacy group. Compared to the control group, the mid-term efficacy group showed up to 55.4% relative weight loss in 12 weeks. Compared to the case group, the control group showed higher mean ghrelin hormone level from 6 to 12 weeks. Glucose level was significantly lower in the efficacy group than in the control group after 6 weeks. Serum alanine transferase levels and histological collagen deposition were lower in the liver of the case group than in the control group. Although it did not demonstrate consistent performance with respect to migration, a well-positioned G-DFR in the pyloroduodenal portion may lead to relative weight loss, lowering of glucose levels, and improved hepatic parameters.
A Short-Term Sucrose Diet Impacts Cell Proliferation of Neural Precursors in the Adult Hypothalamus
Authors: Recabal Antonia , López Sergio , Salgado Magdiel , Palma Alejandra , Obregón Ana M. , Elizondo-Vega Roberto , Sáez Juan C. , García-Robles María Á.
Published: June 2022

Radial glia-like cells in the hypothalamus and dorsal vagal complex are neural precursors (NPs) located near subventricular organs: median eminence and area postrema, respectively. Their strategic position can detect blood-borne nutrients, hormones, and mitogenic signals. Hypothalamic NPs increase their proliferation with a mechanism that involves hemichannel (HC) activity. NPs can originate new neurons in response to a short-term high-fat diet as a compensatory mechanism. The effects of high carbohydrate Western diets on adult neurogenesis are unknown. Although sugars are usually consumed as sucrose, more free fructose is now incorporated into food items. Here, we studied the proliferation of both types of NPs in Sprague Dawley rats exposed to a short-term high sucrose diet (HSD) and a control diet. In tanycyte cultures, we evaluated the effects of glucose and fructose and a mix of both hexoses on HC activity. In rats fed an HSD, we observed an increase in the proliferative state of both precursors. Glucose, either in the presence or absence of fructose, but not fructose alone, induced in vitro HC activity. These results should broaden the understanding of the nutrient monitoring capacity of NPs in reacting to changes in feeding behavior, specifically to high sugar western diets.
Isoflavone Protects the Renal Tissue of Diabetic Ovariectomized Rats via PPARγ
Authors: Ferraz Carbonel Adriana Aparecida , da Silva Rafael André , de Souza Ferreira Luiz Philipe , Vieira Renata Ramos , dos Santos Simões Ricardo , da Silva Sasso Gisela Rodrigues , de Jesus Simões Manuel , Soares Junior José Maria , Azevedo Lima Patrícia Daniele , Borges Fernanda Teixeira
Published: June 2022

Diabetes associated with post-menopause is related to a worse condition of kidney disease. Taking into consideration that this disorder may be regulated by estrogenic mediators, we evaluated the renal protective effect of isoflavone. We investigated the role of the PPARγ in the pathogenesis of the disease. For this study, we used diabetic female rats in a postmenopausal model through ovariectomy. The animals were treated with isoflavone or 17β-estradiol. A dosage was administered to bring on blood glycemia, and through immunohistochemistry, we evaluated the immunoreactivity of PPARγ in the endometrium and renal tissue. We analyzed the immunoreactivity of renal injury molecule KIM-1 and the collagen and glycogen densities in the kidney. Through bioinformatics analysis, we observed PPARγ and COL1A1 gene expression under the influence of different glucose doses. In particular, we observed that isoflavone and 17β-estradiol regulate blood glycemia. Renal injury was inhibited by isoflavone, observed by a reduction in KIM-1, along with glycogen accumulation. These benefits of isoflavone may be associated with PPARγ overexpression in the kidneys and endometrium of diabetic ovariectomized rats.
The Effects of Time-Restricted Eating on Metabolism and Gut Microbiota: A Real-Life Study
Authors: Ferrocino Ilario , Pellegrini Marianna , D’Eusebio Chiara , Goitre Ilaria , Ponzo Valentina , Fadda Maurizio , Rosato Rosalba , Mengozzi Giulio , Beccuti Guglielmo , Merlo Fabio Dario , Rahimi Farnaz , Comazzi Isabella , Cocolin Luca , Ghigo Ezio , Bo Simona
Published: June 2022

The metabolic benefits of time-restricted eating (TRE) in humans are statistically significant but not clinically relevant. Few data are available about the effects of TRE on the gut microbiota. We compared the effects of a TRE regimen (<12 h feeding; n = 25) with a time-unrestricted (TUE) regimen (>12 h feeding; n = 24), on the clinical and dietary variables and gut-microbiota composition in patients with obesity, who were subjected for 12 weeks to the same caloric restriction. Median weight loss was 4.0 kg and 2.2 kg in the TRE and TUE groups, respectively, with a between-group borderline difference (p = 0.049). No significant between-group difference was found in other dietary, anthropometric, or laboratory variables. There were no substantial between-group differences in alpha and beta diversity or gut-microbiota composition. The TRE group showed a significant increase in the frequency of Lachnospiraceae, Parasutterella, and Romboutsia at the study’s end. A TRE regimen induced small changes both in metabolic/dietary variables and in the gut-microbiota composition, with respect to the TUE. The microbial changes we have found were of uncertain clinical significance.
The Impact of the Different Stages of COVID-19, Time of the Week and Exercise Frequency on Mental Distress in Men and Women
Authors: Begdache Lina , Danesharasteh Anseh , Ertem Zeynep
Published: June 2022

The COVID-19 pandemic produced life disturbances and loss of routine which affected diet and sleep quality as well as physical exercise frequency. Interestingly, mental distress was higher even in those who exercised. The purpose of this study was to assess exercise frequency in relation to different levels of mental distress severity in men and women while accounting for working days and weekends. A de-identified secondary data set was analyzed. Regression analyses produced models of the different stages of COVID-19 in relation to physical exercise frequency and mental distress levels. Margin analysis generated predictive models that could be used prophylactically to customize physical exercise frequencies in men and women to reduce their risk of mental distress during future pandemics. Mental distress during the lockdown and after ease of restrictions was associated with different physical exercise frequencies, with a noticeable difference between men and women. During a pandemic, sedentary men are more likely to be mentally distressed during working days. Nevertheless, moderately active, but not very active women, may be less distressed during pandemic weekends. These findings may provide a framework to optimize mental health during different stages of a pandemic by customizing physical exercise frequencies based on gender and time of the week.
Tripartite Quantum Key Distribution Implemented with Imperfect Sources
Authors: Sekga Comfort , Mafu Mhlambululi
Published: June 2022

Multipartite quantum key distribution (QKD) is a promising area of quantum networks that provides unconditional secret keys among multiple parties, enabling only legitimate users to decrypt the encrypted message. However, security proofs of existing multipartite QKD typically assume perfect state preparation devices of legitimate users and neglect the relative rotation of reference frames. These presumptions are, nevertheless, very difficult to meet in practice, and thus the security of current multipartite QKD implementations is not guaranteed. By combining the idea of a loss tolerant technique, introduced by Tamaki et al. (K. Tamaki et al., Phys. Rev. A, 90, 052314, 2014), and the concept of a reference frame-independent protocol, we propose a three-party QKD protocol that considers state preparation flaws and the slow drift of reference frames. Through a numerical simulation, the influence of misaliged reference frames on the protocol’s stability was examined by drifting reference frames through angles β=π/5, β=π/6 and β=π/7. In addition, the performance of the proposed protocol was examined for the encoding flaws set at δ=0.35, δ=0.20, and δ=0.10. The results show that the protocol is robust against state preparation flaws, and is insignificantly impacted by misalignment of the reference frames because the achieved transmission distances and secret key rates are comparable to the perfect scenarios. This work dramatically contributes toward the realization of practical and secure multipartite QKD. The proposed protocol has direct applications in quantum communication network environments that involve unknown and slowly varying reference frames, web conferences, and online communications.
Monkeypox: Another Sexually Transmitted Infection?
Authors: Rodriguez-Morales Alfonso J. , Lopardo Gustavo
Published: June 2022

Monkeypox virus is a zoonotic DNA virus (Poxviridae family), identified in 1958 in Asian monkeys (mostly Macaca fascicularis) in a polio vaccine research animal facility in Copenhagen, Denmark [...]
Novel Potent and Selective Agonists of the GPR55 Receptor Based on the 3-Benzylquinolin-2(1H)-One Scaffold
Authors: Ceni Costanza , Benko Michael J. , Mohamed Kawthar A. , Poli Giulio , Di Stefano Miriana , Tuccinardi Tiziano , Digiacomo Maria , Valoti Massimo , Laprairie Robert B. , Macchia Marco , Bertini Simone
Published: June 2022

A growing body of evidence underlines the crucial role of GPR55 in physiological and pathological conditions. In fact, GPR55 has recently emerged as a therapeutic target for several diseases, including cancer and neurodegenerative and metabolic disorders. Several lines of evidence highlight GPR55′s involvement in the regulation of microglia-mediated neuroinflammation, although the exact molecular mechanism has not been yet elucidated. Nevertheless, there are only a limited number of selective GPR55 ligands reported in the literature. In this work, we designed and synthesized a series of novel GPR55 ligands based on the 3-benzylquinolin-2(1H)-one scaffold, some of which showed excellent binding properties (with Ki values in the low nanomolar range) and almost complete selectivity over cannabinoid receptors. The full agonist profile of all the new derivatives was assessed using the p-ERK activation assay and a computational study was conducted to predict the key interactions with the binding site of the receptor. Our data outline a preliminary structure–activity relationship (SAR) for this class of molecules at GPR55. Some of our compounds are among the most potent GPR55 agonists developed to date and could be useful as tools to validate this receptor as a therapeutic target.
Roles of Bacterial Mechanosensitive Channels in Infection and Antibiotic Susceptibility
Authors: Sidarta Margareth , Baruah Luna , Wenzel Michaela
Published: June 2022

Bacteria accumulate osmolytes to prevent cell dehydration during hyperosmotic stress. A sudden change to a hypotonic environment leads to a rapid water influx, causing swelling of the protoplast. To prevent cell lysis through osmotic bursting, mechanosensitive channels detect changes in turgor pressure and act as emergency-release valves for the ions and osmolytes, restoring the osmotic balance. This adaptation mechanism is well-characterized with respect to the osmotic challenges bacteria face in environments such as soil or an aquatic habitat. However, mechanosensitive channels also play a role during infection, e.g., during host colonization or release into environmental reservoirs. Moreover, recent studies have proposed roles for mechanosensitive channels as determinants of antibiotic susceptibility. Interestingly, some studies suggest that they serve as entry gates for antimicrobials into cells, enhancing antibiotic efficiency, while others propose that they play a role in antibiotic-stress adaptation, reducing susceptibility to certain antimicrobials. These findings suggest different facets regarding the relevance of mechanosensitive channels during infection and antibiotic exposure as well as illustrate that they may be interesting targets for antibacterial chemotherapy. Here, we summarize the recent findings on the relevance of mechanosensitive channels for bacterial infections, including transitioning between host and environment, virulence, and susceptibility to antimicrobials, and discuss their potential as antibacterial drug targets.
Anti-Inflammatory Activity of Piquerol Isolated from Piqueria trinervia Cav.
Authors: Campos-Xolalpa Nimsi , Esquivel-Campos Ana Laura , Martínez-Casares Rubria Marlen , Pérez-Gutiérrez Salud , Pérez-Ramos Julia , Sánchez-Mendoza Ernesto
Published: June 2022

Background: Inflammation is a complex process as a response to several stimuli, such as infection, a chemical irritant, and the attack of a foreign body. Piquerol was isolated from Piqueria trinervia, and its anti-inflammatory activity was evaluated using in vivo and in vitro models. Methods: Piquerol is a monoterpene that was identified using NMR, FT-IR spectroscopy, and mass spectrometry analysis. The anti-inflammatory activity was tested in vivo in ear edema induced with TPA in mice. Piquerol was also tested on J774A.1 macrophages stimulated with lipopolysaccharide (LPS), and the levels of NO, NF-κB, TNF-α, IL-1β, IL-6, and IL-10 were determined using ELISA. Results: The results show that piquerol diminished ear edema (66.19%). At 150.51 µM, it also inhibited the levels of NO (31.7%), TNF-α (49.8%), IL-1β (69.9%), IL-6 (47.5%), and NF-κB (26.7%), and increased the production of IL-10 (62.3%). Piquerol has a membrane stabilization property in erythrocyte, and at 100 µg/mL, the membrane protection was of 86.17%. Conclusions: Piquerol has anti-inflammatory activity, and its possible mechanism of action is through the inhibition of pro-inflammatory mediators. This compound could be a candidate in the development of new drugs to treat inflammatory problems.
Photoinduced Antibacterial Activity and Cytotoxicity of CdS Stabilized on Mesoporous Aluminosilicates and Silicates
Authors: Stavitskaya Anna , Sitmukhanova Eliza , Sayfutdinova Adeliya , Khusnetdenova Elnara , Mazurova Kristina , Cherednichenko Kirill , Naumenko Ekaterina , Fakhrullin Rawil
Published: June 2022

Inactivation of bacteria under the influence of visible light in presence of nanostructured materials is an alternative approach to overcome the serious problem of the growing resistance of pathogenic bacteria to antibiotics. Cadmium sulfide quantum dots are superefficient photocatalytic material suitable for visible light transformation. In this work, CdS nanoparticles with size of less than 10 nm (QDs) were synthesized on the surface of natural and synthetic mesoporous aluminosilicates and silicates (halloysite nanotubes, MCM-41, MCM-41/Halloysite, SBA-15). Materials containing 5–7 wt.% of CdS were characterized and tested as agents for photocatalytic bacteria degradation of Gram-positive S. aureus and Gram-negative E. coli with multiple antibiotic resistance. Eukaryotic cell viability tests were also conducted on the model cancer cells A 459. We found that the carrier affects prokaryotic and eukaryotic toxicity of CdS quantum dots. CdS/MCM-41/HNTs were assumed to be less toxic to eukaryotic cells and possess the most prominent photocatalytic antibacterial efficiency. Under visible light irradiation, it induced 100% bacterial growth inhibition at the concentration of 125 μg/mL and the bacteriostatic effect at the concentration of 63 μg/mL. CdS/MCM-41/HNTs showed 100% E. coli growth inhibition in the concentration of 1000 μg/mL under visible light irradiation.
The Evolution of the 3D-Printed Drug Delivery Systems: A Review
Authors: Bácskay Ildikó , Ujhelyi Zoltán , Fehér Pálma , Arany Petra
Published: June 2022

Since the appearance of the 3D printing in the 1980s it has revolutionized many research fields including the pharmaceutical industry. The main goal is to manufacture complex, personalized products in a low-cost manufacturing process on-demand. In the last few decades, 3D printing has attracted the attention of numerous research groups for the manufacturing of different drug delivery systems. Since the 2015 approval of the first 3D-printed drug product, the number of publications has multiplied. In our review, we focused on summarizing the evolution of the produced drug delivery systems in the last 20 years and especially in the last 5 years. The drug delivery systems are sub-grouped into tablets, capsules, orodispersible films, implants, transdermal delivery systems, microneedles, vaginal drug delivery systems, and micro- and nanoscale dosage forms. Our classification may provide guidance for researchers to more easily examine the publications and to find further research directions.
Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz
Authors: Mukubwa Grady K. , Safari Justin B. , Walker Roderick B. , Krause Rui W. M.
Published: June 2022

Despite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efavirenz (EFV) as a drug model. EFV solubility was assessed in water, Labrafac Lipophile and medium chain triglycerides oil (MCT oil). EFV turned out to be more soluble in the two latter dissolving media (solubility > 250 mg/mL); hence, given its affordability, MCT oil was used for LNC formulation. LNC were prepared using a low-energy method named phase inversion, and following a design of experiments process. This one resulted in polynomial models that predicted LNC particle size, polydispersity index and zeta potential that were, respectively, around 50 nm, below 0.2 and below −33 mV, for the optimized formulations. Once synthesized, we were able to achieve an encapsulation efficacy of 87%. On the other hand, high EFV release from the LNC carrier was obtained in neutral medium as compared to acid milieu (pH 4) with, respectively, 42 and 27% EFV release within 74 h. Other characterization techniques were applied and further supported the successful encapsulation of EFV in LNCs in an amorphous form. Stability studies revealed that the developed LNC were quite stable over the period of 28 days. Ultimately, LNCs have been demonstrated to improve the biopharmaceutical properties of EFV and could therefore be used to fight against antiviral resistance.
Performance Analysis of Dual-Hop FSO Cooperative Systems over ℱ Turbulence with Pointing Errors
Authors: Le-Tran Manh , Kim Sunghwan
Published: June 2022

Recently, atmospheric-turbulence-induced fading in free-space optical (FSO) communication with pointing error impairment was modeled and studied using the Fisher–Snedecor F distribution with a good fit to experimental data. In this letter, we investigate the end-to-end performance of dual-hop FSO fixed-gain relaying systems operating over F turbulence channels. More specifically, we present closed-form expressions for the cumulative distribution function and the probability density function of the end-to-end signal-to-noise (SNR) ratio of the proposed system. Consequently, the outage probability, ergodic capacity, and average bit error rate performance are derived with tight asymptotic results in high-SNR regimes to gain more insight into the impacts of system parameters and channel turbulence conditions. Finally, Monte Carlo simulations are provided to validate the analytical results, revealing a significant performance gain compared to a single FSO link in the medium- to high-SNR range by using dual-hop FSO relaying.
High-Efficiency and High-Power Multijunction InGaAs/InP Photovoltaic Laser Power Converters for 1470 nm
Authors: Fafard Simon , Masson Denis P.
Published: June 2022

The high-efficiency capabilities of multijunction laser power converters are demonstrated for high-power applications with an optical input of around 1470 nm. The InP-based photovoltaic power converting III-V semiconductor devices are designed here, with 10 lattice-matched subcells (PT10-InGaAs/InP), using thin InGaAs absorbing layers connected by transparent tunnel junctions. The results confirm that such long-wavelength power converter devices are capable of producing electrical output voltages greater than 4–5 V. The characteristics are compatible with common electronics requirements, and the optical input is well suited for propagation over long distances through fiber-based optical links. Conversion efficiencies of ~49% are measured at electrical outputs exceeding 7 W for an input wavelength of 1466 nm at 21 °C. The Power Converter Performance Chart has been updated with these PT10-InGaAs/InP results.
Improving the Carotenoid Content in Maize by Using Isonuclear Lines
Authors: Calugar Roxana Elena , Muntean Edward , Varga Andrei , Vana Carmen Daniela , Has Voichita Virginia , Tritean Nicolae , Ceclan Loredana Anca
Published: June 2022

Carotenoids are important biologically active compounds in the human diet due to their role in maintaining a proper health status. Maize (Zea mays L.) is one of the main crops worldwide, in terms of production quantity, yield and harvested area, as it is also an important source of carotenoids in human nutrition worldwide. Increasing the carotenoid content of maize grains is one of the major targets of the research into maize breeding; in this context, the aim of this study was to establish the influence of some fertile cytoplasm on the carotenoid content in inbred lines and hybrids. Twenty-five isonuclear lines and 100 hybrids were studied for the genetic determinism involved in the transmission of four target carotenoids: lutein, zeaxanthin, β-cryptoxanthin and β-carotene. The analysis of carotenoids was carried out using high performance liquid chromatography using a Flexar system with UV-VIS detection. The obtained data revealed that the cytoplasms did not have a significant influence on the carotenoid content of the inbred lines; larger differences were attributed to the cytoplasm × nucleus interaction. For hybrids, the cytoplasmic nuclear interactions have a significant influence on the content of lutein, zeaxanthin and β-cryptoxanthin. For the cytoplasm × nucleus × tester interactions, significant differences were identified for all traits.
Impact of Internal Faraday Shields on RF Driven Hydrogen Discharges
Authors: Rauner David , Zielke Dominikus , Briefi Stefan , Fantz Ursel
Published: June 2022

At RF plasma reactors operated at high power, internal Faraday shields are required to shield dielectric vessel or windows from erosion due to isotropic heat and particle fluxes. By utilizing a flexible and diagnostically well-equipped laboratory setup, crucial effects that accompany the application of internal Faraday shields at low-pressure hydrogen (and deuterium) RF discharges are identified and quantified in this contribution. Both an inductively coupled plasma (ICP) utilizing a helical coil and a low-field helicon discharge applying a Nagoya-type III antenna at magnetic fields of up to 12 mT are investigated. Discharges are driven at 4 MHz and in the pressure range between 0.3 and 10 Pa while the impact of the Faraday shields on both the RF power transfer efficiency and spectroscopically determined bulk plasma parameters (electron density and temperature, atomic density) is investigated. Three main effects are identified and discussed: (i) due to the Faraday shield, the measured RF power transfer efficiency is globally reduced. This is mainly caused by increased power losses due to induced eddy currents within the electrostatic shield, as accompanying numerical simulations by a self-consistent fluid model demonstrate. (ii) The Faraday shield reduces the atomic hydrogen density in the plasma by one order of magnitude, as the recombination rate of atoms on the metallic (copper) surfaces of the shield is considerably higher compared to the dielectric quartz walls. (iii) The Faraday shield suppresses the transition of the low-field helicon setup to a wave heated regime at the present conditions. This is attributed to a change of boundary conditions for wave propagation, as the plasma is in direct contact with the conductive surfaces of the Faraday shield rather than being operated in a laterally fully dielectric vessel.
Facile Electrodeposition of NiCo2O4 Nanosheets on Porous Carbonized Wood for Wood-Derived Asymmetric Supercapacitors
Authors: Yang Jingjiang , Li Huiling , He Shuijian , Du Haijuan , Liu Kunming , Zhang Chunmei , Jiang Shaohua
Published: June 2022

Multichannel-porous carbon derived from wood can serve as a conductive substrate for fast charge transfer and ion diffusion, supporting the high-theory capacitance of pseudocapacitive materials. Herein, NiCo2O4 nanosheets, which are hierarchically porous, anchored on the surface of carbonized wood via electrodeposition for free-binder high-performance supercapacitor electrode materials, were proposed. Benefiting from the effectively alleviated NiCo2O4 nanosheets accumulation and sufficient active surface area for redox reaction, a N-doped wood-derived porous carbon-NiCo2O4 nanosheet hybrid material (NCNS–NCW) electrode exhibited a specific electric capacity of 1730 F g−1 at 1 A g−1 in 1 mol L−1 KOH and splendid electrochemical firmness with 80% capacitance retention after cycles. Furthermore, an all-wood-based asymmetric supercapacitor based on NCNS–NCW//NCW was assembled and a high energy density of 56.1 Wh kg−1 at a watt density of 349 W kg−1 was achieved. Due to the great electrochemical performance of NCNS–NCW, we expect it to be used as an electrode material with great promise for energy storage equipment.
Preparation of the Carbonized Zif−8@PAN Nanofiber Membrane for Cadmium Ion Adsorption
Authors: Sun Hui , Feng Jiangli , Song Yaoyao , Xu Lei , Cui Xiaogang , Yu Bin
Published: June 2022

The zeolitic imidazolate framework (ZIF−8)@polyacrylonitrile (PAN) nanofiber membrane was prepared and carbonized for heavy metal cadmium ion (Cd2+) adsorption in aqueous medium. Zinc oxide (ZnO) was first sputtered onto the surface of the PAN electrospun nanofiber membrane to provide a metal ion source. Then, the ZIF−8@PAN nanofiber membrane was prepared via in situ solvothermal reaction and carbonized in a tube furnace at 900 °C under a N2 atmosphere to enhance adsorption performance. The synthesized ZIF−8 particles with polyhedral structure were uniformly immobilized on the surface of the PAN electrospun nanofiber membrane. After being heated at 900 °C, the polygonal ZIF−8 shrank, and the carbonized ZIF−8@PAN nanofiber membrane was obtained. Compared with the nanofiber membrane without being carbonized, the adsorption capacity of the carbonized ZIF−8@PAN nanofiber membrane reached 102 mg L−1, and its Cd2+ adsorption efficiency could be more than 90% under the adsorption temperature of 35 °C and solution of pH = 7.5 conditions. According to the adsorption thermodynamics analysis, the Cd2+ adsorption process of the carbonized ZIF−8@PAN nanofiber membrane was spontaneous. The whole Cd2+ adsorption process was more suitably described by the pseudo second-order adsorption kinetics model, indicating that there exists a chemical adsorption mechanism besides physical adsorption.
Influence of Paste Strength on the Strength of Expanded Polystyrene (EPS) Concrete with Different Densities
Authors: He Diyang , Zheng Wukui , Chen Zili , Qi Yongle , Zhang Dawang , Li Hui
Published: June 2022

Concrete in which EPS (expanded polystyrene) particles partially or completely replace concrete aggregates is called EPS concrete. Compared to traditional concrete, EPS concrete has a controllable low density and good thermal-insulation performance, which make it promising for prospective applications. At present, research on EPS concrete mostly focuses on increasing its strength and EPS surface modifications. Few researchers have studied the influence of cementitious material strength and EPS-concrete density on the strength of EPS concrete. In this research, cement was used as the main material, and fly ash, silica fumes, and blast furnace slag were selected as admixtures. By changing the mixing proportions of the admixtures, the basic properties, such as the paste strength, change. Based on the mix proportions of the above different raw materials, EPS concrete with different density levels was prepared to explore the influence of the density of EPS concrete and the strength of cementitious materials on the strength of EPS concrete. The influence of the slurry strength on EPS-concrete strength was weaker than that of the density of EPS concrete. When the strength range of the cementitious materials is 35.7~70.5 MPa, the compressive strength range of 1000 kg/m3, 1200 kg/m3, and 1400 kg/m3 EPS concrete is 8.8~17.6 MPa, 11.4~18.0 MPa, and 15.7~26.6 MPa, respectively. Based on the experiments, the fitting equation to determine the EPS-concrete strength–EPS-concrete density–cementitious material strength is z = 69.00087 + 0.0244x − 0.1746y − 0.00189x2 + 0.0000504706y2 + 0.00028401xy. Additionally, a strength-increasing design method for EPS concrete with different densities prepared by conventional Portland cement is clarified. This study can guide the preparation of EPS concrete.
Mechanical Behavior of Thermoplastic Starch: Rationale for the Temperature-Relative Humidity Equivalence
Authors: Leroy Lise , Stoclet Gregory , Lefebvre Jean-Marc , Gaucher Valerie
Published: June 2022

This paper aimed at understanding and rationalizing the influence of both temperature and relative humidity on the mechanical behavior of thermoplastic starch (TPS). DMA experiments revealed that water molecules impact the crosslinking network by reducing the intermolecular hydrogen bond density, resulting in a less dense entanglement network. In addition, the in-situ X-ray characterization during hydration of starch revealed structural changes, which were ascribed to conformational changes in the starch chain, due to their interaction with the uptake water molecules. Finally, the study of TPS uniaxially stretched at different temperatures and humidity showed that the mechanical behavior of TPS could be rationalized by considering the ΔT parameter, which corresponds to the temperature difference between the drawing temperature and the glass transition temperature of TPS.