bluuebunny/crossref_metadata_2025_split huggingface dataset:
Quinoline Hydrazide/Hydrazone Derivatives: Recent Insights on Antibacterial Activity and Mechanism of Action
Authors: Verma Sangeeta , Lal Sukhbir , Narang Rakesh , Sudhakar Kalvatala 
Published: January 2023

AbstractAntibiotics are becoming gradually ineffective due to drug resistance, leading to greater difficulty in the treatment of infectious diseases. Therefore, the development of new chemical entities with different mechanisms of action is essential in the fight against resistant microorganisms. Various studies have shown that quinoline hydrazide/hydrazone derivatives possess several biological activities, such as antimalarial, antitubercular, anticancer, anti‐inflammatory, and antimicrobial. Among these activities, the antibacterial activity of quinoline hydrazide/hydrazone derivatives is noteworthy. The synthetic flexibility of the quinoline ring has led to the development of a wide range of structurally diverse quinoline hydrazide/hydrazone derivatives, which can act at various bacterial targets such as DNA gyrase, glucosamine‐6‐phosphate synthase, enoyl ACP reductase, and 3‐ketoacyl ACP reductase. This review emphasizes the antibacterial potential of various reported quinoline hydrazide/hydrazone derivatives based on substitution in the quinoline ring. The antibacterial activity of various metal‐quinoline hydrazide/hydrazone complexes is also discussed. The aim of this review is to assemble and scrutinize the latest reports in this promising area of drug development.
Emerging photo‐integrated rechargeable aqueous zinc‐ion batteries and capacitors toward direct solar energy conversion and storage
Authors: Wang Kexuan , Li Heng , Xu Zhu , Wang Huibo , Ge Mingzheng , Zhang Yanyan , Chen Shi , Tang Yuxin 
Published: January 2023

AbstractPhoto‐integrated rechargeable aqueous zinc‐ion batteries (ZIBs)/zinc‐ion capacitors (ZICs) have recently attracted substantial attention as a viable strategy to realize solar to electrochemical energy conversion and storage in a single device. Herein, a timely perspective on the latest advances in photo‐integrated rechargeable ZIBs/ZICs is presented. We first provide a brief introduction for the three different device types and working principles of the photo‐integrated rechargeable ZIB/ZIC devices, including tandem connected photo‐rechargeable hybrid energy systems, photo‐electrode integrated ZIBs, and photo‐rechargeable ZIBs/ZICs. Then, the significant advances in configuration design, materials chemistry, and performance evaluation of photo‐integrated rechargeable ZIBs/ZICs are systematically discussed. At last, the current challenges and future research emphases are suggested, which is to pave the way for the photo‐integrated rechargeable ZIBs/ZICs from laboratory technology to commercialization. This short yet informative perspective aims to evoke more research interests in developing high‐performance photo‐integrated rechargeable ZIBs/ZICs and other hybrid energy systems toward the direct conversion and storage of solar energy to electrochemical energy.
Synergy of Pt Single Atom and Clusters toward Selective Glycerol Oxidation
Authors: Luo Zhicheng , Zhu Zhiguo , Xiao Rui , Chu Dawang 
Published: January 2023

AbstractSelective oxidation of excess glycerol to glyceric acid is a significant reaction but the reaction is inhibited by the C−H activation that has a high energy barrier. Here, we introduced Pt single atom species (Pt−O−Ce) into Pt/CeO2, which gave a high glycerol conversion of 90.9% with a high glyceric acid selectivity of 83.2% under the mild reaction conditions (T=100 °C, O2 flow of 5 mL min−1, and non‐alkaline). The C−H bond can be easily adsorbed and activated over Pt−O−Ce, which facilitated the selective oxidation of primary C−OH with a bidentate adsorption on Ptcluster, verified by the CO‐DRIFT, XPS, HRTEM, and in situ IR adsorption experiments. This synergy provided a way to design stable and active catalyst in biomass conversion.
Relative Bioavailability and Food Effect of Asciminib Pediatric Mini‐tablet Formulation Compared to the Reference Tablet Formulation in Healthy Adult Participants
Authors: Hoch Matthias , Bebrevska Lidiya , Singh Namrata , Hourcade‐Potelleret Florence 
Published: January 2023

AbstractAsciminib, a first‐in‐class allosteric BCR::ABL1 inhibitor that works by Specifically Targeting the ABL Myristoyl Pocket (STAMP) is used in the treatment of chronic myeloid leukemia. We describe a randomized, single‐dose, open‐label, four‐period crossover study in healthy adult participants (N = 24) which evaluated the relative bioavailability of a single 40‐mg dose of asciminib in pediatric formulation (1‐mg mini‐tablets) compared with the reference adult tablet under fasted conditions. Additionally, the effect of food on the bioavailability of the mini‐tablet formulation was evaluated. Under fasted conditions, asciminib exposure was similar for both formulations (geometric mean [Gmean] area under the concentration–time curve from time 0 to infinity [AUCinf] 5970 and 5700 ng ×h/mL, respectively). Food decreased the AUCinf and maximum plasma concentration (Cmax) of the asciminib mini‐tablets; this effect was more pronounced with a high‐fat meal (Gmean ratios [90% confidence interval]: fasted/low‐fat meal, 0.42 [0.38–047], 0.32 [0.28–0.37], respectively; fasted/high‐fat meal, 0.30 [0.27–0.34], 0.22 [0.19–0.25], respectively). The mini‐tablets were assessed to be easy to ingest with good palatability. Asciminib doses for a pivotal pediatric clinical trial will be defined using physiologically based pharmacokinetic modeling, which will consider the age and the higher food effect observed with the mini‐tablets.
Predicting Treatment Responses in Patients With Osteoarthritis: Results From Two Phase III Tanezumab Randomized Clinical Trials
Authors: Colloca Luana , Dworkin Robert H. , Farrar John T. , Tive Leslie , Yang Jiyue , Viktrup Lars , Dasic Gorana , West Christine R. , Whalen Ed , Brown Mark T. , Gilbert Steven A. , Verburg Kenneth M. 
Published: January 2023

Prediction of treatment responses is essential to move forward translational science. Our question was to identify patient‐based variables that predicted responses to treatments. We conducted secondary analyses on pooled data from two randomized phase III clinical trials (NCT02697773 and NCT02709486) conducted in participants with moderate to severe osteoarthritis randomized to subcutaneous placebo (n = 514) or tanezumab 2.5 mg (n = 514). We used gradient boosted regression trees to identify variables that predicted Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain subscale scores at Week 16 and marginal plots to determine the directional relationship between each variable category and responses to placebo or tanezumab within the models. We also used Virtual Twins models to identify potential subgroups of response to the active treatment vs. placebo. We found that responses to placebo were predicted by baseline WOMAC Physical Function, baseline WOMAC Pain, the radiographic classification of the index joint, and the standard deviation of diary pain scores at baseline. In contrast, baseline WOMAC Pain along with failure of prior medications, duration of disease, and standard deviation of diary pain scores at baseline were predictive of tanezumab responses as expressed by the WOMAC Pain scores at Week 16. Those who responded to tanezumab vs. placebo were identified based on the radiographic classification of the index joint and either age or smoking status. These secondary‐data analyses identified distinct and common patient‐based variables to predict response to placebo or tanezumab. These findings will inform the design of future clinical trials, helping to move forward clinical pharmacology and translational science.
Long‐distance and anti‐disturbance wireless power transfer based on concentric three‐coil resonator and inhomogeneous electromagnetic metamaterials
Authors: An Huilin , Yuan Jian , Li Jun , Cao Liqiang 
Published: January 2023

SummaryFor wireless power transfer system (WPTS), the deflection of the resonant coil and the increase of the transmission distance will cause a sharp decline in transmission efficiency. This paper presents a novel long‐distance and anti‐deflection wireless power transfer based on concentric three‐coil resonator and inhomogeneous electromagnetic metamaterials (IEM). First, the effective receiving area of the resonator is analyzed, and the anti‐disturbance concentric three‐coil resonator is designed quantitatively. Considering the magnetic field distribution generated by the transmitting coil, this paper proposes and designs IEM with three kinds of effective permeability, which is applied in different design area, respectively. Meanwhile, the finite‐element‐method simulation proves an improvement in magnetic field modulation and flux leakage control when WPTS with IEM is used. The experimental results show that, compared with the traditional one‐coil to one‐coil, the WPTS designed in this paper achieves an increase of 43% in the efficiency at a 90° deflection. Furthermore, the efficiency of WPTS with IEM is 17% and 7% higher than that of WPTS with homogeneous electromagnetic metamaterials (HEM) and without electromagnetic metamaterials. As a result, the design method in this paper can improve the anti‐disturbance capability and increase the transmission distance and efficiency.
PDE4 inhibitor Roflumilast modulates inflammation and lipid accumulation in PCOS mice to improve ovarian function and reduce DHEA‐induced granulosa cell apoptosis in vitro
Authors: Ji Xiaowei , Ye Yao , Wang Lin , Liu Suying , Dong Xi 
Published: January 2023

AbstractThis study was implemented to address the role of Roflumilast in polycystic ovary syndrome (PCOS) as well as to discuss its reaction mechanism in vivo and in vitro. In vivo, mice were administrated with 6 mg dehydroepiandrosterone (DHEA) per 100 g body weight and fed with 60% high fat diet to induce PCOS. The expression of phosphodiesterases 4 (PDE4) was assessed with RT‐qPCR. The ovary pathology was observed by hematoxylin and eosin staining and follicles were counted. Enzyme‐linked immunosorbent assay was adopted for the estimation of progesterone, testosterone and inflammatory factors and lipid accumulation was observed by Oil Red O staining. With the application of reverse transcription‐quantitative PCR (RT‐qPCR) and western blot, the messenger RNA (mRNA) and protein expressions of low‐density lipoprotein receptor (LDLR) was resolved. In vitro, Cell counting kit‐8 and flow cytometry analysis were applied for the assessment of cell proliferation and apoptosis. The proliferation‐ and apoptosis‐related proteins were appraised with western blot. Additionally, the expressions of PDE‐4 at both mRNA and protein levels were tested with RT‐qPCR and western blot. Here, it was discovered that PDE4 was greatly elevated in PCOS mice and DHEA‐induced ovarian granulosa cells (KGN). In PCOS mice, PDE4 was negative correlated with progesterone and had positive correlation with testosterone. Roflumilast could enhanced progesterone expression, increased the number of primary follicles, preantral follicles and antral follicles but reduced testosterone and decreased the number of cystic follicles in PCOS mice. It was also testified that Roflumilast could inhibit the release of inflammatory factors and lipid accumulation in PCOS mice. Besides, the proliferation of DHEA‐induced KGN cells was enhanced while the apoptosis was declined by Roflumilast, accompanied by elevated contents of PCNA, Ki67 and antiapoptotic protein Bcl‐2. Collectively, Roflumilast inhibited inflammation and lipid accumulation in PCOS mice to improve ovarian function and reduce DHEA‐induced granulosa cell apoptosis.
Guidelines for visualization and analysis of DC in tissues using multiparameter fluorescence microscopy imaging methods
Authors: Bayerl Felix , Bejarano David A. , Bertacchi Giulia , Doffin Anne‐Claire , Gobbini Elisa , Hubert Margaux , Li Lijian , Meiser Philippa , Pedde Anna‐Marie , Posch Wilfried , Rupp Luise , Schlitzer Andreas , Schmitz Marc , Schraml Barbara U. , Uderhardt Stefan , Valladeau‐Guilemond Jenny , Wilflingseder Doris , Zaderer Viktoria , Böttcher Jan P. 
Published: January 2023

AbstractThis article is part of the Dendritic Cell Guidelines article series, which provides a collection of state‐of‐the‐art protocols for the preparation, phenotype analysis by flow cytometry, generation, fluorescence microscopy, and functional characterization of mouse and human dendritic cells (DC) from lymphoid organs and various non‐lymphoid tissues. Here, we provide detailed procedures for a variety of multiparameter fluorescence microscopy imaging methods to explore the spatial organization of DC in tissues and to dissect how DC migrate, communicate, and mediate their multiple functional roles in immunity in a variety of tissue settings. The protocols presented here entail approaches to study DC dynamics and T cell cross‐talk by intravital microscopy, large‐scale visualization, identification, and quantitative analysis of DC subsets and their functions by multiparameter fluorescence microscopy of fixed tissue sections, and an approach to study DC interactions with tissue cells in a 3D cell culture model. While all protocols were written by experienced scientists who routinely use them in their work, this article was also peer‐reviewed by leading experts and approved by all co‐authors, making it an essential resource for basic and clinical DC immunologists.
Norms and COVID‐19 health behaviours: A longitudinal investigation of group factors
Authors: Zhou Haochen , Cárdenas Diana , Reynolds Katherine J. 
Published: January 2023

AbstractMost studies on norms and COVID‐19 have ignored the group‐based and dynamic nature of normative influence where self‐relevant and salient groups might emerge and change along with their impact on health behaviours. The current research seeks to explore these issues using a three‐wave longitudinal design with a representative sample of Australians (Nwave 1 = 3024) where two group sources of potential normative influence (neighbourhood and national groups) and two COVID‐19 health behaviours (physical distancing and hand hygiene) were investigated in May, June/July and September/October 2020. Results indicated that especially from Wave 1 to Wave 2 neighbourhood descriptive norms (rather than national or injunctive norms) had the most impact on health behaviours while controlling for demographic and individual‐level health variables. This demonstrates that groups and associated norms that influence behaviours vary across time. It is concluded that research on norms needs to study which groups matter and when.
Susceptibility of Salmonella serotypes isolated from meat and meat contact surfaces to thermal, acidic, and alkaline treatments and disinfectants
Authors: Manafi Leila , Aliakbarlu Javad , Dastmalchi Saei Habib 
Published: January 2023

AbstractThe present study was conducted to evaluate the response of 29 Salmonella isolates to exposure to thermal (60°C for 2 min), acidic (pH 2.9 for 30 min), and alkaline (pH 11 for 60 min) treatments and investigate the susceptibility of the isolates and their biofilms to disinfectants. The reductions of Salmonella isolates populations subjected to each treatment were analyzed according to their isolation source, serotype, antibiotic resistance pattern, and biofilm formation ability. Median reductions for all of Salmonella isolates populations after thermal, acidic, and alkaline treatments were 1.8, 2.1, and 0.7 log CFU/ml, respectively. The isolates behavior under stress conditions were not related to their isolation source, serotype, or biofilm formation ability. The median reduction after alkaline treatment in non‐MDR (multidrug‐ resistant) isolates populations was significantly (p < .05) higher than MDR isolates. The median reduction in biofilms of moderate biofilm producers by disinfectants was significantly (p < .05) higher than that of strong biofilm producers. In conclusion, Salmonella isolates showed the highest susceptibility to acidic treatment and MDR isolates were more resistant to alkaline treatment than non‐MDR ones. The current study also revealed that the strong biofilm producer isolates were more resistant to disinfectants than moderate biofilm producers. This study facilitated the understanding of the relationship between Salmonella characteristics (isolation source, serotype, antibiotic resistance pattern, and biofilm formation ability) and its susceptibility to thermal, acidic, and alkaline treatments and disinfectants. The findings are helpful for the prevention and control of Salmonella.
Yes‐associated protein regulates glutamate homeostasis through promoting the expression of excitatory amino acid transporter‐2 in astrocytes via β‐catenin signaling
Authors: Xu Xingxing , Wang Jiaojiao , Du Siyu , Shen Xiya , Lian Jiashu , Zhou Jian , Wang Mianxian , Feng Wenjin , Lv Zhaoting , Zhu Junzhe , Jin Lingting , Sun Huankun , Wu Lihao , Wang Xiaoning , Qiu Haoyu , Wang Wei , Teng Honglin , Wang Ying , Huang Zhihui 
Published: January 2023

AbstractThe homeostasis of glutamate is mainly regulated by the excitatory amino acid transporters (EAATs), especially by EAAT2 in astrocytes. Excessive glutamate in the synaptic cleft caused by dysfunction or dysregulation of EAAT2 can lead to excitotoxicity, neuronal death and cognitive dysfunction. However, it remains unclear about the detailed regulation mechanism of expression and function of astrocytic EAAT2. In this study, first, we found increased neuronal death and impairment of cognitive function in YAPGFAP‐CKO mice (conditionally knock out Yes‐associated protein [YAP] in astrocytes), and identified EAAT2 as a downstream target of YAP through RNA sequencing. Second, the expression of EAAT2 was decreased in cultured YAP−/− astrocytes and the hippocampus of YAPGFAP‐CKO mice, and glutamate uptake was reduced in YAP−/− astrocytes, but increased in YAP‐upregulated astrocytes. Third, further investigation of the mechanism showed that the mRNA and protein levels of β‐catenin were decreased in YAP−/− astrocytes and increased in YAP‐upregulated astrocytes. Wnt3a activated YAP signaling and up‐regulated EAAT2 through β‐catenin. Furthermore, over‐expression or activation of β‐catenin partially restored the downregulation of EAAT2, the impairment of glutamate uptake, neuronal death and cognitive decline that caused by YAP deletion. Finally, activation of EAAT2 also rescued neuronal death and cognitive decline in YAPGFAP‐CKO mice. Taken together, our study identifies an unrecognized role of YAP signaling in the regulation of glutamate homeostasis through the β‐catenin/EAAT2 pathway in astrocytes, which may provide novel insights into the pathogenesis of brain diseases that closely related to the dysfunction or dysregulation of EAAT2, and promote the development of clinical strategy.
An event‐based magnetoencephalography study of simulated driving: Establishing a novel paradigm to probe the dynamic interplay of executive and motor function
Authors: Walshe Elizabeth A. , Roberts Timothy P. L. , Ward McIntosh Chelsea , Winston Flaura K. , Romer Dan , Gaetz William 
Published: January 2023

AbstractMagnetoencephalography (MEG) is particularly well‐suited to the study of human motor cortex oscillatory rhythms and motor control. However, the motor tasks studied to date are largely overly simplistic. This study describes a new approach: a novel event‐based simulated drive made operational via MEG compatible driving simulator hardware, paired with differential beamformer methods to characterize the neural correlates of realistic, complex motor activity. We scanned 23 healthy individuals aged 16–23 years (mean age = 19.5, SD = 2.5; 18 males and 5 females, all right‐handed) who completed a custom‐built repeated trials driving scenario. MEG data were recorded with a 275‐channel CTF, and a volumetric magnetic resonance imaging scan was used for MEG source localization. To validate this paradigm, we hypothesized that pedal‐use would elicit expected modulation of primary motor responses beta‐event‐related desynchronization (B‐ERD) and movement‐related gamma synchrony (MRGS). To confirm the added utility of this paradigm, we hypothesized that the driving task could also probe frontal cognitive control responses (specifically, frontal midline theta [FMT]). Three of 23 participants were removed due to excess head motion (>1.5 cm/trial), confirming feasibility. Nonparametric group analysis revealed significant regions of pedal‐use related B‐ERD activity (at left precentral foot area, as well as bilateral superior parietal lobe: p < .01 corrected), MRGS (at medial precentral gyrus: p < .01 corrected), and FMT band activity sustained around planned braking (at bilateral superior frontal gyrus: p < .01 corrected). This paradigm overcomes the limits of previous efforts by allowing for characterization of the neural correlates of realistic, complex motor activity in terms of brain regions, frequency bands and their dynamic temporal interplay.
Time trends in treatment patterns and survival of older patients with synchronous metastatic colorectal cancer in the Netherlands: A population‐based study
Authors: Baltussen Joosje C. , de Glas Nienke A. , Liefers Gerrit‐Jan , Slingerland Marije , Speetjens Frank M. , van den Bos Frederiek , Cloos‐van Balen Marissa , Verschoor Arjan J. , Jochems Anouk , Spierings Leontine E. A. M. M. , Holterhues Cynthia , van Gerven Leander A. , Mooijaart Simon P. , Portielje Johanneke E. A. , Derks Marloes G. M. 
Published: January 2023

AbstractNew treatment strategies have improved survival of metastatic colorectal cancer in trials. However, it is not clear whether older patients benefit from these novel therapies, as they are often not included in pivotal trials. Therefore, we investigated treatment patterns and overall survival over time in older patients with metastatic colorectal cancer in a population‐based study. We identified 22.192 Dutch patients aged ≥70 years diagnosed with synchronous metastatic colorectal cancer between 2005 and 2020 from the Netherlands Cancer Registry. Changes in treatment over time were assessed with logistic regression models. Survival was assessed by Cox proportional hazard ratios (HR). Results showed that chemotherapy use increased between 2005 and 2015, but declined from 2015 onwards, while more patients received best supportive care. Over time, fewer patients underwent primary tumor resection alone. Although survival of both metastatic colon and rectal cancer improved until 2014, survival of colon cancer decreased from 2014 onwards (HR 1.04, 95% confidence interval [CI] 1.01‐1.05), which was seen in all age groups. Survival of metastatic rectal cancer patients remained unchanged from 2014 onwards (HR 1.00, 95% CI 0.98‐1.03) in all age groups. In conclusion, treatment patterns of Dutch older patients with synchronous metastatic colorectal cancer rapidly changed from 2005 to 2020, with increasing percentages of patients receiving best supportive care. Survival of metastatic colon cancer decreased from 2014 onwards. The implementation of a colorectal cancer screening program and patient selection might explain why only a subset of older patients seem to benefit from the availability of novel treatment options.