bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis, Computational Studies, and Biological Evaluation of Sulpha-methoxazole-Based Schiff Bases as Antimicrobial Agents
Authors: Kumar Sushil , Haider Mohd 
Published: September 2024

Background:
Sulphamethoxazole-based Schiff-base compounds display poten-tial antibacterial and antifungal activity. Sulphamethoxazole is considered to be a versatile pharmacophore that can be utilized for designing and developing numerous bioactive lead compounds. In this work, some new sulphamethoxazole-based Schiff base compounds were synthesized, which are expected to possess antimicrobial activity, making them potentially useful for treating microbial infections.

Objective:
Concerning issues of drug resistance in presently available drugs, this study aimed to synthesize new sulphamethoxazole-based Schiff bases and evaluate their antimi-crobial activity.

Methods:
New sulphamethoxazole-based Schiff bases were synthesized by condensing sul-phamethoxazole with various acetophenones in methanol in the presence of glacial acetic acid. The synthesized compounds were characterized using various techniques, such as TLC, melting point, IR, NMR, and mass analysis. The computational properties of the com-pounds were also assessed using online software programs, and the similarity of the target compounds was also calculated as compared to sulphamethoxazole and clotrimazole. The antimicrobial activity of the target compounds was tested against Bacillus subtilis (Gram-positive), Escherichia coli (Gram-negative), and Candida albicans.

Results:
The target compounds (3a-f) were successfully synthesized and characterized by spectroscopic and analytical methods. The results of computational properties, similarity, and antimicrobial activity against B. subtilis, E. coli, and C. albicans of new sulphamethox-azole-based Schiff bases showed significant antimicrobial potential.

result:
The results of computational properties, similarity and antimicrobial activity against B. subtilis, E. coli and C. albicans of new sulphamethoxazole based Schiff bases showed significant antimicrobial potential.

Conclusion:
The synthesized new Schiff bases, particularly compound 3c, exhibited prom-ising antimicrobial activity and good physicochemical properties as compared to standard drugs, indicating their potential for further development as antimicrobial agents.
Crack Growth Behavior in Metal-elastomer Bonding Interface under Cyclic Deformation
Authors: Chen Xuming , Zonoz Ray , Salem Hamid 
Published: September 2024

Introduction:
Metal-elastomer adhesion becomes increasingly important for elastomer
parts comprising metal components, such as packer elements for Blowout Preventers (BOP),
completion packers, metal encapsulated seals, and stator/rotors. As the bonding between metal
and elastomer deteriorates under cyclic deformation, cracks can appear on the adhesion interface
and reduce the function of the parts.

Methods:
Thus, the fatigue performance or crack growth rate of the metal-elastomer adhesion
affects the service life of the whole elastomer part. In this study, the metal-elastomer bonded
parts were fabricated and evaluated under cyclic shear and peel deformation at both room temperature
and high temperature.

Results:
The crack growth rates (dc/dN) on the metal-elastomer interface were measured based
on the strain energy release rate (Gc) for different elastomers with both excellent and poor adhesion,
and the API lifetime of BOP packers were therefore estimated.

Conclusion:
The results indicated that the crack growth rates in the adhesion interface can be
correlated with the API lifetime of BOP packers, and the elastomer with a low crack growth rate
will have a better fatigue life for the BOP application.
Predicting Adherence to Computer-Based Cognitive Training Programs Among Older Adults: Study of Domain Adaptation and Deep Learning
Authors: Singh Ankita , Chakraborty Shayok , He Zhe , Pang Yuanying , Zhang Shenghao , Subedi Ronast , Lustria Mia Liza , Charness Neil , Boot Walter 
Published: September 2024

Abstract

Background
Cognitive impairment and dementia pose a significant challenge to the aging population, impacting the well-being, quality of life, and autonomy of affected individuals. As the population ages, this will place enormous strain on health care and economic systems. While computerized cognitive training programs have demonstrated some promise in addressing cognitive decline, adherence to these interventions can be challenging.

Objective
The objective of this study is to improve the accuracy of predicting adherence lapses to ultimately develop tailored adherence support systems to promote engagement with cognitive training among older adults.

Methods
Data from 2 previously conducted cognitive training intervention studies were used to forecast adherence levels among older participants. Deep convolutional neural networks were used to leverage their feature learning capabilities and predict adherence patterns based on past behavior. Domain adaptation (DA) was used to address the challenge of limited training data for each participant, by using data from other participants with similar playing patterns. Time series data were converted into image format using Gramian angular fields, to facilitate clustering of participants during DA. To the best of our knowledge, this is the first effort to use DA techniques to predict older adults’ daily adherence to cognitive training programs.

Results
Our results demonstrated the promise and potential of deep neural networks and DA for predicting adherence lapses. In all 3 studies, using 2 independent datasets, DA consistently produced the best accuracy values.

Conclusions
Our findings highlight that deep learning and DA techniques can aid in the development of adherence support systems for computerized cognitive training, as well as for other interventions aimed at improving health, cognition, and well-being. These techniques can improve engagement and maximize the benefits of such interventions, ultimately enhancing the quality of life of individuals at risk for cognitive impairments. This research informs the development of more effective interventions, benefiting individuals and society by improving conditions associated with aging.
An Electronic Medical Record–Based Prognostic Model for Inpatient Falls: Development and Internal-External Cross-Validation
Authors: Parsons Rex , Blythe Robin , Cramb Susanna , Abdel-Hafez Ahmad , McPhail Steven 
Published: September 2024

Background
Effective fall prevention interventions in hospitals require appropriate allocation of resources early in admission. To address this, fall risk prediction tools and models have been developed with the aim to provide fall prevention strategies to patients at high risk. However, fall risk assessment tools have typically been inaccurate for prediction, ineffective in prevention, and time-consuming to complete. Accurate, dynamic, individualized estimates of fall risk for admitted patients using routinely recorded data may assist in prioritizing fall prevention efforts.

Objective
The objective of this study was to develop and validate an accurate and dynamic prognostic model for inpatient falls among a cohort of patients using routinely recorded electronic medical record data.

Methods
We used routinely recorded data from 5 Australian hospitals to develop and internally-externally validate a prediction model for inpatient falls using a Cox proportional hazards model with time-varying covariates. The study cohort included patients admitted during 2018-2021 to any ward, with no age restriction. Predictors used in the model included admission-related administrative data, length of stay, and number of previous falls during the admission (updated every 12 hours up to 14 days after admission). Model calibration was assessed using Poisson regression and discrimination using the area under the time-dependent receiver operating characteristic curve.

Results
There were 1,107,556 inpatient admissions, 6004 falls, and 5341 unique fallers. The area under the time-dependent receiver operating characteristic curve was 0.899 (95% CI 0.88-0.91) at 24 hours after admission and declined throughout admission (eg, 0.765, 95% CI 0.75-0.78 on the seventh day after admission). Site-dependent overestimation and underestimation of risk was observed on the calibration plots.

Conclusions
Using a large dataset from multiple hospitals and robust methods to model development and validation, we developed a prognostic model for inpatient falls. It had high discrimination, suggesting the model has the potential for operationalization in clinical decision support for prioritizing inpatients for fall prevention. Performance was site dependent, and model recalibration may lead to improved performance.
The effectiveness of psychotherapies in reducing further suicide attempts: a systematic review with meta-analysis of randomized controlled trials
Authors: Santos Luciana Almeida , Teodoro Maycoln Leôni Martins , De Oliveira Fellipe Couto 
Published: September 2024

There is little evidence on the effectiveness of psychotherapeutic interventions in reducing new suicide attempts. This article aims to evaluate the effectiveness of psychotherapeutic interventions in reducing suicide attempts among patients with a history of previous attempts. We selected 17 articles from four databases: PubMed, Cochrane, APA PsycInfo and LILACS, in 2023. Six studies showed statistical differences that favored psychotherapeutic intervention at some point during the follow-up period. These psychotherapies addressed: problem-solving, hope induction, skills training. When comparing psychotherapy with usual care, a meta-analysis revealed an odds ratio of 0.41 (95 % CI, 0.17-0.99, p = .05) in the analysis up to 12 months of follow-up, and an odds ratio of 0.48 (95 % CI, 0.30-0.78, p < .001) after 12 months of follow-up. The results indicate the efficacy of these interventions in reducing additional suicide attempts, but they should be analyzed with caution, given the heterogeneity of the sample, treatments, and comparators. This review supports the development of prevention strategies indicated for patients who have attempted suicide.
AKTIVITAS ANTIFUNGI EKSTRAK DAUN Asystasia gangetica (L.) T. Anderson TERHADAP BIBIT KELAPA SAWIT (Elaeis guineensis Jacq.) TERINFEKSI Ganoderma boninense
Authors: Saragih Wismaroh Sanniwati 
Published: September 2024

Aktivitas antijamur ekstrak daun Asystasia gangetica (L.) T. Anderson diketahui mengandung senyawa kimia flavonoid, alkaloid, terpenoid, tanin, dan saponin yang berfungsi sebagai antijamur. Sementara itu senyawa kimia daun pada tanaman yang dapat bersifat antijamur terhadap Ganoderma boninense pada tanaman kelapa sawit diperoleh dengan cara ekstraksi. Oleh karena itu, penelitian ini bertujuan untuk mengetahui potensi ekstrak daun A. gangetica sebagai antijamur pada tanaman kelapa sawit yang disebabkan oleh patogen G. boninense. Penelitian dilakukan di rumah kaca dengan metode rancangan acak lengkap non faktorial pada taraf nyata 95%. Pengujian konsentrasi ekstrak daun A. gangetica 1 mg/mL, 2 mg/mL, 4 mg/mL, dan 8 mg/mL sebanyak 50 mL/tanaman menggunakan teknik siram keliling. Hasil penelitian menunjukkan pemberian ekstrak daun A. gangetica pada tanaman terinfeksi umur 8 bulan setelah inokulasi dosis 8 mg/mL dapat memacu pertumbuhan vegetatif tanaman, yaitu: tinggi tanaman (78,7 cm), jumlah daun (11,3 helai), diameter batang (25,7 mm), dan jumlah klorofil daun 57 SPAD (Soil Plant Analyses Development), rata-rata kejadian penyakit (11,12%), dan keparahan penyakit (7,88%). Analisis histologis akar tanaman yang terinfeksi menunjukkan di sel parenkim dari ikatan pembuluh telah hancur, tetapi bibit kelapa sawit yang diberi ekstrak daun A. gangetica memiliki sel yang utuh, dan sehat. Aktivitas antijamur metabolit sekunder A. gangetica berpotensi menekan perkembangan patogen G. boninense pada bibit kelapa sawit di rumah kaca.
Enhanced biomedical potential of polyurethane/hydroxyapatite composites through chemical modification: A comprehensive study on structure, morphology, and cytocompatibility for tissue regeneration
Authors: Sultan Misbah , Parveen Shaista , Uddin Mohammad N. , Jubeen Farhat , Kazi Mohsin 
Published: September 2024

Abstract
Polyurethane/hydroxyapatite (PU/HA) composites are well-known for various biomedical applications. This study reports a chemical approach to improve the interaction between HA and PU matrix. HA was surface-modified with 1,6-hexamethylene diisocyanate (HMDI). First, an isocyanate-modified HA (IHA) was synthesized by hydro-thermal method. Second, IHA was incorporated into a separately synthesized thermoplastic PU by a solvent casting technique. A series of PU/IHA composites was prepared by varying PU᾿s soft and hard segments. The IHA was added to PU (5 and 10 %). The FTIR spectra exhibited characteristic bands of urethane and HA, confirming the synthesis of the composites. XRD study showed the crystallite size of IHA (20 Å) with hexagonal geometry and an amorphous to semicrystalline nature of composites. SEM showed that composites displayed porous and granular morphology. The TGA thermograms of the composites revealed the thermal stability up to 400 °C. The IHA addition considerably improved hydrophilicity and degradation of the composites in simulated body fluid (SBF). MTT assay revealed improved cytocompatibility (> 80 %) of the composites. These results demonstrated an appreciable improvement in structure, morphology, hydrophilicity, degradation, and cytocompatibility of PU/IHA composites by chemical modification of HA. Hence, these composites possess remarkable potential for biomedical applications such as tissue regeneration.
Alternative buffer systems in biopharmaceutical formulations and their effect on protein stability
Authors: Lebar Blaž , Zidar Mitja , Mravljak Janez , Šink Roman , Žula Aleš , Pajk Stane 
Published: September 2024

Abstract
The formulation of biopharmaceutical drugs is designed to eliminate chemical instabilities, increase conformational and colloidal stability of proteins, and optimize interfacial stability. Among the various excipients involved, buffer composition plays a pivotal role. However, conventional buffers like histidine and phosphate buffers may not always be the optimal choice for all monoclonal antibodies (mAbs). In this study, we investigated the effects of several alternative buffer systems on seven different mAbs, exploring various combinations of ionic strengths, concentrations of the main buffer component, mAb concentrations, and stress conditions. Protein stability was assessed by analyzing soluble aggregate formation through size exclusion chromatography. At low protein concentrations, protein instability after temperature stress was exclusively observed in the bis-TRIS/ glucuronate buffer. Conversely, freeze-thaw stress led to a significant increase in aggregate formation in tested formulations, highlighting the efficacy of several alternative buffers, particularly arginine/ citrate, in preserving protein stability. Under temperature stress, the introduction of arginine to histidine buffer systems provided additional stabilization, while the addition of lysine resulted in protein destabilization. Similarly, the incorporation of arginine into histi-dine/HCl buffer further enhanced protein stability during freeze--thaw cycles. At high protein concentrations, the histidine/citrate buffer emerged as one of the most optimal choices for addressing temperature and light-induced stress. The efficacy of histidine buffers in combating light stress might be attributed to the light-absorbing properties of histidine molecules. Our findings demonstrate that the development of biopharmaceutical formulations should not be confined to conventional buffer systems, as numerous alternative options exhibit comparable or even superior performance.
Synthesis and biochemical evaluation of new 3-amido-4-substituted monocyclic ß-lactams as inhibitors of penicillin-binding protein(s)
Authors: Grabrijan Katarina , Benedik Nika Strašek , Krajnc Alen , Bozovičar Krištof , Knez Damijan , Proj Matic , Zdovc Irena , Sosič Izidor , Contreras-Martel Carlos , Dessen Andréa , Rambaher Martina Hrast , Gobec Stanislav 
Published: September 2024

Abstract
In the final phases of bacterial cell wall synthesis, penicillin-binding proteins (PBPs) catalyze the cross-linking of peptidoglycan. For many decades, effective and non-toxic β-lactam antibiotics have been successfully used as mimetics of the d-Ala-d-Ala moiety of the natural substrate and employed as irreversible inhibitors of PBPs. In the years following their discovery, the emergence of resistant bacteria led to a decline in their clinical efficacy. Using Staudinger cycloaddition, we synthesized a focused library of novel monocyclic β-lactams in which different substituents were introduced at the C4 position of the β-lactam ring, at the C3 amino position, and at the N1 lactam nitrogen. In biochemical assays, the compounds were evaluated for their inhibitory effect on the model enzyme PBP1b from Streptococcus pneumoniae. Upon investigation of the antibacterial activity of the newly prepared compounds against ESKAPE pathogens, some compounds showed moderate inhibition. We also examined their reactivity and selectivity in a biochemical assay with other enzymes that have a catalytic serine in the active site, such as human cholinesterases, where they also showed no inhibitory activity, highlighting their specificity for bacterial targets. These compounds form the basis for further work on new monocyclic β-lactams with improved antibacterial activity.
The tyrosine kinase inhibitor lenvatinib is oxidized by rat cytochromes P450 and affects their expression in rat liver
Authors: Indra Radek , Jelínková Sandra , Kollárová Katarína , Zahumenská Petra , Dvořák Josef , Dušková Šárka , Dračínská Helena 
Published: September 2024

Abstract
Lenvatinib is an orally effective tyrosine kinase inhibitor used to treat several types of tumors, including progressive, radioiodine-refractory differentiated thyroid cancer and advanced renal cell carcinoma. Although this drug is increasingly used in therapy, its metabolism and effects on the organism are still not described in detail. Using the rat as an experimental animal model, this study aimed to investigate the metabolism of lenvatinib by rat microsomal enzymes and cytochrome P450 (CYPs) enzymes recombinantly expressed in SupersomesTM
in vitro and to assess the effect of lenvatinib on rat CYP expression in vivo. Two metabolites, O-desmethyl lenvatinib, and lenvatinib N-oxide, were produced by rat CYPs in vitro. CYP2A1 and 2C12 were found to be the most effective in forming O-desmethyl lenvatinib, while CYP3A2 was found to primarily form lenvatinib N-oxide. The administration of lenvatinib to rats caused changes in the expression of mRNA and protein, as well as the activity of various CYPs, particularly in an increase in CYP1A1. Thus, the administration of lenvatinib to rats has an impact on the level of CYPs.
PPIA, HRPT1, and PGK1 genes as the appropriate combination for RT-qPCR normalization in alveolar and femoral bone remodeling in olanzapine-treated rats
Authors: Disha-Ibrahimi Saranda , Drevenšek Gorazd , Drevenšek Martina , Marc Janja , Žitnik Irena Prodan 
Published: September 2024

Abstract
Reliable gene expression analysis in bone remodeling studies requires an appropriate selection of internal controls, i.e. stable reference genes for the normalization of quantitative real-time PCR (RT-qPCR), the most common method used for quantifying gene expression measurements. Even the most widely used reference genes can have variable expression under different experimental conditions, or in different tissue types or treatment regimes, so selecting appropriate controls is a key step in ensuring reliable results. The aim of this research was to identify the most stable reference gene(s) for the study of olanzapine modulated bone remodeling in rats. RNA was isolated from the maxillary alveolar and femoral bones of olanzapine or placebo-treated Wistar rats and transcribed to cDNA. The expression of 12 candidate reference genes was assessed by RT-qPCR. Their expressions were analysed using GeNorm, NormFinder, BestKeeper and delta Ct algorithms, and by the comprehensive ranking method. PPIA, HRPT1 and PGK1 were the most stably expres sed reference genes and the combination of the three genes was optimal for normalization. This study is the first to identify the optimal reference genes for research in olanzapine-exposed rats, which serve as a pivotal benchmark for enhancing the accuracy and reliability of future RT-qPCR expression in bone studies.
Association of Cartilage, Synovial Fluid and Membrane Pathological Findings in Serbian Mountain Horses Without Signs of Lameness
Authors: Marković Lazar , Radaković Milena , Radovanović Anita , Andrić Jelena Francuski , Đoković Stefan , Milošević Ivan , Kovačević Filipović Milica 
Published: September 2024

Abstract
Osteoarthritis (OA) in horses often affects the metacarpal/metatarsophalangeal (MCP/MTP) joints and its detection in the early stages is crucial for effective management. I t was hypothesized that the extent of cartilage damage positively correlates with synovial membrane (SM) and synovial fluid (SF) pathological findings in the MCP/MTP joints of Serbian mountain horses that transported heavy loads but did not show signs of lameness. The study was conducted on 32 MCP/MTP joints of eight horses between seven to 12 years of age. Horse limbs were transferred from the abattoir to the necropsy room and SF was sampled. Its appearance, total nucleated cell count (TNCC), mononuclear cell count (MNC), total proteins (TP), and haptoglobin (Hp) were determined. Samples of SM were collected from the dorsal palmar/plantar pouch for histology. A macroscopic examination of gross condylar pathology of the third metacarpal/metatarsal bone was performed with Indian Ink staining. Scoring was done based on Osteoarthritis Research Society International recommendations. SF was clear, pale yellow, and mostly fairly viscous. Half of the samples had TNCC above, and all had TP within the reference range. Hp values were below the reference range and were omitted from further analyses. TNCC correlated with MNC (ρs=0.81, P<0.001), microscopic (ρs=0.62, P=0.003) and macroscopic scores (ρs=0.47, P=0.008). In addition, MNC correlated with macroscopic scores (ρs=0.40, P=0.03). All pathological findings were mild and their correlation indicated that these processes are interrelated and that could be ascribed to early OA.
Development of a Simple and Rapid DNA Extraction Method for Aspergillus flavus
Authors: Sanioğlu Gölen Gökçenur , Akar Kadir 
Published: September 2024

Abstract

Aspergillus species are known to be very important in human and domestic animal health. Aspergillus species commonly cause severe systemic and skin infections, as well as allergic lung diseases. With the development of PCR techniques, these methods are used to identify and diagnose fungi. DNA extraction from Aspergillus species is difficult because the fungal cell wall structure is very durable and complex. Fungal DNA extraction methods containing proteinase K and liquid nitrogen are widely used to break down the cell wall. However, these methods cause DNA loss during the extraction in Aspergillus species. In this study, on the contrary, the commonly used DNA extraction by means of ammonium hydroxide, which is generally used to break down chitin in DNA extraction of ticks and plants, is used. The efficiency of the cell wall lysis method from A. flavus with ammonium hydroxide was compared with methods containing proteinase K and liquid nitrogen. For this purpose, DNA extraction of A. flavus was tried using three different methods. As a result, the cell wall of A. flavus was lysed using ammonium hydroxide in this study. The obtained DNA’s quality, concentration, and PCR performance were sufficient. This method has been evaluated as a faster, more straightforward, and more economical alternative.