Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones

A series of biorelevant triethylammonium isatin hydrazones containing various substituents in the aromatic fragment have been synthesized. Their structure and composition were confirmed by NMR- and IR-spectroscopies, mass-spectrometry and elemental analysis. It was found that some representatives show activity against Staphylococcus aureus and Bacillus cereus higher or at the level of norfloxacin, including methicillin-resistant Staphylococcus aureus strains. The study also showed low hemo- and cytotoxicity (Chang Liver) and high antiaggregatory and anticoagulant activity of these compounds. The high potential of new ammonium isatin-3-acylhydrazones in the search for antimicrobial activity against phytopathogens of bacterial and fungal nature has been shown for the first time.

EVALUATION OF ANALGESIC EFFECT OF TAB TRAILOKYA VIJAYA VATI IN POST-OPERATIVE PAIN IN KSHARKARMA PATIENTS: AN OBSERVATIONAL STUDY

Despite the advances in technology and robotics, the basics of surgical management are not changed drastically. The science of life, Ayurveda has extensive knowledge of surgeries, including complicated procedures mentioned in the classical texts. However, with time, the ability of anaesthetics and analgesic agents has been lost. This resulted in the lagging of Ayurvedic Surgical wisdom and the rise of modern analgesics and anaesthetics in the market. These current products have potential side effects, and hence a safer and better alternative to these products can boost Ayurveda Surgery worldwide. Trailokya Vijaya Vati (TVV) is one such Ayurvedic formulation that is explained for its potent analgesic activity. The present study was conducted to evaluate the safety and efficacy of TVV in post-operative pain management in patients undergoing anorectal procedures. The observational trial suggested a reduction in time to sleep (p < 0.05), less incidence of insomnia and undisturbed sleep in the treatment group than the control. The formulation was also well tolerated with no or minimal requirement of rescue analgesics. The efficacy observed in the study suggests the formulation can be explored further on a larger population with a diverse activity profile.

Mansouramycins E–G, Cytotoxic Isoquinolinequinones from Marine Streptomycetes

Chemical investigation of the ethyl acetate extract from the marine-derived Streptomyces sp. isolate B1848 resulted in three new isoquinolinequinone derivatives, the mansouramycins E–G (1a–3a), in addition to the previously reported mansouramycins A (5) and D (6). Their structures were elucidated by computer-assisted interpretation of 1D and 2D NMR spectra, high-resolution mass spectrometry, and by comparison with related compounds. Cytotoxicity profiling of the mansouramycins in a panel of up to 36 tumor cell lines indicated a significant cytotoxicity and good tumor selectivity for mansouramycin F (2a), while the activity profile of E (1a) was less attractive.

A Multiparametric Activity Profiling Platform for Neuron Disease Phenotyping and Drug Screening

Patient stem cell-derived models enable imaging of complex disease phenotypes and the development of scalable drug discovery platforms. Current preclinical methods for assessing cellular activity do not, however, capture the full intricacies of disease-induced disturbances, and instead typically focus on a single parameter, which impairs both the understanding of disease and the discovery of effective therapeutics. Here, we describe a cloud-based image processing and analysis platform that captures the intricate activity profile revealed by GCaMP fluorescent recordings of intracellular calcium changes and enables the discovery of molecules that correct 153 parameters that define the amyotrophic lateral sclerosis motor neuron disease phenotype. In a high-throughput screen, we identified compounds that revert the multiparametric disease profile to that found in healthy cells, a novel and robust measure of therapeutic potential quite distinct from unidimensional screening. This platform can guide the development of therapeutics that counteract the multifaceted pathological features of diseased cellular activity.

Tracking Systems Used to Monitor the Performance and Activity Profile in Elite Team Sports

Technology has become established in elite sport in recent years and is used on a regular basis, especially in team sports [...]

Clustering Accelerometer Activity Patterns from the UK Biobank Cohort

Many researchers are beginning to adopt the use of wrist-worn accelerometers to objectively measure personal activity levels. Data from these devices are often used to summarise such activity in terms of averages, variances, exceedances, and patterns within a profile. In this study, we report the development of a clustering utilising the whole activity profile. This was achieved using the robust clustering technique of k-medoids applied to an extensive data set of over 90,000 activity profiles, collected as part of the UK Biobank study. We identified nine distinct activity profiles in these data, which captured both the pattern of activity throughout a week and the intensity of the activity: “Active 9 to 5”, “Active”, “Morning Movers”, “Get up and Active”, “Live for the Weekend”, “Moderates”, “Leisurely 9 to 5”, “Sedate” and “Inactive”. These patterns are differentiated by sociodemographic, socioeconomic, and health and circadian rhythm data collected by UK Biobank. The utility of these findings are that they sit alongside existing summary measures of physical activity to provide a way to typify distinct activity patterns that may help to explain other health and morbidity outcomes, e.g., BMI or COVID-19. This research will be returned to the UK Biobank for other researchers to use.

The DOMINO web-server for active module identification analysis

Active module identification (AMI) is an essential step in many omics analyses. Such algorithms receive a gene network and a gene activity profile as input and report subnetworks that show significant over-representation of accrued activity signal ("active modules"). Such modules can point out key molecular processes in the analyzed biological conditions. We recently introduced a novel AMI algorithm called DOMINO, and demonstrated that it detects active modules that capture biological signals with markedly improved rate of empirical validation. Here, we provide an online server that executes DOMINO, making it more accessible and user-friendly. To help the interpretation of solutions, the server provides GO enrichment analysis, module visualizations, and accessible output formats for customized downstream analysis. It also enables running DOMINO with various gene identifiers of different organisms. The server is available at http://domino.cs.tau.ac.il. Its codebase is available at https://github.com/Shamir-Lab.