“ Thioureidopeptide”: Novel Synthon for the Synthesis of N, N′, N″-Trisubstituted Guanidinopeptide Mimics

The synthesis of N α-protected N,N′,N″-trisubstituted guanidinopeptide mimic molecules suitably decorated in peptide backbone has been delineated in one pot employing HgCl2 as a desulphurizing agent. Chiral N α -protected thioureidopeptide esters were employed as synthons for the synthesis of title molecules. The protocol is simple and the reaction conditions employed were mild, amenable to the amino acid chemistry

4(2) 50 Case Study Dapsone Hypersensitivity Syndrome in a Leprosy Patient

ABSTRACT Introduction: Dapsone Hypersensitivity Syndrome (DHS) is a rare potentially fatal systemic idiosyncratic adverse reaction, with multiorgan involvement also known as sulphone syndrome which is particularly seen in leprosy patients who are on world health organization recommended multidrug therapy (WHO-MDT regimen). DHS is a variant of drug rash with eosinophilia and systemic symptoms (DRESS syndrome) caused by dapsone. Even though reaction common in the leprosy patients there is need such reporting to identify the most venerable patient pool. Case: Here we present a case of DHS developed after 25 days in a female patient with a history of PB-MDT regimen treatment, high grade intermittent fever associated with nausea, myalgia, headache since 20 days; swelling of face, bilateral lower limbs and erythematous rashes were observed all over the body since 4 days. She was presented with fever (102.2 0 F), posterior cervical and axillary lymphadenopathy and moderate bilateral lower limb pitting pedal edema was present. Multiple erythematous papules coalesced all over body predominantly involved on the face, trunk and extremities. The main laboratory data on admission were showed, hemoglobin: 9.6 g/dL; WBC: 14.6 x 10³/ µL; neutrophils: 48% mild left shift, lymphocyte: 20% reactive forms; eosinophils: 16%; increased serum levels of aspartate amino transferase, alanine transaminase and alkaline phosphatase. Patient was improved and discharged on treating with antipyretics, antibiotics, oral and topical corticosteroids and antihistamines

Fermentation, Isolation, Structure, and antidiabetic activity of NFAT-133 produced by Streptomyces strain PM0324667

Type-2 diabetes is mediated by defects in either insulin secretion or insulin action. In an effort to identify extracts that may stimulate glucose uptake, similar to insulin, a high throughput-screening assay for measuring glucose uptake in skeletal muscle cells was established. During the screening studies to discover novel antidiabetic compounds from microbial resources a Streptomyces strain PM0324667 (MTCC 5543, the Strain accession number at Institute of Microbial Technology, Chandigarh, India), an isolate from arid soil was identified which expressed a secondary metabolite that induced glucose uptake in L6 skeletal muscle cells. By employing bioactivity guided fractionation techniques, a tri-substituted simple aromatic compound with anti-diabetic potential was isolated. It was characterized based on MS and 2D NMR spectral data and identified as NFAT-133 which is a known immunosuppressive agent that inhibits NFAT-dependent transcription in vitro. Our investigations revealed the antidiabetic potential of NFAT-133. The compound induced glucose uptake in differentiated L6 myotubes with an EC50 of 6.3 ± 1.8 μM without activating the peroxisome proliferator-activated receptor-γ. Further, NFAT-133 was also efficacious in vivo in diabetic animals and reduced systemic glucose levels. Thus it is a potential lead compound which can be considered for development as a therapeutic for the treatment of type-2 diabetes. We have reported herewith the isolation of the producer microbe, fermentation, purification, in vitro, and in vivo antidiabetic activity of the compound

Monitoring the spread of water hyacinth (Pontederia crassipes): challenges and future developments

Water hyacinth (Pontederia crassipes, also referred to as Eicchornia crassipes) is one of the most invasive weed species in the world, causing significant adverse economic and ecological impacts, particularly in tropical and sub-tropical regions. Large scale real-time monitoring of areas of chronic infestation is critical to formulate effective control strategies for this fast spreading weed species. Assessment of revenue generation potential of the harvested water hyacinth biomass also requires enhanced understanding to estimate the biomass yield potential for a given water body. Modern remote sensing technologies can greatly enhance our capacity to understand, monitor and estimate water hyacinth infestation within inland as well as coastal freshwater bodies. Readily available satellite imagery with high spectral, temporal and spatial resolution, along with conventional and modern machine learning techniques for automated image analysis, can enable discrimination of water hyacinth infestation from other floating or submerged vegetation. Remote sensing can potentially be complemented with an array of other technology-based methods, including aerial surveys, ground-level sensors, and citizen science, to provide comprehensive, timely and accurate monitoring. This review discusses the latest developments in the use of remote sensing and other technologies to monitor water hyacinth infestation, and proposes a novel, multi-modal approach that combines the strengths of the different methods

Detecting Water Hyacinth Infestation in Kuttanad, India, Using Dual-Pol Sentinel-1 SAR Imagery

Water hyacinth (Pontederia crassipes, also known as Eichhornia crassipes) is a highly invasive aquatic macrophyte species, indigenous to Amazonia, Brazil and tropical South America. It was introduced to India in 1896 and has now become an environmental and social challenge throughout the country in community ponds, freshwater lakes, irrigation channels, rivers and most other surface waterbodies. Considering its large speed of propagation on the water surface under conducive conditions and the adverse impact the infesting weed has, constant monitoring is needed to aid civic bodies, governments and policy makers involved in remedial measures. The synoptic coverage provided by satellite imaging and other remote sensing practices make it convenient to find a solution using this type of data. While there is an established background for the practice of remote sensing in the detection of aquatic plants, the use of Synthetic Aperture Radar (SAR) has yet to be fully exploited in the detection of water hyacinth. This research focusses on detecting water hyacinth within Vembanad Lake, Kuttanad, India. Here, results show that the monitoring of water hyacinth has proven to be possible using Sentinel-1 SAR data. A quantitative analysis of detection performance is presented using traditional and state-of-the-art change detectors. Analysis of these more powerful detectors showed true positive detection ratings of ~95% with 0.1% false alarm, showing significantly greater positive detection ratings when compared to the more traditional detectors. We are therefore confident that water hyacinth can be monitored using SAR data provided the extent of the infestation is significantly larger than the resolution cell (bigger than a quarter of a hectare)

SARS-CoV-2 susceptibility and COVID-19 disease severity are associated with genetic variants affecting gene expression in a variety of tissues

Variability in SARS-CoV-2 susceptibility and COVID-19 disease severity between individuals is partly due to genetic factors. Here, we identify 4 genomic loci with suggestive associations for SARS-CoV-2 susceptibility and 19 for COVID-19 disease severity. Four of these 23 loci likely have an ethnicity-specific component. Genome-wide association study (GWAS) signals in 11 loci colocalize with expression quantitative trait loci (eQTLs) associated with the expression of 20 genes in 62 tissues/cell types (range: 1:43 tissues/gene), including lung, brain, heart, muscle, and skin as well as the digestive system and immune system. We perform genetic fine mapping to compute 99% credible SNP sets, which identify 10 GWAS loci that have eight or fewer SNPs in the credible set, including three loci with one single likely causal SNP. Our study suggests that the diverse symptoms and disease severity of COVID-19 observed between individuals is associated with variants across the genome, affecting gene expression levels in a wide variety of tissue types

A first update on mapping the human genetic architecture of COVID-19

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