Bacterial laccases have proven to be a potential biocatalyst for various industrial applications due to their remarkable catalytic and stability properties. In this study, a novel thermostable ...laccase was produced from the bacterium Bacillus licheniformis VNQ by submerged fermentation. The specific activity of crude and purified laccase was found to be 13.17 U mg−1 and 83.47 U mg−1, respectively. The enzyme possessed a molecular mass of ∼48 kDa when characterized by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). The optimum temperature and pH for enzyme activity was determined to be 55°C and 5.0, respectively. The enzyme was considered to be thermo-tolerant as it possessed a half-life of 4 h at 70°C. The enzyme was utilized for the oxidative biotransformation of in situ synthesized p-quinones to biologically active compounds, 1,4-naphthoquinone and its derivative. The obtained products were characterized using nuclear magnetic resonance (NMR) spectroscopy and gas chromatography–mass spectrometry (GC–MS) analysis. A high yield of naphthoquinones (74.93 ± 1.2%) with 1,4-naphthoquinone (60.61 ± 1.0%), and its derivative 2-hydroxy-1,4-naphthoquinone (14.32 ± 0.2%) was obtained at the optimized reaction conditions.
•Production of thermostable laccase from thermophilic bacterial strain isolated from a geothermal location.•The enzyme possesses a half-life of 4 h at 70oC, thus suitable for the reaction processes performed at high temperature.•The enzyme obtained was utilized for the synthesis of naphthoquinone derivatives, popular bioactive compounds.•A high yield of 1,4-naphthoquinones (74.93 ± 1.2%) was obtained by optimizing the reaction conditions.
Cancer has been recognized as one of the non-communicable diseases with an increasing number of new cases, higher morbidity, and higher mortality rates at the global level. Thus, there is non-stop ...search for novel targets and small molecules to improve the chemotherapeutic outcomes concerning potency, selectivity, efficiency, affinity, ADMET, etc. Among anticancer therapeutic targets, tyrosine kinase has been documented well and approved as an important target with the development of various clinically used drugs. There are several structurally diverse small molecules in different preclinical and clinical stages of development that act by affecting tyrosine kinases in cancerous cells. Here, we have summarized different potent molecules acting against tyrosine kinases that can be considered as anticancer agents.
The current review focused on structural aspects of different chemical agents for inhibition of tyrosine kinases as anticancer agents.
The present study provides a summarized review of published information on tyrosine kinase inhibitors, their binding pattern, potencies, and structure-activity relationships. The review also highlighted the structural aspects of the interaction between inhibitors and amino acid residues of tyrosine kinases. Moreover, it also provided a summary of different types of cancers and the currently available options for treatment.
Several studies are being conducted for the inhibition of different tyrosine kinases using small molecules for the treatment of cancer. Tyrosine kinases have been reported involving in routine cellular functions, growth, and division of cells through different pathways which depend on phosphorylation. The overexpression and uncontrolled activity of tyrosine kinases have been identified as an important feature of cancerous cells. Thus, various small molecules have been reported which inhibit tyrosine kinases to block the growth and division of cancer cells. Here, more than 30 highly potent inhibitors of tyrosine kinases are summarised, which consist of pyrimidine, pyrazole, triazine, quinazoline, quinoline, pyrazine, chromene, etc. rings as a basic skeleton with different substituents.
Inhibition of tyrosine kinases by different small molecules is an approved strategy for the development of novel anticancer agents. Several published reports have mentioned the characteristics of the different binding sites and crucial residues in tyrosine kinases for the design of novel molecular inhibitors. However, selectivity is an important criterion for the development of chemotherapeutic agents due to the existence of approximately 30 families of tyrosine kinases.
Nb-doped TiO
2
(referred hereafter as NTO) thin films were deposited by sol–gel spin coating method to investigate their use as transparent conducting electrode (TCE). A range of Nb
x
Ti
1−
x
O
2
(
x
... = 0, 0.003, 0.005, 0.008, 0.01, 0.015, 0.02) compositions were synthesized and deposited as thin films via spin coating. The films were deposited at room temperature and showed crystallization on annealing at 550 °C for 1 h in air. The X-ray diffraction confirms formation of anatase TiO
2
by showing dominant peak at 2
θ
~25.5° corresponding to (101) reflection plane. Raman spectroscopy shows the characteristics modes of TiO
2
. Surface topography and morphology measured by atomic force microscopy and field-emission scanning electron microscopy exhibit smooth and uniform deposition of films. Optical transmittance reduces from 85 to 70% as Nb content increases from 0 to 2 at.%. Meanwhile, electrical resistivity attained a minimum value of 3.65 Ω cm for 2 at.% Nb doping. X-ray photoelectron spectroscopy analysis exhibits shifting of Ti 2
p
peak which confirms substitution by Nb
5+
in TiO
2
lattice and Nb–O–Ti bond formation. Transmission electron microscope and selected area electron diffraction patterns reveal that films consist of Nb and crystalline phase of TiO
2
. All films were characterized by Fourier transmission infrared spectroscopy and thermogravimetric analysis. Present study reports low-cost and effective fabrication of TCE for optoelectronic applications.
Actinobacteria represent one of the largest bacterial phyla harboring many species of high medical, biotechnological and ecological relevance. Prophage elements are major contributors to bacterial ...genome diversity and were shown to significantly shape bacterial fitness and host-microbe interactions. In this study, we performed a systematic analysis of prophage elements in 2406 complete actinobacterial genomes. Overall, 2106 prophage elements were predicted to be present in about 50% (1172/2406) of the analyzed datasets. Interestingly, these identified sequences compose a high prevalence of cryptic prophage elements, indicating genetic decay and domestication. Analysis of the sequence relationship of predicted prophages with known actinobacteriophage genomes revealed an exceptional high phylogenetic diversity of prophage elements. As a trend, we observed a higher prevalence of prophage elements in vicinity to the terminus. Analysis of the prophage-encoded gene functions revealed that prophage sequences significantly contribute to the bacterial antiviral immune system, but no biosynthetic gene clusters involved in the synthesis of known antiphage molecules were identified in prophage genomes. Overall, the current study highlights the remarkable diversity of prophages in actinobacterial genomes, with highly divergent prophages in actinobacterial genomes and thus provides an important basis for further investigation of phage-host interactions in this important bacterial phylum.
Intra-articular steroids provide significant pain relief in sacroiliac joint pain (SIJP), but their action is short-lived. Cryoneurolysis is reported to produce prolonged pain relief in various pain ...conditions. However, its efficacy has not been evaluated in patients with SIJP. Thus, we compared the efficacy of cryoneurolysis with steroid injections in adult patients with SIJP.
This retrospective healthcare records review-based study involved 83 patients with SIJP. Patients were divided into two groups: cases (sacroiliac joint SIJ cryoneurolysis,
= 39) and controls (SIJ steroid injection,
= 44). An 11-point numeric pain rating scale (NPRS) was used to assess the pain severity at baseline and immediately, 1, 3 and 6 months post-intervention. A reduction of ≥50% in NPRS score immediately following SIJ cryoneurolysis and steroid injection was considered a successful outcome. The difference between the treatment groups was assessed with a Chi-square test, and
< 0.05 was considered statistically significant.
Both cases and controls showed significantly decreased NPRS scores from baseline to immediately, 1 month, 3 months and 6 months postintervention (
< 0.001). However, compared to controls, cases had significantly lower NPRS scores at all time points (all
< 0.001). Moreover, a significantly greater proportion of cases had ≥50% decrease in NPRS score from baseline, that is, 1 month (97.44% vs. 75%,
= 0.004), 3 months (100% vs. 47.73%,
< 0.001) and 6 months (69.23% vs. 27.27%,
< 0.001).
Although both cryoneurolysis and intra-articular steroid injections provide significant pain relief immediately, 1, 3 and 6 months postintervention, cryoneurolysis resulted in significantly greater pain relief.
This experimental work focuses on how to develop an improved grade of Carbon fiber/epoxy compound material with superior mechanical characteristics, by adding small amounts of functionalized ...multi-walled carbon nanotubes (MWCNTs) into it. These composites could have potential applications in the missile and aerospace industry. Different percentages (0.25, 0.5, 1, and 2%) of amine-functionalized MWCNTs are infused into the epoxy resin (LY556). Sonicator is used to ensure good homogeneity and then hardener is added to the mixture, and then manually stirred. This mixture is finally layed upon carbon fiber mat by the wet layup process and cured in a hot press to produce the samples. Interlaminar shear strength (ILSS) and three-point bending tests are performed on a UTM both on amine-functionalized and unfilled CNT C-fiber/epoxy compound. The results show that amine-functionalized MWCNTs improved the mechanical properties of C-fiber/epoxy composites. The highest improvement of 12.84% in flexural strength is obtained with 0.25% amine-functionalized MWCNT and of 11.67% in ILSS with 0.5% amine-functionalized MWCNTs. Five samples are tested amongst which the standard deviation for flexural strength is found to be minimum (3.9) in 0.25% amine CNTs and for ILSS it is minimum (1.41) in 0.5% amine CNTs. The influence of such amine functionalization produced positive overall trends among the entire mechanical qualities assessed.
This paper addresses a simple energy-based overset finite element method (EbO-FEM) to solve pseudo-static deformation problems consisting of overlapped meshes based on the domain composition method ...(DCM). This scheme is a non-iterative equation-based method for enforcing the continuity of the displacement field. Hence, the scheme consumes possible minimal computational costs for deformation problems with non-conforming overlapping meshes. The system’s total energy is augmented with continuity constraint energy (CCE) which is a function of the gaps in the displacement field between two overlapping regions. Subsequently, two conventional integration schemes, the Gauss-point projection, and the point-to-point projection, are utilized to discretize the CCE. It is confirmed that both schemes can yield accurate and unique solutions in the overlapped region of the finite element meshes. Further, we proposed a dimensionless relative penalty parameter (DRP). We found that DRP ranging between 1 to 10 is appropriate to robustly obtain accurate solutions for a wide range of scales, stiffness, and geometries, which is supported by three numerical simulations without increasing computational costs after assembling the global matrices and vectors.
The present paper discusses the development of a Semi-solid Rapid Curing epoxy Resin-based (RaCER) sealant paste using micro and nanoscale fillers and curing agents. Semi-solid consistency and rapid ...curing behaviour are two essential criteria for a RaCER sealant paste to be qualified to be applicable for repairing leaking defects in oil and gas pipelines. RaCER is a two-part system consisting of a resin-based paste (Part A) and a curing agent-based paste (Part B). The compositions of the micro and nano fillers in Part A and Part B and the amount of curing agent in Part B vary to achieve the required semi-solid consistency and optimum curing time. The optimization of micro and nanofiller compositions and curing agents is done with the help of statistics. A mathematical model for the response of these variables curing time, tensile, compression, and shear strength, is developed using a full factorial design of experiments. The optimum composition is derived using response surface methodology. Hydrostatic burst tests on pipe specimens with 10 mm through hole defect repaired in the live and non-live conditions are conducted to evaluate the performance of RaCER paste. An enhanced repair methodology is also evolved for repairing large-size leaking defects and sealing the leak in live condition. The failure pattern and enhanced pressure-bearing capability of the epoxy resin-based sealant paste indicate better interfacial bonding with steel and Glass Fiber Reinforced Polymer (GFRP) substrates, making the product suitable for oil and gas pipeline repair compared to other commercially available products.
Optimal crop emergence is an important trait in crop breeding for genotypic screening and for achieving potential growth and yield. Emergence is conventionally quantified manually by counting the ...sub-sections of field plots or scoring; these are less reliable, laborious and inefficient. Remote sensing technology is being increasingly used for high-throughput estimation of agronomic traits in field crops. This study developed a method for estimating wheat seedlings using multispectral images captured from an unmanned aerial vehicle. A machine learning regression (MLR) analysis was used by combining spectral and morphological information extracted from the multispectral images. The approach was tested on diverse wheat genotypes varying in seedling emergence. In this study, three supervised MLR models including regression trees, support vector regression and Gaussian process regression (GPR) were evaluated for estimating wheat seedling emergence. The GPR model was the most effective compared to the other methods, with R2 = 0.86, RMSE = 4.07 and MAE = 3.21 when correlated to the manual seedling count. In addition, imagery data collected at multiple flight altitudes and different wheat growth stages suggested that 10 m altitude and 20 days after sowing were desirable for optimal spatial resolution and image analysis. The method is deployable on larger field trials and other crops for effective and reliable seedling emergence estimates.
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