Design, Screening, Synthesis, Characterisation and DFT-based Electronic Properties of Dihydropyridine-based Molecule as L-type Calcium Channel Blocker.

Background: People of all nationalities and social classes are now affected by the growing issue of hypertension. Over time, there has been a consistent rise in the fatality rate. A range of therapeutic compounds, on the other hand, are often used to handle hypertension.

Experimental investigation of a biomass-derived nanofluid with enhanced thermal conductivity as a green, sustainable heat-transfer medium and qualitative comparison mathematical modelling.

In this study, bio-based carbon nanospheres (CNSs) were synthesized from lignocellulosic-rich groundnut skin () and tested for their practical application in nanofluids (NFs) for enhanced heat transfer. The CNSs were characterized using various techniques, including FESEM, EDS, XRD, Raman spectroscopy, zeta potential analysis, and FTIR. Thermal conductivity (TC) and viscosity measurements were conducted using transient plane source (TPS) technique with a Hot Disk thermal analyser and discovery hybrid rheometer, respectively.

'Donor-acceptor', 'interpenetrating polymer network' and 'electrostatic self-assembly' work in tandem to achieve extraordinary specific shielding effectiveness.

The exploration of 'electrostatic self-assembly' on solid surfaces has garnered significant interest across various fields. With the sophistication of gadgets, managing electromagnetic interference (EMI) from stray signals, especially in stealth applications, necessitates materials that can absorb microwaves. A promising approach involves integrating lightweight self-healing polymeric materials.

Self-Healable Interfaces with Improved Mechanical Properties Induced by Dynamic Network Reconfiguration in Carbon Fiber-Reinforced Epoxy Laminates.

Interfacial failure in carbon fiber-reinforced epoxy (CFRE) laminates is a prominent mode of failure, attracting significant research attention. The large surface-energy mismatch between carbon fiber (CF) and epoxy results in a weaker interface. This study presents a facile yet effective method for enhancing the interfacial adhesion between CF and epoxy with self-healable interfaces.

GO-tagged PEI sizing agent imparts self-healing and excellent mechanical properties to carbon fiber reinforced epoxy laminates.

Carbon fiber-reinforced epoxy (CFRE) laminates have attracted significant attention as a structural material specifically in the aerospace industry. In recent times, various strategies have been developed to modify the carbon fiber (CF) surface as the interface between the epoxy matrix and CFs plays a pivotal role in determining the overall performance of CFRE laminates. In the present work, graphene oxide (GO) was used to tag a polyetherimide (PEI, termed BA) containing exchangeable bonds and was employed as a sizing agent to improve the interfacial adhesion between CFs and epoxy.

Temperature Upshifts in Mammalian Cell Culture: A Suitable Strategy for Biosimilar Monoclonal Antibodies?

Temperature downshifts are the gold standard when setting up control strategies for mammalian cell culture processes. These shifts are performed to prolong production phases and attain heightened levels of productivity. For the development of biosimilars, however, the bottleneck is in achieving a prespecified product quality.

Fundamental Understanding of Ultrathin, Highly Stable Self-Assembled Liquid Crystalline Graphene Oxide Membranes Leading to Precise Molecular Sieving through Non-equilibrium Molecular Dynamics.

Self-assembled graphene oxide lyotropic liquid crystal (GO LLC) structures are mostly formed in aqueous medium; however, most GO derivatives are water insoluble, so processing GO LLCs in water poses a practical limitation. The use of polar aprotic solvent (like dimethyl sulfoxide) for the formation of GO LLC structures would be interesting, because it would allow incorporating additives, like photoinitiators or cross-linkers, or blending with polymers that are insoluble in water, which hence would expand its scope. The well-balanced electrostatic interaction between DMSO and GO can promote and stabilize the GO nanosheets' alignment even at lower concentrations.

Polyoxometalate-immobilized carbon nanotube constructs triggered by host-guest assembly result in excellent electromagnetic interference shielding.

In the era of fifth-generation networks and the Internet of Things, new classes of lightweight, ultrathin, and multifunctional electromagnetic interference (EMI) shielding materials have become inevitable prerequisites for the protection of electronics from stray electromagnetic signals. In the present study, for the first time, we have designed a unique nanohybrid composed of a copper-based polyoxometalate (Cu-POM)-immobilized carbon nanotube construct, having a micron (∼100 μm)-level thickness, through a facile vacuum-assisted filtration technique. In this course of study, a total of four Cu-POMs, two from each category of Keggin and Anderson bearing opposite charges, , positive and negative, have been rationally selected to investigate the effects of the host-guest electrostatic interaction between CNT and POMs in the EMI shielding performance.

Synthesis of drug conjugated magnetic nanocomposite with enhanced hypoglycemic effects.

In the present study, a magnetic nanocomposite (magnetite FeO and hematite FeO) has been successfully synthesized by the sol-gel method and coated with polyvinyl alcohol (PVA) followed by conjugation of anti-diabetic drug metformin. Detailed structural and microstructural characterization of the nanocomposite (NP) and drug conjugated nanocomposite (NP-DC) are analyzed by the Rietveld refinement of respective XRD patterns, FTIR analysis, UV-Vis spectroscopy, SEM and TEM results. SEM and TEM image analyses reveal the spherical morphology and average size of NP, PVA coated nanoparticles (NP-PVA) and NP-DC samples, indicating a suitable size to be a nanocarrier.

Evaluation of Efficacy of Curcumin along with Lycopene and Piperine in the Management of Oral Submucous Fibrosis.

Context: Oral submucous fibrosis (OSMF) is a high-risk premalignant condition of the oral cavity and oropharynx. Complete regression of the disease is still not possible with available treatment modalities.

Aims: The aim of the study was to evaluate the efficacy of curcumin, lycopene, and piperine as a combination in the management of OSMF.

Enhanced antifungal activity of fluconazole conjugated with Cu-Ag-ZnO nanocomposite.

Cu-Ag-ZnO nanocomposite (NC) has been successfully synthesized by mechanical alloying the Cu, Zn and Ag powder mixture under Ar atmosphere within 4 h of milling. The nanocomposite is then conjugated with the antifungal drug fluconazole by adding 5 wt% powdered drug to the NC and mechanical alloying the total powder mixture for one more hour. The Rietveld refinement of XRD data and FTIR spectrum analyses reveal the detailed structural and microstructural characterizations of the nanocomposite-drug conjugate (NC-DC).

Engineered magnetic core shell nanoprobes: Synthesis and applications to cancer imaging and therapeutics.

Magnetic core shell nanoparticles are composed of a highly magnetic core material surrounded by a thin shell of desired drug, polymer or metal oxide. These magnetic core shell nanoparticles have a wide range of applications in biomedical research, more specifically in tissue imaging, drug delivery and therapeutics. The present review discusses the up-to-date knowledge on the various procedures for synthesis of magnetic core shell nanoparticles along with their applications in cancer imaging, drug delivery and hyperthermia or cancer therapeutics.

A Nucleus-Imaging Probe That Selectively Stabilizes a Minor Conformation of c-MYC G-quadruplex and Down-regulates c-MYC Transcription in Human Cancer Cells.

The c-MYC proto-oncogene is a regulator of fundamental cellular processes such as cell cycle progression and apoptosis. The development of novel c-MYC inhibitors that can act by targeting the c-MYC DNA G-quadruplex at the level of transcription would provide potential insight into structure-based design of small molecules and lead to a promising arena for cancer therapy. Herein we report our finding that two simple bis-triazolylcarbazole derivatives can inhibit c-MYC transcription, possibly by stabilizing the c-MYC G-quadruplex.

A small molecule peptidomimetic that binds to c-KIT1 G-quadruplex and exhibits antiproliferative properties in cancer cells.

A modular synthesis of l-proline derived peptidomimetics has been developed using the Cu(I) catalyzed Huisgen cycloaddition between an azido prolinamide with pyridine and benzene dicarboxamide containing dialkynes. Förster Resonance Energy Transfer (FRET) melting assay provided an initial indication that the pyridyl analogue can stabilize the c-KIT1 quadruplex DNA. A competitive FRET-melting assay and Fluorescent Intercalator Displacement (FID) assay suggest that the pyridyl ligand shows excellent selectivity for c-KIT1 quadruplex over duplex DNA and other investigated G-quadruplexes.

Synthesis of regiospecifically fluorinated conjugated dienamides.

Modular synthesis of regiospecifically fluorinated 2,4-diene Weinreb amides, with defined stereochemistry at both double bonds, was achieved via two sequential Julia-Kocienski olefinations. In the first step, a Z-a-fluorovinyl Weinreb amide unit with a benzothiazolylsulfanyl substituent at the allylic position was assembled. This was achieved via condensation of two primary building blocks, namely 2-(benzo[d]thiazol-2-ylsulfonyl)-2-fluoro-N-methoxy-N-methylacetamide (a Julia-Kocienski olefination reagent) and 2-(benzo[d]thiazol-2-ylthio)acetaldehyde (a bifunctional building block).

14-Deoxyandrographolide alleviates ethanol-induced hepatosteatosis through stimulation of AMP-activated protein kinase activity in rats.

Andrographis paniculata (AP) is a traditional medicinal plant of Ayurveda. It grows widely in Asia and is prescribed in the treatment of liver diseases. Here we have investigated the beneficial role of 14-deoxyandrographolide (14-DAG), a bioactive diterpenoid from AP, against alcoholic steatosis in rats.

Julia-Kocienski Approach to Trifluoromethyl-Substituted Alkenes.

A Julia-Kocienski approach to trifluoromethyl-substituted alkenes was evaluated in the reactions of 1,3-benzothiazol-2-yl, 1-phenyl-1-tetrazol-5-yl, and 1-butyl-1-tetrazol-5-yl 2,2,2-trifluoroethyl sulfones with aldehydes. Among the various conditions tested, the best yields were obtained with 1-phenyl-1-tetrazol-5-yl 2,2,2-trifluoroethyl sulfone, in CsF-mediated, room temperature olefinations in DMSO. Aromatic aldehydes gave (trifluoromethyl)vinyl derivatives in 23-86% yields, with generally moderate stereoselectivity.

Treatment with garlic restores membrane thiol content and ameliorates lead induced early death of erythrocytes in mice.

Sequelae of chronic lead (Pb(2+) ) toxicity includes anemia that is partially due to early death of erythrocytes characterized by excess accumulation of ROS and downregulation of antioxidant system causing oxidative stress and externalization of phosphatidylserine. In this study, pathophysiological based therapeutic application of garlic was evaluated against erythrocyte death. Results suggest that garlic administration prevents oxidative stress, restored the antioxidant balance in erythrocytes of Pb(2+) exposed mice.

14-Deoxyandrographolide targets adenylate cyclase and prevents ethanol-induced liver injury through constitutive NOS dependent reduced redox signaling in rats.

Chronic alcoholism is one of the most common causes of liver diseases worldwide. Nitric oxide (NO) has been proposed to have potential for clinical application against chronic hepatocellular injuries. However, mechanisms underlying hepatoprotective functions of NO in ethanol-induced apoptosis are largely unknown.

Interaction of carbon nanoparticles to serum albumin: elucidation of the extent of perturbation of serum albumin conformations and thermodynamical parameters.

Carbon nanoparticles continuously generated from industries and vehicles due to incomplete combustion of fuels is one of the potent causes of air pollution. The exposure of this polluted air with carbon nanoparticles, introduced into the bloodstream of animals in the course of respiration, motivated us to study their interaction with plasma proteins, bovine serum albumin and human serum albumin. Carbon nanoparticles with very small size and high purity were synthesized by dehydration of d-glucose using concentrated sulphuric acid as dehydrating agent.

Expedient synthesis of α-substituted fluoroethenes.

A mild and efficient synthesis of 1-aryl-1-fluoroethenes from benzothiazolyl (aryl)fluoromethyl sulfones and paraformaldehyde, under DBU- or Cs(2)CO(3)-mediated conditions at room temperature, is described. A comparable diethyl fluoro(naphthalen-2-yl)methylphosphonate reagent does not react with paraformaldehyde under these mild conditions. The utility of the methodology for synthesis of terminal α-fluoroalkenes bearing electron-withdrawing functionalities is also shown.

S-allyl cysteine in combination with clotrimazole downregulates Fas induced apoptotic events in erythrocytes of mice exposed to lead.

Background: Chronic lead (Pb(2+)) exposure leads to the reduced lifespan of erythrocytes. Oxidative stress and K(+) loss accelerate Fas translocation into lipid raft microdomains inducing Fas mediated death signaling in these erythrocytes. Pathophysiological-based therapeutic strategies to combat against erythrocyte death were evaluated using garlic-derived organosulfur compounds like diallyl disulfide (DADS), S allyl cysteine (SAC) and imidazole based Gardos channel inhibitor clotrimazole (CLT).

Superoxide anion mediated mitochondrial dysfunction leads to hepatocyte apoptosis preferentially in the periportal region during copper toxicity in rats.

Chronic exposure to copper induces hepatocellular apoptosis with greater injury in the periportal region compared to the perivenous region. Here we have identified the factors responsible for the development of regional damage in the liver under in vivo conditions. Enhanced production of reactive oxygen species (ROS) with predominance of superoxide radical (O(2)(-)) indicates the contribution of redox imbalance in the process.

Biocontrol of larval mosquitoes by Acilius sulcatus (Coleoptera: Dytiscidae).

Background: Problems associated with resistant mosquitoes and the effects on non-target species by chemicals, evoke a reason to find alternative methods to control mosquitoes, like the use of natural predators. In this regard, aquatic coleopterans have been explored less compared to other insect predators. In the present study, an evaluation of the role of the larvae of Acilius sulcatus Linnaeus 1758 (Coleoptera: Dytiscidae) as predator of mosquito immatures was made in the laboratory.