Mitochondria-targeted esculetin and metformin delay endothelial senescence by promoting fatty acid β-oxidation: Relevance in age-associated atherosclerosis.

Impaired mitochondrial fatty acid β-oxidation (FAO) plays a role in the onset of several age-associated diseases, including atherosclerosis. In the current work, we investigated the efficacies of mitochondria-targeted esculetin (Mito-Esc) and metformin in enhancing FAO in human aortic endothelial cells (HAECs), and its relevance in the delay of cellular senescence and age-associated atherosclerotic plaque formation in Apoe mice. Chronic culturing of HAECs with either Mito-Esc or metformin increased oxygen consumption rates (OCR), and caused delay in senescence features.

Investigating the role of corrole as an excitation energy relay in light-induced processes in closely connected N,N'-bis(biphenyl-4-yl)aniline functionalized corrole donor-acceptor dyad.

A photosynthetic antenna-reaction center model, BBA-PFCor comprised of N,N'-bis(biphenyl-4-yl)aniline (BBA) covalently functionalized to bis(pentafluoro)corrole moiety has been prepared and the contribution of the BBA as the photoinduced energy transfer antenna was investigated. UV-visible studies have shown that integrating the electron-rich BBA chromophore into the corrole core has broadened the soret band of the corrole moiety with the absorption spanning from 300 to 700 nm. Electrochemical studies, in corroboration with the computational calculations, revealed that, BBA moiety can act as an electron reservoir and, in the excited state, it would transfer the excited energy to the corrole moiety in the dyad.

ROS mediated Cu[Fe(CN)NO] nanoparticles for triple negative breast cancer: A detailed study in preclinical mouse model.

Triple negative breast cancer (TNBC) is an aggressive form of tumor, more prevalent in younger women resulting in poor survival rate (2nd in cancer deaths) because of its asymptomatic existence. The most popular and convenient approach for the treatment of TNBC is chemotherapy which is associated with several limitations. Considering the importance of nanotechnology in health care system, in the present manuscript, we have designed and developed a simple, efficient, cost effective, and ecofriendly method for the synthesis of copper nitroprusside analogue nanoparticles (Cu[Fe(CN)NO] which is abbreviated as CuNPANP that may be the potential anti-cancer nanomedicine for the treatment of TNBC.

Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA-approved drugs and clinical candidates.

Natural products have always served as an important source of drugs for treating various diseases. Among various privileged natural product scaffolds, the benzopyrone class of compounds has a substantial presence among biologically active compounds. One of the pioneering anticoagulant drugs, warfarin approved in 1954 bears a benzo-α-pyrone (coumarin) nucleus.

Synthesis of -fused cyclopentenone-pyrrolidine scaffolds sequential aza-Piancatelli and Conia-ene type reactions in one pot.

A novel one-pot protocol that enables sequential execution of an aza-Piancatelli rearrangement and a Conia-ene type reaction has been developed under Lewis acid catalysis. Here, a combination of B(CF) and Cu(OTf), triethylamine, and triphenylphosphine yielded a wide range of -fused cyclopentenone-pyrrolidine scaffolds in one pot with good yields and diastereoselectivity.

Molecularly Engineered Multifunctional Bridging Layer Derived from Dithiafulavene Capped Spiroxanthene for Stable and Efficient Perovskite Solar Cells.

This study introduces a novel approach centered around the design and synthesis of an interfacial passivating layer in perovskite solar cells (PSCs). This architectural innovation is realized through the development of a specialized material, termed dithiafulvene end-capped Spiro[fluorene-9,9'-xanthene], denoted by the acronym AF32. In this design architecture, dithiafulvene is thoughtfully attached to the spiroxanthene fluorene core with phenothiazine as the spacer unit, possessing multiple alkyl chains.

Ultrasonic-assisted synthesis of CaCuTiO/reduced graphene oxide composites for enhanced photocatalytic degradation of pharmaceutical products: Ibuprofen and Ciprofloxacin.

The objective of this research is to create a highly effective approach for eliminating pollutants from the environment through the process of photocatalytic degradation. The study centers around the production of composites consisting of CaCuTiO (CCTO) and reduced graphene oxide (rGO) using an ultrasonic-assisted method, with a focus on their capacity to degrade ibuprofen (IBF) and ciprofloxacin (CIP) via photodegradation. The impact of rGO on the structure, morphology, and optical properties of CCTO was inspected using XRD, FTIR, Raman, FESEM, XPS, BET, and UV-Vis.

Total Synthesis and Revision of Stereochemistry of a Natural Benzo[]isochromene Stereodiad Isolated from .

This study presents a total synthesis and revision of the stereochemical configuration of the conformationally flexible natural product benzo[]isochromene stereodiad alongside its diastereomeric counterparts. The highlights of the synthesis are the TiCl-mediated diastereoselective aldol reaction, Pd-catalyzed lactonization, and Schmidt glycosidation. Our efforts using total synthesis disclosed herein proved that a previously assigned structure required revision.

Biocatalytic enantioselective synthesis of cenobamate, an antiepileptic drug.

A green and efficient process for the synthesis of cenobamate has been accomplished in 70% yield and >99% ee through the bio-reduction of β-ketotetrazole using Daucus carota whole plant cells. The corresponding β-hydroxytetrazole was isolated in 60% yield and >98% ee. This is the first report on the biocatalytic reduction of β-ketotetrazole using plant enzymes derived from D.

Bis-arylidene oxindoles for colorectal cancer nanotherapy.

Oxindoles are potent anti-cancer agents and are also used against microbial and fungal infections and for treating neurodegenerative diseases. These oxindoles are earlier established as estrogen receptor (ER)-targeted agents for killing ER (+) cancer cells. Our previously developed bis-arylidene oxindole, Oxifen (OXF) exhibits effective targeting towards ER (+) cancer cells which has a structural resemblance with tamoxifen.

Catching an Oxo Vanadate Porous Acetylacetonate Covalent Adaptive Catalytic Network that Renders Mustard-Gas Simulant Harmless.

In this work, we illustrated the design and development of a metal-coordinated porous organic polymer () namely a post-synthetic metalation strategy to incorporate oxo-vanadium sites in a pristine polymer () having acetylacetonate (acac) as anchoring moiety. The as-synthesized exhibited highly robust and porous framework, which has been utilized for thioanisole (TA) oxidation to its corresponding sulfoxide. The catalyst demonstrated notable stability and recyclability by maintaining its catalytic activity over multiple reaction cycles without any significant loss in activity.

Organocatalytic enantioselective desymmetrization of enal-tethered cyclohexane-1,3-diones.

Organocatalytic asymmetric desymmetrization of prochiral cyclohexane-1,3-diones has been demonstrated through the merging of iminium and enamine activation. The tandem annulation reaction proceeds through a sequential oxa-Michael addition/intramolecular aldol reaction/[1,3]-amino oxetane rearrangement pathway. Mechanistic study using an O-water experiment suggests oxetane rearrangement instead of direct dehydration.

Metal-free functionalization of tyrosine residues in short peptides and study of the morphological alterations.

An efficient functionalization of tyrosine residues in phenolic regions is achieved under metal-free conditions. The strategy involves the conversion of a tyrosine residue to 4-amino phenylalanine or 4-amino-3-methoxy phenylalanine in short peptides through a controlled oxidative dearomatization. This transformation is achieved in one pot with good yields and excellent regioselectivity.

6-Strand to Stable 10/12 Helix Conformational Switch by Incorporating Flexible β-hGly in the Homooligomers of Camphor Derived β-Amino Acid: NMR and X-Ray Crystallographic Evidence.

Rational design of unnatural amino acid building blocks capable of stabilizing predictable secondary structures similar to protein fragments is pivotal for foldamer chemistry/catalysis. Here, we introduce novel β-amino acid building blocks: [1S,2R,4R]exoCDA and [1S,2S,4R]endoCDA, derived from the abundantly available R(+)-camphor, which is traditionally known for its medicinal value. Further, we demonstrate that the homooligomers of exoCDA adopt 6-strand conformation, which switches to a robust 10/12-helix simply by inserting flexible β-hGly spacer at alternate positions (1 : 1 β-hGly/exoCDA heterooligomers), as evident by DFT-calculations, solution-state NMR spectroscopy and X-ray crystallography.

Modulating cultivation regimes of Messastrum gracile SVMIICT7 for biomass productivity integrated with resource recovery via hydrothermal liquefaction.

The present study was designed to assess Messastrum gracile SVMIICT7 potential in treating dairy wastewater (autoclaved (ADWW) and raw (DWW)) with relation to nutrient removal, in-vivo Chl-a-based biomass, and bio-oil synthesis. Chlorophyll a fluorescence kinetics revealed improved photochemical efficiency (0.639, Fv/Fm) in M.

Unraveling Multicopper [Cu] and [Cu] Clusters with Rare μ-Sulfato and Linear μ-Oxido-Bridges as Potent Antibiofilm Agents against Multidrug-Resistant .

In this research article, two multicopper [Cu] and [Cu] clusters, [Cu(cpdp)(μ-SO)(Cl)(HO)]·3HO () and [Cu(cpdp)(μ-O)(Cl)(HO)]·2Cl () (Hcpdp = ,'-bis[2-carboxybenzomethyl]-,'-bis[2-pyridylmethyl]-1,3-diaminopropan-2-ol), have been explored as potent antibacterial and antibiofilm agents. Their molecular structures have been determined by a single-crystal X-ray diffraction study, and the compositions have been established by thermal and elemental analyses, including electrospray ionization mass spectrometry. Structural analysis shows that the metallic core of is composed of a trinuclear [Cu] assembly encapsulating a μSO group, whereas the structure of represents a hexanuclear [Cu] assembly in which two trinuclear [Cu] motifs are exclusively bridged by a linear μO group.

Yohimbine Treatment Alleviates Cardiac Inflammation/Injury and Improves Cardiac Hemodynamics by Modulating Pro-Inflammatory and Oxidative Stress Indicators.

Acute myocarditis, also known as myocardial inflammation, is a self-limited condition caused by systemic infection with cardiotropic pathogens, primarily viruses, bacteria, or fungi. Despite significant research, inflammatory cardiomyopathy exacerbated by heart failure, arrhythmia, or left ventricular dysfunction and it has a dismal prognosis. In this study, we aimed to evaluate the therapeutic effect of yohimbine against lipopolysaccharide (LPS) induced myocarditis in rat model.

Access to CF-benzofulvenes palladium-catalyzed cascade arylation/Trost-Oppolzer cyclization/double-bond isomerization.

Herein, we demonstrated a Pd-catalyzed cascade reaction that involves arylation, Trost-Oppolzer type Alder ene reaction, and double bond isomerization using the 4-(2-alkynylphenyl)-allylcarbonates and aryl boronic acids. This cascade process delivers a wide array of distinctive functionalized CF-benzofulvenes in good yields with high stereoselectivity (). A single palladium catalyst orchestrates the two individual reactions in a single operation.

Identification and characterization of impurities in an insecticide, commercial chlorantraniliprole using liquid chromatography-tandem mass spectrometry.

Rationale: Ensuring the global safety and effectiveness of agrochemicals has become imperative. An in-depth understanding of impurity profiles of products is crucial, especially for high-demand agrochemicals, where impurities may be more toxic and persistent than original agrochemicals. This study focuses on the detection and identification of impurities in a commercial chlorantraniliprole (CAP), an anthranilic diamide class broad-spectrum insecticide.

Thiazolotriazoles As Anti-infectives: Design, Synthesis, Biological Evaluation and Studies.

The rational design of novel thiazolo[2,3-][1,2,4]triazole derivatives was carried out based on previously identified antitubercular hit molecule H127 for discovering potent compounds showing antimicrobial activity. The designed compounds were screened for their binding efficacies against the antibacterial drug target enoyl-[acyl-carrier-protein] reductase, followed by prediction of drug-likeness and ADME properties. The designed analogues were chemically synthesized, characterized by spectroscopic techniques, followed by evaluation of antimicrobial activity against bacterial and fungal strains, as well as antitubercular activity against and strains.

Enhanced response of WO thin film through Ag loading towards room temperature hydrogen gas sensor.

This study investigates the enhancement of hydrogen gas-sensing performance by introducing silver (Ag) nanoparticles onto tungsten trioxide (WO) thin films. Herein, the WO thin films are deposited onto SiO/Si substrates using a sputtering technique and Ag nanoparticles are loaded onto the WO surface through a spin coating technique. To evaluate the sensing performance of a hydrogen gas, interdigitated titanium (Ti) electrodes are deposited onto the Ag:WO layer.

Total Synthesis of Macrocyclolipopeptide Dysoxylactam A.

A highly stereoselective total synthesis of potent multidrug-resistant reverser dysoxylactum A has been accomplished in the longest linear sequences of 20 steps with an overall 10.2% yield. The key steps of this synthesis included Brown's crotylation, Evans alkylation, the Carreira protocol to generate the stereogenic center, and Yamaguchi macrolactonization.

Pd-Catalyzed Chelation-Assisted Regioselective and Site Selective Cyclative C-H Annulation of Alkynyl Oximes with Activated Alkynes.

Electrophilic cyclization and concomitant C-H annulation constitute an expedient cascade strategy for the construction of multicyclic scaffolds with precise substitutional patterns. We report here a novel Pd-catalyzed cyclative annulation of ynone oxime with activated alkynes. The cascade features a dual regioselectivity including site selective C-H activation and chelation-assisted selective insertion of alkynes.

NHC-Catalyzed Formal [4 + 2] Annulation of -Formyl-Tethered Michael Acceptors and Ynones to Access Highly Functionalized Naphthalene Derivatives.

Herein we demonstrate a novel organocatalytic method to access multifunctionalized naphthalenes an NHC-catalyzed reaction of ynones and -formyl-tethered Michael acceptors. The presented method proceeds through an intermolecular Stetter reaction-cyclization-aromatization cascade and represents a rare example of organocatalytic benzannulation for the synthesis of substituted arenes by using ynone as a two-carbon synthon. The current method has broad substrate scope; postsynthetic transformations and gram-scale syntheses highlight the practicality of the displayed methodology.

Uncovering Sex-Specific Epigenetic Regulatory Mechanism Involving H3k9me2 in Neural Inflammation, Damage, and Recovery in the Internal Carotid Artery Occlusion Mouse Model.

Cerebral ischemic stroke is one of the foremost global causes of death and disability. Due to inadequate knowledge in its sequential disease mechanisms, therapeutic efforts to mitigate acute ischemia-induced brain injury are limited. Recent studies have implicated epigenetic mechanisms, mostly histone lysine acetylation/deacetylation, in ischemia-induced neural damage and death.