-(-Methoxyphenylpropargyl) Pyrrole-2-carboxylate (PPPC) Glycosides as Donors for Glycosylation.

We developed glycosyl -(-methoxyphenylpropargyl) pyrrole-2-carboxylates (PPPCs) as highly effective donors for chemical glycosylation. The modular design and exceptional stability of the acid precursor provide PPPC donors with synthetic versatility and ease of use. Activated by NIS/TMSOTf, PPPC donors exhibit a broad compatibility for both - and -glycosylation reactions.

The synthesis and bioactivity of apigenin derivatives.

Background: Apigenin, a naturally occurring compound with a flavone core structure, is known for its diverse bioactivities, including anti-inflammation, anti-toxicant, anti-cancer and so on. There has been significant interest in the medicinal chemistry community. To address these challenges, researchers have developed various derivatives of apigenin to address challenges such as poor water-solubility and low intestinal absorption, aiming to enhance the pharmacological activities and pharmacokinetic properties of this compound.

regulates inflorescence development and grain production in plants.

Female inflorescence is the primary output of medical . It contains hundreds of cannabinoids that accumulate in the glandular trichomes. However, little is known about the genetic mechanisms governing inflorescence development.

Incidental Learning of Collocations Under Different Input Modes and the Mediating Role of Perceptual Learning Style.

This study investigated how input modes (reading vs. listening) and learners' perceptual learning style (visual vs. auditory) affected the incidental learning of collocations.

Chalkophomycin Biosynthesis Revealing Unique Enzyme Architecture for a Hybrid Nonribosomal Peptide Synthetase and Polyketide Synthase.

Chalkophomycin is a novel chalkophore with antibiotic activities isolated from sp. CB00271, while its potential in studying cellular copper homeostasis makes it an important probe and drug lead. The constellation of -hydroxylpyrrole, 2-oxazoline, diazeniumdiolate, and methoxypyrrolinone functional groups into one compact molecular architecture capable of coordinating cupric ions draws interest to unprecedented enzymology responsible for chalkophomycin biosynthesis.

Biosynthesis and Anticancer Activity of Genistein Glycoside Derivatives.

As a beneficial natural flavonoid, genistein has demonstrated a wide range of biological functions via regulating a number of targets and signaling pathways, such as anti-cancer, antioxidant, antibacterial, antiinflammatory, antifungal, antiviral, iron chelation, anti-obesity, anti-diabetes, and anti-hypertension. Pub- Med/Medline and Web of Science were searched using appropriate keywords until the end of December 2023. Despite its many potential benefits, genistein's clinical application is limited by low hydrophilicity, poor solubility, and suboptimal bioavailability due to its structure.

Cancer cell membrane-coated nanoparticles: a promising anti-tumor bionic platform.

Nanoparticle (NP) drug delivery systems have shown promise in tumor therapy. However, limitations such as susceptibility to immune clearance and poor targeting in a complex intercellular environment still exist. Recently, cancer cell membrane-encapsulated nanoparticles (CCM-NPs) constructed using biomimetic nanotechnology have been developed to overcome these problems.

Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.

The development of highly selective Janus Kinase 1 (JAK1) inhibitors is crucial for improving efficacy and minimizing adverse effects in the clinical treatment of autoimmune diseases. In a prior study, we designed a series of C-5 4-pyrazol substituted pyrrolopyridine derivatives that demonstrated significant potency against JAK1, with a 10 ∼ 20-fold selectivity over Janus Kinase 2 (JAK2). Building on this foundation, we adopted orthogonal strategy by modifying the C-5 position with 3-pyrazol/4-pyrazol/3-pyrrol groups and tail with substituted benzyl groups on the pyrrolopyridine head to enhance both potency and selectivity.

Moral distress, moral resilience, and job embeddedness among pediatric nurses.

Background: Nurses often face ethical issues in their daily work that can have an impact on their level of job embeddedness. And positive job embeddedness is essential to reduce burnout among nurses and improve professional retention in the medical industry. However, few studies have focused on the relationship between moral distress, moral resilience, and job embeddedness.

Advances in β-Diketocyclisation of Curcumin Derivatives and their Antitumor Activity.

Curcumin, derived from the popular spice turmeric, is a pharmacologically active polyphenol. Curcumin's therapeutic activity has been extensively studied in recent decades, with reports implicating curcumin in many biological activities, particularly, its significant anticancer activity. However, its potential as an oral administration product is hampered by poor bioavailability, which is associated with a variety of factors, including low water solubility, poor intestinal permeability, instability, and degradation at alkaline pH.

Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B).

Developing new scaffolds for highly potent and selective inhibitors of human Monoamine Oxidase B (hMAO-B) is a crucial objective in enhancing the efficacy and safety in the clinical treatment of neurodegenerative diseases. In this study, we have identified a series of C-3 isoxazole-substituted thiochromone S,S-dioxide derivatives that exhibit strong inhibitory activity against hMAO-B. The strategy of oxidizing thiochromone to thiochromone S,S-dioxide solves the key defect of extreme insolubility observed for thiochromone analogues.

PhP/ICHCHI-promoted reductive deoxygenation of alcohols.

Owing to the ubiquity of the hydroxyl group, reductive deoxygenation of alcohols has become an active research area. The classic Barton-McCombie reaction suffers from a tedious two-step procedure. New efficient methods have been developed, but they have some limitations, such as a narrow substrate scope and the use of moisture-sensitive Lewis acids.

The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents.

Chemotherapy is the mainstay in the treatment of breast cancer. However, many drugs that are commonly used in clinical practice have a high incidence of side effects and multidrug resistance (MDR), which is mainly caused by overexpression of drug transporters and related enzymes in breast cancer cells. In recent years, researchers have been working hard to find newer and safer drugs to overcome MDR in breast cancer.

Recent progress in the development of ursolic acid derivatives as anti-diabetes and anti-cardiovascular agents.

Ursolic acid (UA) is a pentacyclic triterpenoid, which exhibits many biological activities, particularly in anti-cardiovascular and anti-diabetes. The further application of UA is greatly limited due to its low bioavailability and poor water solubility. Up to date, various UA derivatives have been designed to overcome these shortcomings.

Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1.

Developing selective inhibitors for Janus kinase 1 (JAK1) is a significant focus for improving the efficacy and alleviating the adverse effects in treating immune-inflammatory diseases. Herein, we report the discovery of a series of C-5 pyrazole-modified pyrrolopyrimidine derivatives as JAK1-selective inhibitors. The potential hydrogen bond between the pyrazole group and E966 in JAK1 is the key point that enhances JAK1 selectivity.

Jiella avicenniae sp. nov., a novel endophytic bacterium isolated from bark of Avicennia marina.

A Gram-stain-negative and short rod-shaped strain CBK1P-4, isolated from surface-sterilized bark of Avicennia marina was investigated by a polyphasic taxonomic approach to resolve its taxonomic position. Strain CBK1P-4 grew at 10-30 °C (optimum, 25 °C), pH 5.0-9.

Optimization of Railway Mixed Goods Loading Layout considering Stability.

It is well known that stability, center-of-gravity balance, and concentrated-weight are key factors of the transportation safety. The reasonable formulation of the loading layout scheme ensures the safety of shipment based on fully utilizing the effective volume and load capacity of freight vehicles. This paper takes the railway mixed goods loading layout as the research object, considering the constraints such as goods loading center-of-gravity balance, the allowable moment of concentrated-weight, supporting and goods placement mode, and taking the maximum comprehensive utilization rates for both effective volume and load capacity of freight vehicle as the optimization objective, an optimization model of railway mixed goods balanced and anticoncentrated-weight loading layout considering stability is built.

Study on the Design and Optimization of Learning Environment Based on Artificial Intelligence and Virtual Reality Technology.

More than half of the universities have recently added advanced technical courses for their students. The specialised courses would be the backbone to keep the students' knowledge updated. In that case, artificial intelligence (AI) and virtual reality (VR) have been lightened up recently.

Characteristics of Cracking Failure in Microbump Joints for 3D Chip-on-Chip Interconnections under Drop Impact.

With the rapid development of microelectronics packaging and integration, the failure risk of micro-solder joints in packaging structure caused by impact load has been increasingly concerning. However, the failure mechanism and reliability performance of a Cu-pillar-based microbump joint can use little of the existing research on board-level solder joints as reference, due to the downscaling and joint structure evolution. In this study, to investigate the cracking behavior of microbump joints targeted at chip-on-chip (CoC) stacked interconnections, the CoC test samples were subjected to repeated drop tests to reveal the crack morphology.

Dual Application of Waste Grape Skin for Photosensitizers and Counter Electrodes of Dye-Sensitized Solar Cells.

Dye-sensitized solar cells (DSSCs), a powerful system to convert solar energy into electrical energy, suffer from the high cost of the Pt counter electrode and photosensitizer. In this study, the dual application of waste grape skin is realized by employing the grape skin and its extract as the carbon source of the carbon-based counter electrode and photosensitizer, respectively. The ultraviolet-visible absorption and Fourier transform infrared spectroscopy verify the strong binding between the dye molecules (anthocyanins) in the extract and the TiO nanostructure on the photoanode, contributing to a high open-circuit voltage () value of 0.

sp. nov., a novel endophytic bacterium isolated from root of (Pilger) Rehd.

A Gram-staining-positive, aerobic, rod-shaped, endospore-forming bacterium, designated strain M5HDSG1-1, was originally isolated from a surface-sterilized root of (Pilger) Rehd. in Guizhou, PR China. This bacterium was tested by a polyphasic approach to determine its taxonomic position.

Effects of terrestrial and marine organic matters on deposition of dechlorane plus (DP) in marine sediments from the Southern Yellow Sea, China: Evidence from multiple biomarkers.

As an emerging halogenated organic contaminant, Dechlorane Plus (DP) was scarcely reported in marine environments, especially in China. In this work, 35 surface sediments and a sediment core were collected across the Southern Yellow Sea (SYS) to comprehensively explore the spatio-temporal distribution and possible migration pathway of DP. DP concentrations ranged from 14.

Method for generating multiple risky barcodes of complex diseases using ant colony algorithm.

Background: Susceptible barcode recognition plays an important role in the diagnosis and treatment of complex diseases. Numerous approaches have been proposed to identify risky barcodes involved in the progress of complex diseases. However, some methods only consider differences in barcode frequencies between the control and disease groups; as such, these methods may be partial or even wrong.

Indentification of vincamine indole alkaloids producing endophytic fungi isolated from Nerium indicum, Apocynaceae.

Vincamine, a monoterpenoid indole alkaloid which had been marketed as nootropic drugs for the treatment of cerebral insufficiencies, is widely found in plants of the Apocynaceae family. Nerium indicum is a plant belonging to the Apocynaceae family. So, the purpose of this research was designed to investigate the vincamine alkaloids producing endophytic fungi from Nerium indicum, Apocynaceae.