Synthesis and pharmacodynamic evaluation of 2-aminoindole derivatives against influenza A virus in vitro/vivo.

Influenza virus is a kind of respiratory pathogen with high morbidity and mortality, which still threatens human health. Existing anti-influenza drugs have various limitations, such as the inability to alleviate body injury and side effects. There remains an urgent need to develop a novel antiviral drug to efficiently inhibit viral infection while avoiding body injury.

Development of Phloroglucinol-Linked Tris-Quaternary Ammonium Salt Antimicrobial Peptide Mimics with Low Cytotoxicity and Broad-Spectrum Antibacterial Activity.

Encouraged by the significantly different toxicities and antibacterial activities of diverse linkers, such as alkyl and aromatic nuclei linkers, and the unique structure of phloroglucinol, we synthesized a series of tris-quaternary ammonium salt (tris-QAS) antibacterial peptide mimics based on the marketed drug phloroglucinol. Among them, displayed excellent activity against (MIC = 0.5 μg/mL) and high selectivity (SI > 2560).

Identification of Two Insulin Receptors from the Swimming Crab : Molecular Characterization, Expression Analysis, and Interactions with Insulin-Like Androgenic Gland Hormone.

AbstractThe insulin-like androgenic gland hormone is a crucial sexual regulator that is involved in the masculine sexual differentiation of crustaceans. As an insulin-like peptide, the insulin-like androgenic gland hormone has been proposed to act through the insulin receptor-mediated pathway. The present study cloned and characterized two insulin receptors ( and ) from the swimming crab hallmarked with a conserved intracellular tyrosine kinase catalytic domain and several other typical insulin receptor domains in their deduced amino acid sequences.

Electroacupuncture pretreatment inhibits ferroptosis and inflammation after middle cerebral artery occlusion in rats by activating Nrf2.

Objective: Electroacupuncture (EA) pretreatment can effectively increase the tolerance of the brain to ischemic stroke. The mechanism of ischemic tolerance induced by EA is related to Nrf2, but its specific mechanism has not been elucidated. This paper was designed to explore the effect of EA pretreatment on brain injury and the related mechanisms.

Synthesis and pharmacodynamic evaluation of Dihydropteridone derivatives against PDCoV in vivo and in vitro.

Porcine Delta Coronavirus (PDCoV) infection can induce serious dehydration, diarrhea and even death of piglets, which has caused huge losses to the breeding industry. PDCoV has been reported to have the potential for cross species transmission, and even reports of infecting humans have emerged. At present, there are still no effective prevention and control measures for PDCoV.

Low-Temperature and Fast-Charge Sodium Metal Batteries.

Low-temperature operation of sodium metal batteries (SMBs) at the high rate faces challenges of unstable solid electrolyte interphase (SEI), Na dendrite growth, and sluggish Na transfer kinetics, causing a largely capacity curtailment. Herein, low-temperature and fast-charge SMBs are successfully constructed by synergetic design of the electrolyte and electrode. The optimized weak-solvation dual-salt electrolyte enables high Na plating/stripping reversibility and the formation of NaF-rich SEI layer to stabilize sodium metal.

TRIM56 protects against nonalcoholic fatty liver disease by promoting the degradation of fatty acid synthase.

Nonalcoholic fatty liver disease (NAFLD) encompasses a disease continuum from simple steatosis to nonalcoholic steatohepatitis (NASH). However, there are currently no approved pharmacotherapies for NAFLD, although several drugs are in advanced stages of clinical development. Because of the complex pathophysiology and heterogeneity of NAFLD, the identification of potential therapeutic targets is clinically important.

A ddPCR platform based on a microfluidic chip with a dual-function flow-focusing structure for sample-to-result DNA quantification analysis.

Droplet digital PCR (ddPCR) is a powerful method for absolute nucleic acid quantification with high precision and accuracy. However, complicated operational steps have hampered the use and diffusion of ddPCR. Therefore, an automated, easy-to-use, low-sample-consumption, and portable ddPCR platform is urgently needed.

Design, synthesis, and anti-respiratory syncytial virus potential of novel 3-(1,2,3-triazol-1-yl)furoxazine-fused benzimidazole derivatives.

Respiratory syncytial virus (RSV) is a major cause of serious lower respiratory tract infections in infants, children, and older persons. Currently, the only approved anti-viral chemotherapeutic drug for RSV treatment is ribavirin aerosol; however, its significant toxicity has led to restricted clinical use. In a previous study, we developed various benzimidazole derivatives against RSV.

Synthesis and pharmacodynamic evaluation of naphthalene derivatives against influenza A virus in vitro and in vivo.

Influenza A virus is a highly mutable pathogenic pathogen that could cause a global pandemic. It is necessary to find new anti-influenza drugs to resist influenza epidemics due to the seasonal popularity of a certain area every year. Naphthalene derivatives had potential antiviral activity.

The influence of national policies on the evolution of industrial design education in China.

This study systematically describes research trends of "industrial design education in China" using bibliometrics mapping from 1992 to 2021. This study aims to sort out industrial design education's historical flow in China and analyze its intrinsic links with Chinese national policies. A combination of quantitative and qualitative methods is used to describe and analyze this study.

Experimental and theoretical study on the photoionization of styrene.

This study employed a vacuum ultraviolet synchrotron radiation source and reflectron time-of-flight mass spectrometry (TOF-MS) to investigate the photoionization and dissociation of styrene. By analyzing the photoionization mass spectrum and efficiency curve alongside G3B3 theoretical calculations, we determined the ionization energy of the molecular ion, appearance energy of fragment ions, and relevant dissociation pathways. The major ion peaks observed in the photoionization mass spectra of styrene correspond to C H , C H and C H .

Necroptosis inhibits autophagy by regulating the formation of RIP3/p62/Keap1 complex in shikonin-induced ROS dependent cell death of human bladder cancer.

Background: Shikonin, a natural naphthoquinone compound, has a wide range of pharmacological effects, but its anti-tumor effect and underlying mechanisms in bladder cancer remain unclear.

Purpose: We aimed to investigate the role of shikonin in bladder cancer in vitro and in vivo in order to broaden the scope of shikonin's clinical application.

Study Design And Methods: We performed MTT and colony formation to detect the inhibiting effect of shikonin on bladder cancer cells.

Synthesis and evaluation of alkoxy-substituted enamides against influenza A virus in vitro and in vivo.

Alkoxy-substituted enamides are often used as synthetic intermediates due to their special reactivity. To the best our knowledge, the biological activity of alkoxy-substituted amines has never been reported so far. We have synthesized a series of alkoxy-substituted enamides to study their anti-influenza A virus activity in vitro and in vivo.

Polydopamine-based nanomedicines for efficient antiviral and secondary injury protection therapy.

Viral infections continue to threaten human health. It remains a major challenge to efficiently inhibit viral infection while avoiding secondary injury. Here, we designed a multifunctional nanoplatform (termed as ODCM), prepared by oseltamivir phosphate (OP)-loaded polydopamine (PDA) nanoparticles camouflaged by the macrophage cell membrane (CM).

Targeting peroxisome proliferator-activated receptor γ proteasomal degradation by magnolol is a potential avenue for adipogenesis-mediated metabolic homeostasis.

Objective: Adipogenesis has been recognized as an attractive avenue for maintaining systemic homeostasis, with peroxisome proliferator-activated receptor γ (PPARγ) showing predominant roles in this process. This study aims to identify promising drug candidates by targeting PPARγ for adipogenesis-based metabolic homeostasis and to clarify the detailed mechanisms.

Methods: Molecular events contributing to adipogenesis were screened, which identified PPARγ as having the predominant role.

A high-throughput drug screening identifies luteolin as a therapeutic candidate for pathological cardiac hypertrophy and heart failure.

Background: Pathological cardiac hypertrophy is commonly resulted from sustained pressure overload and/or metabolic disorder and eventually leads to heart failure, lacking specific drugs in clinic. Here, we aimed to identify promising anti-hypertrophic drug(s) for heart failure and related metabolic disorders by using a luciferase reporter-based high-throughput screening.

Methods: A screen of the FDA-approved compounds based on luciferase reporter was performed, with identified luteolin as a promising anti-hypertrophic drug.

Intelligent fault detection scheme for constant-speed wind turbines based on improved multiscale fuzzy entropy and adaptive chaotic Aquila optimization-based support vector machine.

Timely and effective fault detection is essential to ensure the safe and reliable operation of wind turbines. However, due to the complex kinematic mechanisms and harsh working environments of wind turbine equipment, it is difficult to extract sensitive features and detect faults from acquired wind turbine signals. To address this challenge, a novel intelligent fault detection scheme for constant-speed wind turbines based on refined time-shifted multiscale fuzzy entropy (RTSMFE), supervised isometric mapping (SI), and adaptive chaotic Aquila optimization-based support vector machine (ACAOSVM) is proposed.

Honokiol acts as an AMPK complex agonist therapeutic in non-alcoholic fatty liver disease and metabolic syndrome.

Background: Non-alcoholic fatty liver (NAFLD) and its related metabolic syndrome have become major threats to human health, but there is still a need for effective and safe drugs to treat these conditions. Here we aimed to identify potential drug candidates for NAFLD and the underlying molecular mechanisms.

Methods: A drug repositioning strategy was used to screen an FDA-approved drug library with approximately 3000 compounds in an in vitro hepatocyte model of lipid accumulation, with honokiol identified as an effective anti-NAFLD candidate.

The influence of target layout and target graphic type on searching performance based on eye-tracking technology.

With the development of various intelligent technologies, the application of interactive interfaces is becoming more and more widespread, and the related researches conducted for interactive interfaces are also increasing. The purpose of this study was to explore the influence of icon layout location, icon graphic type, and icon layout method on users' searching performance in interactive interfaces through eye-tracking technology. Participants were asked to perform search tasks for the search target (facet icon or linear icon) on each image.

Ensemble Dilated Convolutional Neural Network and Its Application in Rotating Machinery Fault Diagnosis.

Fault diagnosis of rotating machinery is an attractive yet challenging task. This paper presents a novel intelligent fault diagnosis scheme for rotating machinery based on ensemble dilated convolutional neural networks. The novel fault diagnosis framework employs a model training strategy based on early stopping optimization to ensemble several one-dimensional dilated convolutional neural networks (1D-DCNNs).