Design, synthesis, and biological evaluation of highly potent and selective hMAO-B inhibitors featuring a tetrahydrobenzo[f][1,4]oxazepine core.

The advancement of human monoamine oxidase B (hMAO-B) inhibitors for the management of Parkinson's disease (PD) has seen notable progress, however, the clinical application of existing hMAO-B inhibitors is hindered by their limited efficacy and associated adverse effects. This article presents highly potent and selective hMAO-B inhibitors characterized by either a 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepine core or a 2,3,4,5-tetrahydro-1H-benzo[c]azepine core. These compounds were designed through the cyclization of the amine group with the phenyl ring of safinamide, a second-generation hMAO-B inhibitor that has received approval for PD treatment.

Application progress of magnetic resonance imaging in thyroid associated ophthalmopathy.

Thyroid associated ophthalmopathy (TAO) is an autoimmune orbital disease associated with thyroid dysfunction, which may significantly impact the appearance and quality of life of patients. The course of TAO includes active stage and inactive stage, and the treatment methods are different in different stages. The clinical activity score is often used to evaluate the activity of TAO, but it is easy to be affected by subjective factors because it is based on the symptoms and signs of patients.

Emergence of ciprofloxacin- and tigecycline-resistant extended-spectrum β-lactamase (ESBL)-producing Salmonella enterica serovar Kentucky ST198 from horse, China.

Objectives: Salmonella enterica serovar Kentucky ST198 has been increasingly reported in diverse sources worldwide, emerging as a globally epidemic clone. In this study, we aim to characterise the first isolated S. Kentucky ST198 strain from a horse in China.

Development of NIR-II Ratiometric Fluorescent Nanoprobe for HClO Imaging in Acute Lung Injury.

Efficient and high-contrast bioimaging of acute lung injury (ALI) is crucial for studying disease progression and enabling timely interventional treatments. However, developing bioimaging probes in the second near-infrared (NIR-II) window to assess ALI remains challenging. In particular, ratiometric NIR-II probes with self-calibration functions are rare, hindering reliable detection of information during the ALI process.

[Sequential treatment with siltuximab and tocilizumab for childhood idiopathic multicentric Castleman disease: a case report].

The patient, an 11-year-old girl, was admitted with recurrent fever for 20 days, worsening with abdominal distension for 7 days. Upon admission, she presented with recurrent fever, lymphadenopathy, hepatosplenomegaly, polyserositis, and multiple organ dysfunction. Lymph node pathology and clinical manifestations confirmed the diagnosis of idiopathic multicentric Castleman disease-TAFRO syndrome.

Neuroprotective Effects of Tectoridin in HO-Induced Oxidative Stress and an Amyloid-Infused Rat Model of Alzheimer's Disease.

This study aims to examine the effects of tectoridin in both in vitro and in vivo models of Alzheimer's disease. In vitro, oxidative stress was induced in PC12 cells using 400 µM of hydrogen peroxide (H₂O₂) to simulate cellular damage. In vivo, a rat model of Alzheimer's disease was established through repeated intracerebroventricular administration of soluble amyloid-beta (Aβ1-42) to induce neurodegeneration.

Inverse association of healthy diet scores with non-alcoholic fatty liver disease among Chinese patients with type 2 diabetes mellitus.

We aimed to investigate the association of healthy diet scores (HDS), comprising major components (fruits and vegetables, soybean, fish, and sugar-sweetened beverages), with non-alcoholic fatty liver disease (NAFLD) in patients with type 2 diabetes mellitus (T2DM). In this cross-sectional study of 2,404 T2DM individuals aged 35-70 years, individuals with higher HDS (≥3 components) had a lower odds of NAFLD (adjusted odds ratio [OR]: 0.64; 95% confidence interval [CI]: 0.

Metabolomic profiling of adenine-induced CKD: pathway interconnections and kidney injury.

Chronic kidney disease (CKD) is acknowledged as one of the largest public health problems in the world, characterized by a complex and diverse pathogenesis. Adenine-induced CKD, a classical model with multiple injury mechanisms, has been extensively employed in CKD research. However, the complete elucidation of the mechanisms underlying adenine-induced CKD remains elusive.

Development of Dual-Responsive Fluorescent Probe for Drug Screening of Diabetes Cardiomyopathy.

For specific drug research and development, a drug-screening strategy (DSS) plays an indispensable role in the biomedical field. Unfortunately, traditional strategies are complicated and insufficiently accurate due to the widely used single-target screening method. Herein, a simple dual-target-based drug-screening strategy (dt-DSS) is proposed to screen highly effective drugs by fluorescence imaging.

Dihydropyridopyrazine Functionalized Xanthene: Generating Stable NIR Dyes with Small-Molecular Weight by Enhanced Charge Separation.

Near-infrared region (NIR; 650-1700 nm) dyes offer many advantages over traditional dyes with absorption and emission in the visible region. However, developing new NIR dyes, especially organic dyes with long wavelengths, small molecular weight, and excellent stability and biocompatibility, is still quite challenging. Herein, we present a general method to enhance the absorption and emission wavelengths of traditional fluorophores by simply appending a charge separation structure, dihydropyridopyrazine.

Inhaled aerosolized algal polysaccharides: A novel and reliable strategy for treating pneumonia through inflammation and oxidative stress inhibition.

Sepsis-associated acute lung injury (ALI) poses a significant threat, characterized by inflammation and oxidative damage. Effective drugs targeting these aspects with reliable drug delivery systems are vital for ALI management. This study aimed to evaluate the influence of algal polysaccharides (APs) with aerosolized drug delivery in ALI mice and clarify the underlying mechanism.

Early embryonic failure caused by a novel mutation in the gene: A case report.

Background: This study aimed to explore the relationship between gene mutations and early embryonic development arrest and to provide more possibilities for the diagnosis and treatment of repeated implantation failure.

Case Summary: Here, we collected and described the clinical data of a patient with early embryonic development stagnation after repeated fertilization attempts for primary infertility at the Department Reproductive Center of Zaozhuang Maternal and Child Healthcare Hospital. We also detected the whole-exon gene of the patient's spouse and parents, and conducted bioinformatics analysis to determine the pathogenesis of the gene.

Discovery of novel and potent CDK8 inhibitors for the treatment of acute myeloid leukaemia.

It has been reported that CDK8 plays a key role in acute myeloid leukaemia. Here, a total of 40 compounds were rational designed and synthesised based on the previous SAR. Among them, compound () showed the most potent inhibiting activity against CDK8 with an IC value of 39.

A new perspective on the current and future development potential of ABCG1.

ABCG1 is an essential protein involved in the efflux of intracellular cholesterol to the extracellular space, thus playing a critical role in reducing cholesterol accumulation in neighboring tissues. Bibliometric analysis pertains to the interdisciplinary field of quantitative examination of diverse documents using mathematical and statistical techniques. It integrates the investigation of structural and temporal patterns in academic publications with an exploration of subject focus and forms of uncertainty.

Correlation of Coagulation Dysfunction with Infection and Hypercapnia in Acute Exacerbation of COPD Patients.

Background: This study aims to explore the factors influencing the coagulation function of patients with chronic obstructive pulmonary disease (COPD) and its effects on thrombosis.

Methods: A total of 155 COPD patients, including 118 patients with acute exacerbation of COPD (AECOPD) and 37 patients with stable COPD (SCOPD), were enrolled in this study. Meanwhile, 50 patients with gastrointestinal polyps found during physical examination and treated with surgery in the same period were enrolled as the control group.

In situ orderly self-assembly strategy affording NIR-II-J-aggregates for in vivo imaging and surgical navigation.

J-aggregation, an effective strategy to extend wavelength, has been considered as a promising method for constructing NIR-II fluorophores. However, due to weak intermolecular interactions, conventional J-aggregates are easily decomposed into monomers in the biological environment. Although adding external carriers could help conventional J-aggregates stabilize, such methods still suffer from high-concentration dependence and are unsuitable for activatable probes design.

Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia.

CDK8 plays a key role in acute myeloid leukemia, colorectal cancer and other cancers. Here, a total of 54 compounds were designed and synthesized. Among them, the most potent one compound 43 (3-(1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide), a novel CDK8 Ⅰ inhibitor, showed strong inhibitory activity against CDK8 (IC = 51.

Neck-to-height ratio is positively associated with diabetic kidney disease in Chinese patients with type 2 diabetes mellitus.

Introduction: The aim of this study was to investigate the associations of neck circumference (NC) and neck-to-height (NHR) with diabetic kidney disease (DKD) in Chinese patients with type 2 diabetes mellitus (T2DM).

Materials And Methods: A total of 2,615 patients with prevalent T2DM were enrolled. NHR was calculated through NC (cm) divided by height (cm), and prevalent DKD was defined as the urinary albumin-to-creatinine ratio (UACR) ≥ 30 mg/g or the estimated glomerular filtration rate (eGFR) < 60 ml/min per 1.

Olfactory mucosa tissue-derived mesenchymal stem cells lysate ameliorates LPS-induced acute liver injury in mice.

Background: Acute liver injury (ALI) induced by sepsis seriously endangers the health of human beings every year. Mesenchymal stem cells (MSCs) lysate containing various regulators had a positive effect on anti-inflammation, hoping to provide a promising strategy in ALI.

Methods: Olfactory mucosa-derived mesenchymal stem cells (OM-MSCs) were extracted and identified.

Inverse Association of Fruit and Vegetable Consumption with Nonalcoholic Fatty Liver Disease in Chinese Patients with Type 2 Diabetes Mellitus.

We aimed to investigate the association of fruit and vegetable consumption with nonalcoholic fatty liver disease (NAFLD) in Chinese patients with type 2 diabetes mellitus (T2DM). This cross-sectional study included 2667 Chinese patients with T2DM aged 18 to 76 years from March 2017 to October 2021. Dietary intake was assessed using a food frequency questionnaire, and prevalent NAFLD was diagnosed with abdominal ultrasonography.