Anti-Mycobacterial Activity of Bacterial Topoisomerase Inhibitors with Dioxygenated Linkers.

Developing new classes of drugs that are active against infections caused by is a priority for treating and managing this deadly disease. Here, we describe screening a small library of 20 DNA gyrase inhibitors and identifying new lead compounds. Three structurally diverse analogues were identified with minimal inhibitory concentrations of 0.

Public perceptions and attitudes of drive-through pharmacy services: Insights from a cross-sectional survey in Saudi Arabia.

Disease-related fatalities in Saudi Arabia (SA) are on the rise, with 28% of all deaths attributed to cardiovascular diseases, followed by cancer, diabetes, and chronic respiratory disorders. In response to this issue, pharmacy dispensing practices have been significantly altered. One such innovative approach is the drive-through pharmacy service.

Phytochemicals Withanolide N and Dryobalanolide as Potential Bioactive Leads for Developing Anticancer Drugs Targeting Tyrosine-Protein Kinase Mer.

There is a growing interest in harnessing natural compounds and bioactive phytochemicals to accelerate drug discovery and development, including in the treatment of human cancers. Receptor tyrosine kinases (RTKs) are critical regulators of many fundamental cellular processes and have been implicated in cancer pathogenesis as well as targets for anticancer drug development. The members of TAM, Tyro3, Axl, and MERTK subfamily RTKs, especially Mer, affect immune homeostasis in the tumor microenvironment.

Sensory Characteristics and Impact of Flavanol-Rich Grape and Blueberry Extract on Blood Flow Velocity and Oxidative Stress.

Background: Several epidemiological studies and intervention trials have demonstrated that grapes and blueberries, which are rich in flavanols, can lower the risk of cardiovascular disease. However, the mechanisms of action of these compounds remain unclear due to their low bioavailability.

Objective: This study aimed to characterize the sensory properties, blood flow velocity, and oxidative stress of a polyphenol rich grape and blueberry extract (PEGB) containing approximately 16% flavanols (11% monomers and 4% dimers).

Drug repurposing for sustainable antimicrobial use: exploring pharmacists' awareness, attitudes, facilitators and barriers.

This study utilized a validated questionnaire that aimed to assess pharmacists' awareness and attitude towards drug repurposing for antimicrobial use. Despite the reasonable awareness, pharmacists reported unfavourable attitudes. Pharmacists with a B.

Ultra-Sensitive Gaseous Styrene and Isoprene Detection with a Ratiometric Fluorescence Probe of Eu(III)-Incorporated UiO-67.

The development of probes for the efficient detection of volatile organic compounds is crucial for both human health protection and environmental monitoring. In this study, we successfully synthesized a ratiometric fluorescent sensing material [Eu-UiO-67 (1:1)], featuring dual-emission fluorescence peaks via a one-pot method. This material demonstrated exceptional ratiometric fluorescence recognition properties for liquid styrene and isoprene, achieving low limit of detections (LODs) of 6.

A Five-Year Analysis of Market Share and Sales Growth for Original Drugs after Patent Expiration in Korea.

Introduction: The sales patterns of original drugs after patent expiration in Korea show a relatively high market share and continuous sales growth differently from those in the U.S. and European countries.

Medicaid Policy and Hepatitis C Treatment Among Rural People Who Use Drugs.

Background: Restrictive Medicaid policies regarding hepatitis C virus (HCV) treatment may exacerbate rural health care disparities for people who use drugs (PWUD). We assessed associations between Medicaid restrictions and HCV treatment among rural PWUD.

Methods: We compiled state-specific Medicaid treatment policies across 8 US rural sites in 10 states and merged these with participant survey data.

The Aryl Hydrocarbon Receptor (AhR) Is a Novel Gene Involved in Proper Physiological Functions of Pancreatic β-Cells.

The Kynurenine pathway is crucial in metabolizing dietary tryptophan into bioactive compounds known as kynurenines, which have been linked to glucose homeostasis. The aryl hydrocarbon receptor (AhR) has recently emerged as the endogenous receptor for the kynurenine metabolite, kynurenic acid (KYNA). However, the specific role of AhR in pancreatic β-cells remains largely unexplored.

Exploring Patient Activation and Compliance in Patients with Different Rheumatological Disorders.

This study aimed to assess patient activation using patient activation measure 13 (PAM-13) in systemic lupus erythematosus (SLE), psoriatic arthritis (PsA), and axial spondyloarthritis (axSPA). A cross-sectional study was conducted involving patients with three rheumatological conditions (SLE, PsA, and axSPA). Patients were contacted either at the clinic or through social media platforms.

Machine Learning Algorithm-Based Prediction of Diabetes Among Female Population Using PIMA Dataset.

: Diabetes is a metabolic disorder characterized by increased blood sugar levels. Early detection of diabetes could help individuals to manage and delay the progression of this disorder effectively. Machine learning (ML) methods are important in forecasting the progression and diagnosis of different medical problems with better accuracy.

A multicenter micro-costing analysis of flexible cystoscopic procedures in Korea.

Purpose: This study aims to develop and implement an economic evaluation using a micro-costing approach to provide a precise and transparent analysis of the direct costs of cystoscopic procedures in Korean hospitals. The study seeks to identify key cost components and evaluate whether current reimbursement rates accurately reflect these direct costs.

Materials And Methods: Significant variations in cost items were identified across different studies.

Recent Developments in Azetidinone-Azole Conjugates: Emerging Antimicrobial Potentials.

The emergence of multidrug-resistant microbial strains poses a significant challenge to global public health. In response, researchers have been exploring innovative antimicrobial agents with enhanced efficacy and novel mechanisms of action. One promising approach involves the synthesis of hybrid molecules combining azetidinone and azole moieties, capitalizing on the respective antimicrobial properties of both structural elements.

Anti-neuroinflammatory and Neuroprotective Effects of T-006 on Alzheimer's Disease Models by Modulating TLR4-Mediated MyD88/ NF-κB Signaling.

Introduction: Neuroinflammation derived from the activation of the microglia is considered a vital pathogenic factor of Alzheimer's Disease (AD). T-006, a tetramethylpyrazine derivative, has been found to alleviate cognitive deficits via inhibiting tau expression and phosphorylation in AD transgenic mouse models. Recently, T-006 has been proven to dramatically decrease the levels of total Amyloid β (Aβ) peptide and Glial Fibrillary Acidic Protein (GFAP) and suppress the expression of ionized calcium binding adaptor molecule-1 (Iba-1) in APP/PS1 mice.

Diabetic Wound Healing: Factors, Mechanisms, and Treatment Strategies Using Herbal Components.

Managing diabetic wounds is a significant challenge for healthcare professionals since severe complications and delayed recovery greatly impact the patients' quality of life. This article aimed to explore various factors affecting diabetic wound healing, the mechanism of wound healing, and potential natural products having wound healing capability. It focuses on mechanisms of action and the therapeutic effectiveness of the compounds employed in the management of diabetic wounds.

One-Step Synthesis of 2-Arylquinolin-4(1)-Ones from 1-(2-Aminoaryl)-3-Arylpropan-1-Ones via Pd(II)-Catalyzed Dehydrogenative Cyclization.

In this study, we developed palladium-catalyzed dehydrogenative cyclization to transform 1-(2-aminoaryl)-3-arylpropan-1-ones into 2-arylquinolin-4(1)-ones, also known as aza-flavones which are the bioisosteres of flavones, in an atom-economic manner. This method exhibited excellent chemical compatibility with a broad substrate scope, accommodating up to 25 derivatives. Additionally, kinetic studies were performed to elucidate the reaction mechanism.

Siblings With Berardinelli-Seip Congenital Lipodystrophy: Clinical Insights and Challenges.

Berardinelli-Seip congenital lipodystrophy (BSCL), also known as congenital generalized lipodystrophy (CGL), is an exceptionally rare autosomal recessive disorder marked by a significant deficiency of adipose tissue throughout the body. This lack of adipose tissue, normally found beneath the skin and between internal organs, leads to impaired adipocyte formation and fat storage, causing lipids to accumulate in atypical tissues such as muscles and the liver. The extent of adipose tissue loss directly influences the severity of symptoms, which can include a muscular appearance, increased appetite, bone cysts, marrow fat depletion, acromegalic features, severe insulin resistance, skeletal muscle hypertrophy, hypertrophic cardiomyopathy, hepatic steatosis, hepatomegaly, cirrhosis, and intellectual disability.

Anti-angiogenic and anti-oxidant effects of 2-NTI indole derivative vs. suramin in ex vivo, in vivo, and in vitro studies.

Angiogenesis is an intricate pathway that involves the formation of new blood capillaries from old, functioning ones. Improper angiogenesis is a feature of numerous maladies, including malignancy and autoimmune disorders. Indole-related derivatives are believed to interfere with the mitotic spindle, inhibiting the multiplication, and invasion of cancerous human cells.

Week 96 Results of Bictegravir/Emtricitabine/Tenofovir Alafenamide for HIV Treatment in People With Substance Use Disorders.

Background: The BASE study (NCT03998176), a phase 4, 48-week (W), single-arm, prospective trial, revealed that the use of bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) in people with HIV and substance use disorders (PWH/SUD) was safe and effective without emergent antiretroviral resistance despite incomplete adherence. Here, we present the W96 results.

Methods: A retrospective analysis of all participants enrolled in the BASE study was completed from W48 to W96.

Development of a Novel Intraperitoneal Icodextrin/Dextrose Solution for Enhanced Sodium Removal.

Rationale & Objective: Peritoneal dialysis (PD) solutions provide both clearance of uremic toxins and sodium and water. An intraperitoneal (IP) solution of icodextrin and glucose designed without the requirement for uremic toxin clearance could provide substantially greater sodium and water removal than PD solutions.

Study Design: We examined varying concentrations of icodextrin and dextrose IP solutions in rats.

Therapeutic Potential of Hongjam in A Diethylnitrosamine and Thioacetamide-induced Hepatocellular Carcinoma Mouse Model.

Hepatocellular carcinoma (HCC) is the most common and lethal type of primary liver cancer, frequently arising from chronic liver injury and inflammation. Despite treatment advancements, HCC prognosis remains poor, emphasizing the need for effective preventive and therapeutic strategies. This study investigates the hepatoprotective and anti-tumor effects of Hongjam, a steamed freeze-dried silkworm powder, in a diethylnitrosamine (DEN) and thioacetamide (TAA)-induced HCC mouse model.

Non-canonical Function of Prolyl Hydroxylase Domain 2 in Breast Cancer Cell Growth and Progression: Role of Peptidyl-prolyl Cis-trans Isomerase NIMA-interacting 1.

Prolyl hydroxylase domain 2 (PHD2) is the primary oxygen sensing enzyme involved in hydroxylation of hypoxia-inducible factor (HIF). Under normoxic conditions, PHD2 hydroxylates specific proline residues in HIF-1α and HIF-2α, promoting their ubiquitination and subsequent proteasomal degradation. Although PHD2 activity decreases in hypoxia, notable residual activity persists, but its function in these conditions remains unclear Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) targets proteins with phosphorylated serine/threonine-proline (pSer/Thr-Pro) motifs.

Kelch-like ECH-associated Protein 1/Nuclear Factor Erythroid 2-related Factor 2 Pathway and Its Interplay with Oncogenes in Lung Tumorigenesis.

Nuclear factor erythroid 2-related factor 2 (NRF2), a transcription factor regulating cellular redox homeostasis, exhibits a complex role in cancer biology. Genetic mutations in the Kelch-like ECH-associated protein 1 (KEAP1)/NRF2 system, which lead to NRF2 hyperactivation, are found in 20% to 30% of lung cancer cases. This review explores the intricate interplay between NRF2 and key oncogenic pathways in lung cancer, focusing on the interaction of KEAP1/NRF2 system with Kirsten rat sarcoma virus (KRAS), tumor protein P53 (TP53), epidermal growth factor receptor (EGFR), and phosphatidylinositol 3-kinases (PI3K)/AKT signaling.

Dual EGFR and telomerase inhibitory potential of new triazole tethered Schiff bases endowed with apoptosis: design, synthesis, and biological assessments.

Many cancers have displayed resistance to chemotherapeutic drugs over the past few decades. EGFR has emerged as a leading target for cancer therapy inhibiting tumor angiogenesis. Besides, studies strongly suggest that blocking telomerase activity could be an effective way to control the growth of certain cancer cells.

Proteomics: An In-Depth Review on Recent Technical Advances and Their Applications in Biomedicine.

Proteins hold pivotal importance since many diseases manifest changes in protein activity. Proteomics techniques provide a comprehensive exploration of protein structure, abundance, and function in biological samples, enabling the holistic characterization of overall changes in organisms. Nowadays, the breadth of emerging methodologies in proteomics is unprecedentedly vast, with constant optimization of technologies in sample processing, data collection, data analysis, and its scope of application is steadily transitioning from the bench to the clinic.