523,424 results match your criteria: "Department of Pharmacy & Radboud Institute for Health Sciences[Affiliation]"

Ferulic acid (FA) is a phenolic compound obtained naturally and is a versatile antioxidant identified for its potential in managing hypertension. However, its application is constrained due to its classification as a BCS Class IV moiety. To address this, we concentrated on improving its solubility and permeability by developing nanostructured lipid carriers (NLCs) of FA using emulsification probe sonication technique.

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Unfolding the Potential of Pyrrole- and Indole-Based Allylidene Hydrazine Carboximidamides as Antimicrobial Agents.

ACS Infect Dis

January 2025

Pharmaceutical Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Pilani, Vidya Vihar 333031, (RJ) India.

Antimicrobial drug resistance is a significant global health challenge, causing hundreds of thousands of deaths annually and severely impacting healthcare systems worldwide. Several reported antimicrobial compounds have a guanidine motif, as the positive charge on guanidine promotes cell lysis. Therefore, pyrrole- and indole-based allylidene hydrazine carboximidamide derivatives with guanidine motifs are proposed as antimicrobial agents that mimic cationic antimicrobial peptides (CAMPs).

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In this study, a new reversed phase high performance liquid chromatography method using two detectors was developed for the analysis of degradation and process impurities of ivabradine in pharmaceutical preparations. A PDA detector set to 285 nm wavelength and a QDa detector set to positive scan mode were used in the method. In the developed method, the separation process was carried out in a Zorbax phenyl column with a gradient application of a 0.

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Atopic dermatitis (AD), also known as eczema, is a chronic or relapsing inflammatory skin disease characterized by repeated exacerbations and remissions. Here, we investigated the effects of squid phospholipids (PLs) extracted from Todarodes pacificus on AD. The composition of squid PLs was analyzed using thin-layer chromatography and high-performance liquid chromatography, and the effects of PLs on AD were investigated using a rat paw edema model and an AD-like mouse model (NC/Nga mice).

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A fluorescent aptasensor was developed based on target-induced hairpin conformation switch coupled with nicking enzyme-assisted signal amplification (NESA) to detect the oligomeric form of ß-amyolid peptide (AβO) in cerebrospinal fluid. The hairpin DNA probe (HP) was specifically designed to recognize AβO. When AβO is present in the sensing system, it induces an HP conformational switch and triggers the NESA reaction.

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Statin use is reported to reduce the risk of Graves' orbitopathy (GO) in Western populations. However, study regarding the protective effect of statins against GO in Asians with Graves' disease (GD) is scarce. This study aims to investigate the efficacy of statins in preventing GO in Asian GD patients.

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Drug Property Optimization: Design, Synthesis, and Characterization of Novel Pharmaceutical Salts and Cocrystal-Salt of Lumefantrine.

Mol Pharm

January 2025

Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.

Lumefantrine (LMF) is a low-solubility antimalarial drug that cures acute, uncomplicated malaria. It exerts its pharmacological effects against erythrocytic stages of spp. and prevents malaria pathogens from producing nucleic acid and protein, thereby eliminating the parasites.

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Anxiety is one of the most common and debilitating mental health disorders, and is related to changes in interoception (perception of bodily states). While anxiety is more prevalent in women than men, gender differences in interoception-anxiety associations are often overlooked. Here, we examined gender-specific relationships between anxiety and interoception in the breathing domain, utilising multicentre data pooled from four study sites (N = 175; 51% women).

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Pharmacodynamics of NOSO-502 studied in vitro and in vivo: determination of the dominant pharmacodynamic index driver.

J Antimicrob Chemother

January 2025

Bristol Centre for Antimicrobial Research & Evaluation (BCARE), Infection Sciences, Southmead Hospital, Westbury-on-Trym, Bristol, UK.

Background: NOSO-5O2 is the first clinical candidate of a new antimicrobial class-the odilorhabdins. The pharmacodynamics of NOSO-502 were studied in vitro and in vivo to establish the pharmacodynamic index (PDI) driver.

Methods: A dilutional pharmacokinetic system was used for in vitro experiments.

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Aims: The gastrointestinal (GI) tract is composed of distinct sub-regions, which exhibit segment-specific differences in microbial colonization and (patho)physiological characteristics. Gut microbes can be collectively considered as an active endocrine organ. Microbes produce metabolites, which can be taken up by the host and can actively communicate with the immune cells in the gut lamina propria with consequences for cardiovascular health.

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Purpose: Intravitreal bevacizumab has been utilized to mitigate radiation retinopathy, yet the potential role of intravitreal melatonin for its prevention remains unexplored. This study aims to evaluate and compare the efficacy of intravitreal melatonin and bevacizumab in preventing radiation retinopathy in an experimental animal model.

Materials And Methods: Twelve healthy male New Zealand white rabbits ( = 24 eyes) received a single 3000 cGy irradiation dose in both eyes.

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The etiology of rheumatoid arthritis (RA) is multifaceted. One of the hypothesized pathways that results in the progression of RA is regulatory T cell (Treg) dysfunction. The pro-osteoclastogenic and immunogenic characteristics of microribonucleic acid (microRNA)-21 (miR-21) suggest its role in RA progression.

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Anticoagulation during extracorporeal membrane oxygenation.

Cochrane Database Syst Rev

June 2024

Department of Anesthesiology, Mayo Clinic, Rochester, MN, USA.

This is a protocol for a Cochrane Review (intervention). The objectives are as follows: To determine the efficacy and safety of anticoagulation for maintaining extracorporeal membrane oxygenation in people of all ages with cardiac or respiratory failure, or both.

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This is a protocol for a Cochrane Review (qualitative). The objectives are as follows: To explore the use of evidence from civil society in national and subnational health policy processes. The specific research questions will include the following.

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The outbreak of the monkeypox epidemic underscores the importance of developing a rapid and sensitive virus detection technique. Microneedles (MNs) offer minimally invasive sampling capabilities, providing a solution for the development of integrated extraction and diagnostic portable devices. Here, we report an integrated MNs and hydrogel biosensor (IMHB) platform, composed of an electronic device, an MN patch, and a hydrogel patch.

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detection of hypochlorous acid (HOCl) is critical for understanding its complex physiological and pathological roles. Fluorescent probes, known for their sensitivity and selectivity, are the preferred approach for such detections. Anthracene carboxyimide, an analog of naphthalimide, offers extended excitation and emission wavelengths, making it an excellent candidate for developing new fluorescent probes that address the limitations of naphthalimide.

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Discovery of WDR5-MLL1 and HDAC Dual-Target Inhibitors for the Treatment of Acute Myeloid Leukemia.

J Med Chem

January 2025

Jiangsu Key Laboratory of Drug Design and Optimization and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.

Targeting the WDR5-MLL1 protein-protein interaction (PPI) is considered to be an effective approach for the treatment of MLL-rearranged leukemia. However, interfering with WDR5-MLL1 PPI reduces methylated H3K4 levels and induces a decline in acetylated H3 levels, which may contribute to the suboptimal cellular efficacy of WDR5 inhibitors. We observed that cotreatment with WDR5-MLL1 PPI and HDAC inhibitors augmented the antiproliferative effect in MV-4-11 cells.

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Background And Aims: Primary sclerosing cholangitis (PSC) is a chronic cholestatic liver disease characterised by progressive biliary inflammation and fibrosis, leading to liver cirrhosis and cholangiocarcinoma. GPBAR1 (TGR5) is a G protein-coupled receptor for secondary bile acids. In this study, we have examined the therapeutic potential of BAR501, a selective GPBAR1 agonist in a PSC model.

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Purpose: Lung cancer mortality rates for American Indians (AIs) are the highest among US race groups. End-of-life (EOL) care presents opportunities to limit aggressive and potentially unnecessary treatment. We evaluated differences in EOL quality of care between AI and White (WH) decedents with lung cancer.

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Silicosis represents a formidable occupational lung pathology precipitated by the pulmonary assimilation of respirable crystalline silica particulates. This condition engenders a cascade of cellular oxidative stress via the activation of bioavailable silica, culminating in the generation of reactive oxygen species (ROS). Such oxidative mechanisms lead to irrevocable pulmonary impairment.

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Toward Grid-Based Models for Molecular Association.

J Chem Theory Comput

January 2025

Department of Biology, Chemistry and Pharmacy, Freie Universität Berlin, Arnimallee 22, 14195 Berlin, Germany.

This paper presents a grid-based approach to model molecular association processes as an alternative to sampling-based Markov models. Our method discretizes the six-dimensional space of relative translation and orientation into grid cells. By discretizing the Fokker-Planck operator governing the system dynamics via the square-root approximation, we derive analytical expressions for the transition rate constants between grid cells.

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Identification of a Chemical Probe for BLT2 Activation by Scaffold Hopping.

J Med Chem

January 2025

Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, and Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, Theodor-Stern-Kai 7, Frankfurt am Main 60596, Germany.

The leukotriene B4 receptor 2 (BLT2) is a G-protein coupled receptor, which is endogenously activated by 12()-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT). BLT2 is gaining attention as a potential therapeutic target involved in various pathologies including diabetic wound healing, ophthalmic diseases, and colitis. However, validation of BLT2 as drug target requires chemical probes and pharmacological tools which will allow for application in vivo.

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Antimicrobial resistance poses a growing threat to public health globally. Multidrug resistant Pseudomonas (P.) aeruginosa is detected in many infected wounds and is very challenging to treat with antibiotics.

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4-O-Methylglucuronoxylan from Hygrophila Ringens var. Ringens Seeds: Chemical Composition and Anti-Inflammatory Activity.

Macromol Biosci

January 2025

Friedrich Schiller University Jena, Institute for Organic Chemistry and Macromolecular Chemistry, Center of Excellence for Polysaccharide Research, Humboldtstraße 10, D-07743, Jena, Germany.

Hygrophila ringens var. ringens is a medicinal plant of the Acanthaceae family. A soluble polysaccharide is extracted from H.

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Seven-membered nitrogen-containing heterocycles, particularly azepine-based compounds, represent an intriguing class of molecules with vast arrays of applications. These compounds have garnered considerable attention in synthetic and medicinal chemistry due to their non-planar, non-aromatic features, which offer structural flexibility and diversity to design new drugs with improved pharmacological properties. This review summarizes the recent advances in the synthesis of azepine derivatives, including eco-friendly methodologies that align with the principles of green chemistry, which emphasize atom economy, sustainability, and waste reduction.

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