Design, Synthesis, Antitumor Activity and NMR-Based Metabolomics of Novel Amino Substituted Tetracyclic Imidazo[4,5-b]Pyridine Derivatives.

Newly prepared tetracyclic imidazo[4,5-b]pyridine derivatives were synthesized to study their antiproliferative activity against human cancer cells. Additionally, the structure-activity was studied to confirm the impact of the N atom position in pyridine nuclei as well as the chosen amino side chains on antiproliferative activity. Targeted amino substituted regioisomers were prepared by using uncatalyzed amination from corresponding chloro substituted precursors.

Photodynamic inactivation of E. coli with cationic imidazolyl-porphyrin photosensitizers and their synergic combination with antimicrobial cinnamaldehyde.

Bacterial infections are a global health concern, particularly due to the increasing resistance of bacteria to antibiotics. Multi-drug resistance (MDR) is a considerable challenge, and novel approaches are needed to treat bacterial infections. Photodynamic inactivation (PDI) of microorganisms is increasingly recognized as an effective method to inactivate a broad spectrum of bacteria and overcome resistance mechanisms.

Biochar-derived dissolved organic matter enhanced the release of residual ciprofloxacin from the soil solid phase.

Biochar has been utilized to reduce ciprofloxacin (CIP) residues in soil. However, little is known about the effect of biochar-derived dissolved organic matter (DOM) on residual CIP transformation. Thus, we analyzed the residual soil CIP as influenced by biochar generated from rice straw (RS3 and RS6), pig manure (PM3 and PM6), and cockroach shell (CS3 and CS6) at 300 °C and 600 °C.

Improved Chemical and Radiochemical Synthesis of Neuropeptide Y Y Receptor Antagonist -Methyl-JNJ-31020028 and Preclinical Positron Emission Tomography Studies.

Neuropeptide Y (NPY) is one of the most abundant peptides in the central nervous system of mammals and is involved in several physiological processes through NPY Y, Y, Y and Y receptors. Of those, the Y receptor has particular relevance for its autoreceptor role in inhibiting the release of NPY and other neurotransmitters and for its involvement in relevant mechanisms such as feeding behaviour, cognitive processes, emotion regulation, circadian rhythms and disorders such as epilepsy and cancer. PET imaging of the Y receptor can provide a valuable platform to understand this receptor's functional role and evaluate its potential as a therapeutic target.

Impact of equipment technology on reference levels in fluoroscopy-guided gastrointestinal procedures.

Objectives: To evaluate the effect of equipment technology on reference point air kerma (K), air kerma-area product (P), and fluoroscopic time for fluoroscopically-guided gastrointestinal endoscopic procedures and establish benchmark levels.

Methods: This retrospective study included the consecutive patients who underwent fluoroscopically-guided gastrointestinal endoscopic procedures from May 2016 to August 2023 at a tertiary care hospital in the U.S.

Polysaccharide-fecal microbiota-based colon-targeted self-nanoemulsifying drug delivery system of curcumin for treating polycystic ovarian syndrome.

The gut microbiome is involved in the pathogenesis of many diseases including polycystic ovarian syndrome (PCOS). Modulating the gut microbiome can lead to eubiosis and treatment of various metabolic conditions. However, there is no proper study assessing the delivery of microbial technology for the treatment of such conditions.

Engineered nanomicelles inhibit the tumour progression via abrogating the prostaglandin-mediated immunosuppression.

Cancer treatment is challenged due to immunosuppressive inflammatory tumour microenvironment (TME) caused by infiltration of tumour-promoting and inhibition of tumour-inhibiting immune cells. Here, we report the engineering of chimeric nanomicelles (NMs) targeting the cell proliferation using docetaxel (DTX) and inflammation using dexamethasone (DEX) that alters the immunosuppressive TME. We show that a combination of phospholipid-DTX conjugate and PEGylated-lipid-DEX conjugate can self-assemble to form sub-100 nm chimeric NMs (DTX-DEX NMs).

The association of off-hour vs. on-hour intensive care unit admission time with mortality in patients with cardiogenic shock: a retrospective multi-centre analysis.

Aims: Studies have shown a so-called off-hour effect for many different diseases, but data are scarce concerning cardiogenic shock. We therefore assessed the association of off-hour vs. on-hour intensive care unit admission with 30-day mortality in patients with cardiogenic shock.

Optimizing workflow of urgent stroke endovascular intervention: A focused lean six sigma project.

Introduction: Urgent endovascular intervention is currently accepted as the primary and critical therapeutic approach to patients whose acute ischemic stroke results from a large arterial occlusion (LAO). In this context, one of the quality metrics most widely applied to the assessment of emergency systems performance is the "door-to-puncture" (D-P) time. We undertook a project to identify the subinterval of the D-P metric causing the most impact on workflow delays and created a narrowly focused project on improving such subinterval.

Chlorination-Promoted Skeletal Transformations in Isolated-Pentagon Rule (IPR) Isomers of Fullerene C to Non-IPR Chloro- and Trifluoromethyl Derivatives.

Fullerene C contains two isomers obeying the Isolated-Pentagon Rule (IPR), -C(16) and -C(17). Both isomers undergo unprecedented skeletal transformations at high-temperature (400 °C) chlorination with SbCl. One-step Stone-Wales rearrangement (SWR) in C(17) results in the pentagon-fused C cage found in the structure of CCl.

Scalable Production of Peptides for Enhanced Struvite Formation via Expression on the Surface of Genetically Engineered Microbes.

A promising method for recycling phosphate from wastewater is through precipitation of struvite (MgNHPO·6HO), a slow-release fertilizer. Peptides have been shown to increase the yield of struvite formation, but producing peptides via solid phase synthesis is cost prohibitive. This work investigates the effects of peptide-expressing bacteria on struvite precipitation to provide a sustainable and cost-efficient means to enhance struvite precipitation.

Azorean Black Tea () Antidermatophytic and Fungicidal Properties.

The treatment of dermatophytoses, the most common human fungal infections, requires new alternatives. The aim of this study was to determine the antidermatophytic activity of the aqueous Azorean Black Tea extract (ABT), together with an approach to the mechanisms of action. The phytochemical analysis of ABT extract was performed by HPLC.

Synthesis and In Vitro Biocompatibility Studies of Novel Alkoxy 4,4-Difluoro-4-bora-3a,4a-diaza-s-indacenes.

BODIPYs are bicyclic aromatic compounds with unique spectroscopic, photophysical, and chemical properties. This study aimed to find BODIPYs with characteristics biocompatible with human cell lines for possible use as imaging agents. Six BODIPY derivatives were synthesised with groups linked to boron, fluorine, phenol, or catechol, resulting in compounds with different physicochemical characteristics.

Synergistic approach for synthesis of functionalized biochar for efficient adsorption of Lopinavir from polluted water.

The COVID-19 pandemic has led to a significant increase in antibiotic consumption, along with a 70% rise in antiviral drug concentrations in aquatic ecosystems. For the effective adsorption of antibiotics, biochar was modified by incorporating layered double hydroxide (LDH) through hydrothermal method. The results showed that LDH provides additional hydroxyl groups, positive surface charges and ion exchange.

Comparative Study of Inhaled Fluticasone Versus Oral Prednisone in 30 Dogs with Cough and Tracheal Collapse.

Coughing is common in dogs with tracheal collapse (TC). The use of inhaled corticosteroids is less widespread than oral ones. This study aims to compare the effects of oral and inhaled corticosteroids in dogs with cough and TC.

CogDrisk, ANU-ADRI, CAIDE, and LIBRA Risk Scores for Estimating Dementia Risk.

Importance: While the Australian National University-Alzheimer Disease Risk Index (ANU-ADRI), Cardiovascular Risk Factors, Aging, and Dementia (CAIDE), and Lifestyle for Brain Health (LIBRA) dementia risk tools have been widely used, a large body of new evidence has emerged since their publication. Recently, Cognitive Health and Dementia Risk Index (CogDrisk) and CogDrisk for Alzheimer disease (CogDrisk-AD) risk tools have been developed for the assessment of dementia and AD risk, respectively, using contemporary evidence; comparison of the relative performance of these risk tools is limited.

Objective: To evaluate the performance of CogDrisk, ANU-ADRI, CAIDE, LIBRA, and modified LIBRA (LIBRA with age and sex estimates from ANU-ADRI) in estimating dementia and AD risks (with CogDrisk-AD and ANU-ADRI).

Creatine and creatinine quantified using nuclear magnetic resonance: A method validation study and clinical associations between circulating creatine and fatigue in kidney transplant recipients.

Background: A potential contributor to fatigue in kidney transplant recipients (KTR) may be impaired creatine homeostasis. We developed and validated a high-throughput NMR assay allowing for simultaneous measurement of circulating creatine and creatinine, and determined plasma creatine and estimated intramuscular creatine concentrations in KTRs, delineated their determinants and explored their associations with self-reported fatigue.

Methods: An NMR assay was developed and validated for measurement of circulating creatinine and creatine concentrations.

Metabolism of vitamin D is not affected by sport activity.

Background: Higher levels of physical activity are related to higher 25-(OH)D levels. Total 25-(OH)D (25-(OH)D) are routinely used in clinical practice to assess vitamin D, however novel biomarkers are currently being investigated as free 25-(OH)D (25-(OH)D) or vitamin D metabolite ratios (VMRs). The primary aim of our study was to assess 25-(OH)D, vitamin D metabolites and VMRs in inactive men and athletes.

Selective Inhibition of Na1.8 with VX-548 for Acute Pain.

Background: The Na1.8 voltage-gated sodium channel, expressed in peripheral nociceptive neurons, plays a role in transmitting nociceptive signals. The effect of VX-548, an oral, highly selective inhibitor of Na1.

Tranexamic Acid for Intracerebral Hemorrhage in Patients on Non-Vitamin K Antagonist Oral Anticoagulants (TICH-NOAC): A Multicenter, Randomized, Placebo-Controlled, Phase 2 Trial.

Background: Evidence-based hemostatic treatment for intracerebral hemorrhage (ICH) associated with non-vitamin K antagonist oral anticoagulants (NOACs) is lacking. Tranexamic acid (TXA) is an antifibrinolytic drug potentially limiting hematoma expansion. We aimed to assess the efficacy and safety of TXA in NOAC-ICH.

Prevalence and Burden of Illness of Rome IV Chronic Idiopathic Constipation, Opioid-Induced Constipation, and Opioid-Exacerbated Constipation in the United States.

Introduction: Chronic idiopathic constipation (CIC) and opioid-induced constipation (OIC) are disorders that negatively affect quality of life. We sought to assess the prevalence, symptom severity, and medication use among people with Rome IV CIC, OIC, and opioid-exacerbated constipation (OEC) using a nationally representative data set with nearly 89,000 people in the United States.

Methods: From May 3, 2020, to June 24, 2020, we recruited a representative sample of people in the United States ≥ 18 years to complete an online national health survey.

Rutin, Puerarin and Silymarin Regulated Aluminum-Induced Imbalance of Neurotransmitters and Metal Elements in Brain of Rats.

Non-specifically binding of aluminum to various substances in the organism can result in toxicity. The accumulation of large amounts of aluminum can cause an imbalance in metal homeostasis and interfere with the synthesis and release of neurotransmitters. Flavonoids have strong metal chelating activity, which can reduce damage to the central nervous system.