Food Insecurity across Age Groups in the United States during the COVID-19 Pandemic.

Food insecurity increased during the COVID-19 pandemic, but the impact varied across different age groups during the prolonged public health emergency. This study sought to describe national food insecurity prevalence by adult age group at multiple stages of the pandemic and explore differences by demographic characteristics. Data were from the nationally representative US Census Bureau's Household Pulse Survey from April 2020 to May 2023 (N = 4,153,462).

-Disubstituted 4-Sulfamoylbenzoic Acid Derivatives as Inhibitors of Cytosolic Phospholipase A: Synthesis, Aqueous Solubility, and Activity in a Vesicle and a Whole Blood Assay.

Background: Cytosolic phospholipase A2α (cPLA) is the key enzyme that initiates the arachidonic acid cascade through which pro-inflammatory lipid mediators can be formed. Therefore, cPLA is considered an interesting target for the development of anti-inflammatory drugs. Although several effective inhibitors of the enzyme have been developed, none of them has yet reached clinical application.

1-Benzylindoles as inhibitors of cytosolic phospholipase Aα: synthesis, biological activity, aqueous solubility, and cell permeability.

Cytosolic phospholipase Aα (cPLAα) is considered an interesting target for the development of new anti-inflammatory drugs, as it is significantly involved in the formation of pro-inflammatory lipid mediators. Recently, in a ligand-based virtual screening approach, 2,4-dichlorobenzyl-substituted 4-[2-(indol-3-ylmethylene)hydrazineyl]benzoic acid 7 was found to be an inhibitor of cPLAα with micromolar activity. This compound has now been systematically varied to increase inhibitory potency.

ω-(5-Phenyl-2H-tetrazol-2-yl)alkyl-substituted glycine amides and related compounds as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1).

Vascular adhesion protein-1 (VAP-1), also known as plasma amine oxidase or semicarbazide-sensitive amine oxidase, is an enzyme that degrades primary amines to aldehydes with the formation of hydrogen peroxide and ammonia. Among others, it plays a role in inflammatory processes as it can mediate the migration of leukocytes from the blood to the inflamed tissue. We prepared a series of ω-(5-phenyl-2H-tetrazol-2-yl)alkyl-substituted glycine amides and related compounds and tested them for inhibition of purified bovine plasma VAP-1.

Measurement of Ambulatory Medication Errors in Children: A Scoping Review.

Background And Objectives: Children use most medications in the ambulatory setting where errors are infrequently intercepted. There is currently no established measure set for ambulatory pediatric medication errors. We have sought to identify the range of existing measures of ambulatory pediatric medication errors, describe the data sources for error measurement, and describe their reliability.

Synthesis, activity and metabolic stability of propan-2-one substituted tetrazolylalkanoic acids as dual inhibitors of cytosolic phospholipase Aα and fatty acid amide hydrolase.

The serine hydrolases cytosolic phospholipase Aα (cPLAα) and fatty acid amide hydrolase (FAAH) are interesting targets for the development of new anti-inflammatory and analgesic drugs. Structural modifications of a potent dual inhibitor with a propan-2-one substituted tetrazolylpropionic acid moiety led to compounds with also nanomolar activity against both enzymes but better physicochemical properties. The structure-activity relationships showed that the variations had partially divergent effects on the inhibitory activity of the compounds towards cPLAα and FAAH reflecting differences in the binding mode to the enzymes.

Synthesis, activity, metabolic stability and cell permeability of new cytosolic phospholipase Aα inhibitors with 1-indolyl-3-phenoxypropan-2-one structure.

Cytosolic phospholipase Aα (cPLAα), the key enzyme of the arachidonic acid cascade, is considered to be an interesting target for the development of new anti-inflammatory drugs. Potent inhibitors of the enzyme include indole-5-carboxylic acids with propan-2-one residues in position 1 of the indole. Previously, it was found that central pharmacophoric elements of these compounds are their ketone and carboxylic acid groups, which unfortunately are subject to pronounced metabolism by carbonyl reductases and glucuronosyltransferases, respectively.

HPLC fluorescence assay for measuring the activity of NAPE-PLD and the action of inhibitors affecting this enzyme.

N-Acyl phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD) is the major enzyme for the biosynthesis of the endocannabinoid anandamide. The role of NAPE-PLD in various physiological and pathophysiological conditions is currently under investigation. For example, the enzyme might be involved in the control of neuronal activity, embryonic development and pregnancy, and prostate cancer.

Metabolism of sumatriptan revisited.

Scientific literature describes that sumatriptan is metabolized by oxidative deamination of its dimethylaminoethyl residue by monoamine oxidase A (MAO A) and not by cytochrome P450 (CYP)-mediated demethylation, as is usual for such structural elements. Using recombinant human enzymes and HPLC-MS analysis, we found that CYP enzymes may also be involved in the metabolism of sumatriptan. The CYP1A2, CYP2C19, and CYP2D6 isoforms converted this drug into N-desmethyl sumatriptan, which was further demethylated to N,N-didesmethyl sumatriptan by CYP1A2 and CYP2D6.

Synthesis and pharmacokinetic properties of novel cPLAα inhibitors with 1-(carboxyalkylpyrrolyl)-3-aryloxypropan-2-one structure.

Indole-5-carboxylic acids with 3-aryloxy-2‑oxopropyl residues in position 1 have been shown to be potent inhibitors of cytosolic phospholipase Aα (cPLAα), an enzyme involved in the formation of pro-inflammatory lipid mediators. Unfortunately, in animal experiments, only very low plasma concentrations could be achieved after peroral administration of this type of compound. Since insufficient metabolic stability was suspected as the cause, structural modifications were made to optimize this property.

Light-Controlled Destruction and Assembly: Switching between Two Differently Composed Cage-Type Complexes.

We report on two regioisomeric, diazocine ligands 1 and 2 that can both be photoswitched between the E- and Z-configurations with violet and green light. The self-assembly of the four species (1-Z, 1-E, 2-Z, 2-E) with Co ions was investigated upon changing the coordination vectors as a function of the ligand configuration (E vs Z) and regioisomer (1 vs 2). With 1-Z, Co (1-Z) was self-assembled, while a mixture of ill-defined species (oligomers) was observed with 2-Z.

HPLC fluorescence assay for measuring the activity of diacylglycerol lipases and the action of inhibitors thereof.

1,2-Diacylglycerol lipases (DAGLs) are the most important enzymes for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol (2-AG), and their role in various pathophysiological conditions is currently under investigation. We synthesized a new 1,2-diacylglycerol substrate for these enzymes with a fluorogenic 4-(pyren-1-yl)butanoyl residue in sn-2 position. Using the fluorescent substrate, we measured DAGL activity in rat liver S9 fraction and brain microsomes.

ω-(5-Phenyl-2H-tetrazol-2-yl)alkyl-substituted hydrazides and related compounds as inhibitors of amine oxidase copper containing 3 (AOC3).

Amine oxidase copper containing 3 (AOC3), also known as plasma amine oxidase, semicarbazide-sensitive amine oxidase, or vascular adhesion protein-1, catalyzes the oxidative deamination of primary amines to aldehydes using copper and a quinone as cofactors. Because it is involved in the transmigration of inflammatory cells through blood vessels into tissues, AOC3 is thought to play an important role in inflammatory diseases. Therefore, inhibitors of this enzyme could lead to new therapeutics for the treatment of inflammation-related diseases.

M-CPOnes: transition metal complexes with cyclopropenone-based ligands for light-triggered carbon monoxide release.

A new class of CO-releasing molecules, M-CPOnes, was prepared combining cyclopropenone-based ligands for CO release with the modular scaffold of transition metal complexes. In proof-of-concept studies, M-CPOnes based on Zn, Fe and Co are stable in the dark but undergo light-triggered CO release with the cyclopropenone substituents and metal ions enabling tuning of the photophysical properties. Furthermore, the choice of metal allows the use of different spectroscopic methods to monitor photodecarbonylation from fluorescence spectroscopy to UV/vis spectroscopy and paramagnetic NMR spectroscopy.

Contribution of cyclooxygenase-1-dependent prostacyclin synthesis to bradykinin-induced dermal extravasation.

Background: Non-allergic angioedema is a potentially life-threatening condition caused by accumulation of bradykinin and subsequent activation of bradykinin type 2 receptors (B2). Since COX activity plays a pivotal role in B2 signaling, the aim of this study was to determine which prostaglandins are the key mediators and which COX, COX-1 or COX-2, is predominantly involved.

Methods: We used Miles assays to assess the effects of inhibitors of COX, 5-lipoxygenase, epoxyeicosatrienoic acid generation, cytosolic phospholipase Aα and a variety of prostaglandin receptor antagonists on bradykinin-induced dermal extravasation in C57BL/6 and COX-1-deficient mice (COX-1).

Comparison of manual therapy techniques on ankle dorsiflexion range of motion and dynamic single leg balance in collegiate athletes.

Introduction/purpose: Literature consistently identifies two key examination components when managing ankle/foot pathologies: 1) dorsiflexion range of motion (DFROM) and 2) single limb balance. Mobilizations with movement (MWM) and Instrument-Assisted Soft Tissue (IASTM) are two emerging manual therapy (MT) options in the management of ankle/foot conditions.

Methodology/sample: In this observational cohort study, 147 subjects were randomized in a block fashion as follows: 1) Control, 2) IASTM, 3) MWM, and 4) Combination of both MT interventions.

Hexafluoroisopropyl Carbamates as Selective MAGL and Dual MAGL/FAAH Inhibitors: Biochemical and Physicochemical Properties.

A series of hexafluoroisopropyl carbamates with indolylalkyl- and azaindolylalkyl-substituents at the carbamate nitrogen was synthesized and evaluated for inhibition of the endocannabinoid degrading enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). The synthesized derivatives with butyl to heptyl spacers between the heteroaryl and the carbamate moiety were inhibitors of both enzymes. For investigated compounds in which the alkyl chain was partially incorporated into a piperidine ring, different results were obtained.

Closed chain dorsiflexion and the regional interdependence implications on fundamental movement patterns in collegiate athletes.

Purpose: An association between limited ankle closed kinetic chain dorsiflexion range of motion (CKCDFROM) and movement dysfunction in the lower quarter is often implied, limited research exists linking CKCDFROM and gross movement patterns, such as the squatting. The purpose of this study is to investigate the association between CKCDFROM and movement patterns in collegiate athletes, as measured by the functional movement screen (FMS).

Materials And Methods: A quasi-experimental observational analytical cohort study with 147 athletes from five Division III collegiate men's and women's athletic teams were included in the study.

Aryl -[ω-(6-Fluoroindol-1-yl)alkyl]carbamates as Inhibitors of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and Butyrylcholinesterase: Structure-Activity Relationships and Hydrolytic Stability.

A series of aryl -[ω-(6-fluoroindol-1-yl)alkyl]carbamates with alkyl spacers of varying lengths between the indole and the carbamate group and with differently substituted aryl moieties at the carbamate oxygen were synthesized and tested for inhibition of the pharmacologically interesting serine hydrolases fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), butyrylcholinesterase (BuChE), and acetylcholinesterase (AChE). Furthermore, the chemical stability in an aqueous solution and the metabolic stability toward esterases in porcine liver homogenate and porcine blood plasma were determined. While most of the synthesized derivatives were potent inhibitors of FAAH, a considerable inhibition of MAGL and BuChE was elicited only by compounds with a high carbamate reactivity, as evidenced by a significant hydrolysis of these compounds in an aqueous solution.

Movement patterns and neuromusculoskeletal impairments observed in a female Olympic Field Hockey team: An observational cohort study.

Purpose: The purpose of the cross-sectional observational cohort study was to quantify movement patterns and neuromuscular impairments in Olympic Female Field Hockey utilizing a standardized movement-centered assessment model.

Methodology/sample: A sample of convenience was obtained from the active roster of the 2016 USA Women's Olympic Field Hockey team. Inclusion and exclusion criteria were applied and resulted in nine participants.

Evaluation of inhibitors of the arachidonic acid cascade with intact platelets using an on-line dilution and on-line solid phase extraction HPLC-MS method.

An automatic on-line dilution/on-line solid phase extraction (SPE) system has been developed for the detection of metabolites of the arachidonic acid cascade in platelets. The method allows the direct injection of larger quantities of centrifugates from cell suspensions previously treated with an equal volume of an acetonitrile/methanol mixture for protein precipitation. The method was used to study the effect of inhibitors of platelet arachidonic acid cascade enzymes (cytosolic phospholipase Aα, cyclooxygenase-1, thromboxane synthase, 12-lipoxygenase) and related targets (cyclooxygenase-2, microsomal prostaglandin E synthase-1, 5-lipoxygenase) in intact platelets after stimulation with calcium ionophore A23187.

Leveraging Antiprogestins in the Treatment of Metastatic Breast Cancer.

Although incurable, the prognosis for patients with metastatic breast cancer (MBC) has considerably improved with the approvals of multiple targeted and cytotoxic therapies. For hormone receptor-positive (HR+), ie, estrogen receptor and progesterone receptor positive (ER+/PgR+) and human epidermal growth factor receptor-2 negative (ie, ERBB2 gene nonamplified or HER2-) MBC, current approved treatment options include palliative endocrine therapy (ET), cyclin-dependent kinase (CDK 4/6) inhibitors, mTOR inhibitors, and PI3 kinase inhibitors. Most treatments target ER+ disease regardless of PgR status.

A Paramagnetic NMR Spectroscopy Toolbox for the Characterisation of Paramagnetic/Spin-Crossover Coordination Complexes and Metal-Organic Cages.

The large paramagnetic shifts and short relaxation times resulting from the presence of a paramagnetic centre complicate NMR data acquisition and interpretation in solution. As a result, NMR analysis of paramagnetic complexes is limited in comparison to diamagnetic compounds and often relies on theoretical models. We report a toolbox of 1D (H, proton-coupled C, selective H-decoupling C, steady-state NOE) and 2D (COSY, NOESY, HMQC) paramagnetic NMR methods that enables unprecedented structural characterisation and in some cases, provides more structural information than would be observable for a diamagnetic analogue.

The Impact of Increasing Sun Protection Counseling and Skin Cancer Screening.

Background: Skin cancer is the most common cancer in the United States. Skin cancer is a broad term that includes squamous cell carcinoma, basal cell carcinoma, and melanoma. Melanoma is the most concerning of the three types of skin cancer and is the focus of this project.

Acylated 1-1,2,4-Triazol-5-amines Targeting Human Coagulation Factor XIIa and Thrombin: Conventional and Microscale Synthesis, Anticoagulant Properties, and Mechanism of Action.

We herein report the conventional and microscale parallel synthesis of selective inhibitors of human blood coagulation factor XIIa and thrombin exhibiting a 1,2,4-triazol-5-amine scaffold. Structural variations of this scaffold allowed identifying derivative , a potent 29 nM inhibitor of FXIIa, with improved selectivity over other tested serine proteases and also finding compound with 27 nM inhibitory activity toward thrombin. For the first time, acylated 1,2,4-triazol-5-amines were proved to have anticoagulant properties and the ability to affect thrombin- and cancer-cell-induced platelet aggregation.