Glycomimetic inhibitors of tandem-repeat galectins: Simple and efficient.

The binding of human galectins by glycomimetic inhibitors is a promising therapeutic approach. The structurally distinct group of tandem-repeat galectins has scarcely been studied so far, and there is hardly any knowledge on their ligand specificity or their inhibitory potential, particularly concerning non-natural carbohydrates. Here, we present the synthesis of a library of seven 3-O-disubstituted thiodigalactoside-derived glycomimetics and their affinity to two tandem-repeat galectins, Gal-8 and Gal-9.

Flavonoids as Aglycones in Retaining Glycosidase-Catalyzed Reactions: Prospects for Green Chemistry.

Flavonoids and their glycosides are abundant in many plant-based foods. The (de)glycosylation of flavonoids by retaining glycoside hydrolases has recently attracted much interest in basic and applied research, including the possibility of altering the glycosylation pattern of flavonoids. Research in this area is driven by significant differences in physicochemical, organoleptic, and bioactive properties between flavonoid aglycones and their glycosylated counterparts.

Computational Study of Complex Formation between Hyaluronan Polymers and Polyarginine Peptides at Various Ratios.

Hyaluronic acid, a naturally occurring carbohydrate biopolymer in human tissues, finds wide application in cosmetics, medicine, and material science. Its anionic properties play a crucial role in its interaction with positively charged macromolecules and ions. Among these macromolecules, positively charged arginine molecules or polyarginine peptides demonstrate potential in drug delivery when complexed with hyaluronan.

Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase.

A new class of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-β-N-acetyl-d-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a view to eventually ameliorating Alzheimer's disease.

Community Solutions to Increase the Healthfulness of Grocery Stores: Perspectives of Immigrant Parents.

Grocery store environments are recognized as one of the most crucial community settings for developing and maintaining healthy nutritional behaviors in children. This is especially true for disadvantaged ethnic minority families, such as immigrants, who reside in the Detroit Metropolitan area and have historically experienced inequities that result in poor health outcomes. Rates of obesity and type II diabetes have affected Detroit 38% more than the rest of the state and nationwide.

Emotion-Driven Eating and Overeating Among Fourth Graders: The Roles of Body Image, Academic Achievement, and Peer and School Factors.

Background: Eating patterns such as breakfast consumption and fruit and vegetable intake have been associated with academic achievement and cognitive function.

Method: The purpose of this study was to learn more about psychological (emotion-driven eating) and behavioral (over-eating) eating patterns and motives, and the roles of body image, academic achievement (reading and math), and social supports (peer acceptance and school attachment), among 378 fourth-grade students (55% boys) from 14 classrooms across 6 schools within a large Midwestern urban area.

Results: Results were analyzed through a 2-group (male and female) path analysis.

Enhanced Measurement of Sugar-Sweetened Beverage Marketing to Young Immigrant Children in Grocery Store Environments.

The marketing of Sugar-Sweetened Beverages (SSBs) within grocers is an obesogenic factor that negatively impacts children's nutritional behavior, specifically for people from racial and ethnic minority groups, such as immigrants. We aimed to develop and employ a methodology that more precisely assesses the availability, price, and promotion of SSBs to young immigrant children within independently owned grocery stores. A case comparison design was used to explore the differences in the grocery store landscape of SSB marketing by conducting an enhanced Nutrition Environment Measures Survey-SSB (NEMS-SSB) within 30 grocery stores in the Hispanic and Latino enclaves in Southwest Detroit, in the Arab and Chaldean enclaves in North-central Detroit, and in Warren, Hamtramck, and Dearborn, in comparison with 48 grocers in Metro Detroit.

Dimerisation of the Yeast K Translocation Protein Trk1 Depends on the K Concentration.

In baker's yeast (), Trk1, a member of the superfamily of K-transporters (SKT), is the main K uptake system under conditions when its concentration in the environment is low. Structurally, Trk1 is made up of four domains, each similar and homologous to a K-channel α subunit. Because most K-channels are proteins containing four channel-building α subunits, Trk1 could be functional as a monomer.

Mutation Hotspot for Changing the Substrate Specificity of β--Acetylhexosaminidase: A Library of GlcNAcases.

β--Acetylhexosaminidase from (Hex; EC 3.2.1.

Modulation of global stability, ligand binding and catalytic properties of trypsin by anions.

Specific salts effect is well-known on stability and solubility of proteins, however, relatively limited knowledge is known regarding the effect on catalytic properties of enzymes. Here, we examined the effect of four sodium anions on thermal stability and catalytic properties of trypsin and binding of the fluorescent probe, p-aminobenzamidine (PAB), to the enzyme. We show that the specific anions effect on trypsin properties agrees with the localization of the anions in the Hofmeister series.

Diaminocyclopentane-derived -GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer's disease.

We developed potent and selective aminocyclopentane-derived inhibitors of human -acetyl-β-D-glucosaminidase (OGA) implicated in Alzheimer's disease. For example compound 13 was a nanomolar OGA inhibitor with 92 000-fold selectivity over human HexB. It was non-toxic and increased protein -GlcNAcylation in the culture of murine neural cells, showing new alternatives in the treatment of tauopathies.

The Association Between Home or Community Garden Access and Adolescent Health.

Little is known about the influence of home or community garden (HCG) access on adolescent health. The objective of this study was to determine the association between adolescent self-rated health, nutrition knowledge, attitudes, and intake with HCG access. Urban high school students (n = 401) completed a questionnaire prior to a nutrition education intervention.

Assessing the Influence of Food Insecurity and Retail Environments as a Proxy for Structural Racism on the COVID-19 Pandemic in an Urban Setting.

A collaborative partnership launched the Great Grocer Project (GGP) in March 2021 in Detroit, Michigan where health inequities, including deaths due to COVID-19, have historically been politically determined and informed by socially entrenched norms. Institutional and structural racism has contributed to a lack of diversity in store ownership among Detroit grocers and limited access to high-quality, affordable healthy foods as well as disparate food insecurity among Detroit residents. The GGP seeks to promote Detroit's healthy grocers to improve community health and economic vitality through research, programs, and policies that have the potential to advance health equity.

Discovery of human hexosaminidase inhibitors by in situ screening of a library of mono- and divalent pyrrolidine iminosugars.

Two libraries of mono- and dimeric pyrrolidine iminosugars were synthesized by CuAAC and (thio)urea-bond-forming reactions from the respective azido/aminohexylpyrrolidine iminosugar precursors. The resulting monomeric and dimeric compounds were screened for inhibition of β-N-acetylglucosaminidase from Jack beans, the plant ortholog of human lysosomal hexosaminidases. A selection of the best inhibitors of these libraries was then evaluated against human lysosomal β-N-acetylhexosaminidase B (hHexB) and human nucleocytoplasmic β-N-acetylglucosaminidase (hOGA).

Self-Assembling Metallocomplexes of the Amphiphilic 1,4-Diazabicyclo[2.2.2]octane Derivative as a Platform for the Development of Nonplatinum Anticancer Drugs.

New 1-cetyl-4-aza-1-azoniabicyclo[2.2.2]octane bromide complexes with copper(II) bromide and lanthanum(III) nitrate were characterized using dynamic light scattering and transmission electron microscopy, with self-assembly and the morphological behavior elucidated.

Interactions between a dsDNA Oligonucleotide and Imidazolium Chloride Ionic Liquids: Effect of Alkyl Chain Length, Part I.

Ionic liquids (ILs) have become nearly ubiquitous solvents and their interactions with biomolecules has been a focus of study. Here, we used the fluorescence emission of DAPI, a groove binding fluorophore, coupled with molecular dynamics (MD) simulations to report on interactions between imidazolium chloride ([Im]) ionic liquids and a synthetic DNA oligonucleotide composed entirely of T/A bases (7(TA)) to elucidate the effects ILs on a model DNA duplex. Spectral shifts on the order of 500-1000 cm, spectral broadening (~1000 cm), and excitation and emission intensity ratio changes combine to give evidence of an increased DAPI environment heterogeneity on added IL.

Sterically Hindered Quaternary Phosphonium Salts (QPSs): Antimicrobial Activity and Hemolytic and Cytotoxic Properties.

Structure-activity relationships are important for the design of biocides and sanitizers. During the spread of resistant strains of pathogenic microbes, insights into the correlation between structure and activity become especially significant. The most commonly used biocides are nitrogen-containing compounds; the phosphorus-containing ones have been studied to a lesser extent.

Isatin-3-acylhydrazones with Enhanced Lipophilicity: Synthesis, Antimicrobial Activity Evaluation and the Influence on Hemostasis System.

Water-soluble trialkylammonium isatin-3-hydrazone derivatives bearing phenolic substituent were easily synthesized with high yields. XRD studies confirmed the presence of these compounds as trans-(Z)-isomers in a crystal. It was shown that an increase in the lipophilicity of the cationic center leads to an increase in activity against Gram-positive bacteria Staphylococcus aureus and Bacillus cereus, including methicillin-resistant Staphylococcus aureus (MRSA) strains.

Nutrition Supports Deconstructed and Disrupted: An Evaluation of a Multilevel School-Based Intervention during the Time of COVID.

The Best Food Forward (BFF) project aims to provide multiple nutrition supports and interventions to improve family food security (FS) and health outcomes associated with FS within two metropolitan school districts. A quasi-experimental time-series design guided a multilevel evaluation for BFF through surveys, biometric screenings, focus groups, and observations among a random sample of caregiver-child dyads. FS, utilization of school meal programs, and nutrition behaviors were observed and analyzed at three time points: preintervention, postintervention pre-COVID-19, and postintervention post-COVID-19.