Objective and subjective measures of the neighbourhood environment: Associations with frailty levels

ObjectivesThe aim of this study was to investigate whether perceptions of the neighbourhood environment (NE) and objective measures of the NE were associated with frailty in older adults.MethodsA cross-sectional study in Adelaide, Australia, recruited a sample of 115 community-dwelling adults aged ≥60 years. Respondents’ perceptions of their NEs were assessed using the Neighbourhood Environment Walkability Scale (NEWS). An objective assessment of these NEWS survey questions was conducted using seven variables: residential density, land use mix diversity, street connectivity, accessibility, seasonal persistent green cover, road crash density and crime rate. Frailty was evaluated using the FRAIL (fatigue, resistance, ambulation, illnesses and loss of weight) scale. Multivariable linear regression analyses were employed to assess the associations between NEWS and frailty, and to assess the associations between objective neighbourhood variables and frailty.ResultsFrail and pre-frail older adults were more likely to live in areas with lower residential density, lower density of road crashes, and higher accessibility than robust participants. Additionally, a poorer perception of the overall environment, worse land-use mix and accessibility and worse crime safety were associated with frailty and pre-frailty after adjustment of covariates and objective GIS variables.DiscussionNeighbourhood characteristics, both objective and perceived, are associated with frailty levels in older adults, and that strategies to tackle frailty must consider the impact of the neighbourhood environment.     

Men with impaired glucose tolerance have lower self-rated health than men with impaired fasting glucose

AimPrevious studies have shown that individuals with impaired glucose tolerance (IGT) have lower self-rated health than normoglycaemic individuals. The aim of this study was to examine differences in self-rated health between individuals with IGT and those with impaired fasting glucose (IFG) and to consider the potentially mediating effect of physical activity.MethodsIn 2002–2005, a total of 2816 individuals were randomly selected for a population-based study in Sweden. All participants performed an oral glucose tolerance test (OGTT). Fasting venous blood samples were drawn, and questionnaires concerning lifestyles were completed. Self-rated health (SRH) and leisure time physical activity (LTPA) were reported on a five-graded and four-graded scale, respectively. A total of 213 individuals with IGT and 129 with IFG were detected.ResultsIGT, but not IFG, was associated with low self-rated health. The difference in self-rated health was seen particularly in men when adjusted for age and BMI (OR = 2.13, CI: 1.13–4.02, p = 0.020). The results became insignificant when including physical activity in the model (OR = 1.8, CI: 0.91–3.58, p = 0.094).ConclusionThe low self-rated health adds further weight to the risk profile in men with IGT and stresses the importance of early detection and lifestyle interventions.     

Bioactive A-ring rearranged limonoids from the root barks of Walsura robusta

Screening active natural products, rapid identification, and accurate isolation are of great important for modern natural lead compounds discovery¹. We hereby reported the isolation of seven new neotecleanin-type limonoids (17), seven new limonoids with 5-oxatricyclo[5.4.0.11., 4.]hendecane ring system (814), and two new precursors (1516) together with four known limonoids (1720) from the root barks of Walsura robusta. Their structures, including their absolute configurations, were elucidated based on analyses of HR-ESI-MS, 1D/2D NMR, ECD spectrum calculations and single-crystal X-ray diffraction techniques. Compounds 2, 8, 9, 11, 13, 14, 18 showed significant anti-inflammatory activities in LPS-induced RAW 264.7 cell line, BV2 microglial cells, and Propionibacterium acnes-stimulated THP-1 human monocytic cells. Walrobsin M (11) exhibited anti-inflammatory activity with IC₅₀ value of 7.96±0.36 μmol/L, and down-regulated phosphorylation levels of ERK and p38 in a dose-dependent manner.     

Design,synthesis, and evaluation of a series of novel phenylpropanoic acid derivatives agonists for the FFA1

Free fatty acid 1 (FFA1/GPR40) has attracted extensive attention as a novel target for the treatment of type 2 diabetes for its role in the enhancement of insulin secretion with glucose dependency. Aiming to develop novel potent FFA1 agonists, a new series of phenylpropionic acid derivatives were designed and synthesized on the basis of the modification of chemical cement of TAK‐875, AMG‐837, and LY2881835. Among them, most promising compounds 7 , 14 , and 15 were obtained with EC₅₀ values of 82, 79, and 88 nM, exhibiting a powerful agonistic activity compared to TAK‐875 (95.1 nM). During Oral glucose tolerance test in normal mice, compound 7 , 14 , and 15 had significant glucose‐lowering effect at the dose of 50 mg/kg. Furthermore, compound 15 (50 mg/kg) also significantly improved in glucose tolerance in type 2 diabetic mice. Herein, we reported the discovery and optimization of a series of potent FFA1 agonists. The discovery supported further exploration surrounding this scaffold.     

Synthesis and Biological Activities of Some Benzimidazolone Derivatives

The reaction of 5-nitrobenzimidazolone with phenoxyethyl bromide in presence of potassium carbonate in dimethyl formamide obtained 6-nitro-1,3-bis(2-phenoxyethyl)-1,3-dihydro-2H-benzimidazol-2-one. It was reduced using stannous chloride to get 6-amino -1,3-bis(2-phenoxyethyl)-1, 3-dihydro-2H-benzimidazol -2-one, which was further treated with aromatic sulphonyl chloride to obtain benzimidazolone derivatives, 6a-k. These compounds were tested for antibacterial, antituberculosis and antifungal activity. Most of them have shown very good activity against some gram positive and gram negative microorganisms and fungal strains. Some of them have shown moderate activity against Mycobacterium tuberculosis.