Synthesis,Conformational and Configurational Studies of Some New Acetylated Glycosides of 2-Thio-3-aryl-4(3H)-quinazolinones,Their Thiono and 3,1-Benzothiazin-2,4-dithione

Abstract

A series of some new acetylated S-glycosides of 2-thioxoquinazolin-4-ones, their thiono analogues and 3,1-benzothazin-2,4-dithione derivatives, including a D-glucose and a D-galactose derivatives and a D-xylose, and an L-arabinose derivatives have been synthesized. The conformation and configuration of these carbohydrate derivatives were determined by analysing their ¹H and ¹³C NMR chemical shifts and coupling constants. The biological activity of these compounds has been studied.     

A9C sensitive Cl? - accumulation in A. thaliana root cells during salt stress is controlled by internal and external calcium

The involvement of chloride in salt stress symptoms and salt tolerance mechanisms in plants has been less investigated in the past. Therefore, we studied the salt-induced chloride influx in Arabidopsis expressing the GFP-based anion indicator Clomeleon. High salt concentrations induce two phases of chloride influx. The fast kinetic phase is likely caused by membrane depolarization, and is assumed to be mediated by channels. This is followed by a slower "saturation" phase, where chloride is accumulated in the cytoplasm. Both phases of chloride uptake are dependent on the presence of external calcium. In general: with high [Ca²⁺] less chloride is accumulated in the cytoplasm. Surprisingly, also the internal calcium availability has an impact on chloride transport. A complete block of the second phase of chloride influx is achieved by the anion channel blocker A9C and trivalent cations (La³⁺, Gd³⁺, and Al³⁺). Other channel blockers and diuretics were found to inhibit the process partially. The results suggest that several transporter species are involved here, including electroneutral cation-chloride-cotransporters, and a part of chloride possibly enters the cells through cation channels after salt application.     

Associations between Active Travel to Work and Overweight,Hypertension, and Diabetes in India: A Cross-Sectional Study

Background

Increasing active travel (walking, bicycling, and public transport) is promoted as a key strategy to increase physical activity and reduce the growing burden of noncommunicable diseases (NCDs) globally. Little is known about patterns of active travel or associated cardiovascular health benefits in low- and middle-income countries. This study examines mode and duration of travel to work in rural and urban India and associations between active travel and overweight, hypertension, and diabetes.

Methods and Findings

Cross-sectional study of 3,902 participants (1,366 rural, 2,536 urban) in the Indian Migration Study. Associations between mode and duration of active travel and cardiovascular risk factors were assessed using random-effect logistic regression models adjusting for age, sex, caste, standard of living, occupation, factory location, leisure time physical activity, daily fat intake, smoking status, and alcohol use. Rural dwellers were significantly more likely to bicycle (68.3% versus 15.9%; p<0.001) to work than urban dwellers. The prevalence of overweight or obesity was 50.0%, 37.6%, 24.2%, 24.9%; hypertension was 17.7%, 11.8%, 6.5%, 9.8%; and diabetes was 10.8%, 7.4%, 3.8%, 7.3% in participants who travelled to work by private transport, public transport, bicycling, and walking, respectively. In the adjusted analysis, those walking (adjusted risk ratio [ARR] 0.72; 95% CI 0.58–0.88) or bicycling to work (ARR 0.66; 95% CI 0.55–0.77) were significantly less likely to be overweight or obese than those travelling by private transport. Those bicycling to work were significantly less likely to have hypertension (ARR 0.51; 95% CI 0.36–0.71) or diabetes (ARR 0.65; 95% CI 0.44–0.95). There was evidence of a dose-response relationship between duration of bicycling to work and being overweight, having hypertension or diabetes. The main limitation of the study is the cross-sectional design, which limits causal inference for the associations found.

Conclusions

Walking and bicycling to work was associated with reduced cardiovascular risk in the Indian population. Efforts to increase active travel in urban areas and halt declines in rural areas should be integral to strategies to maintain healthy weight and prevent NCDs in India. Please see later in the article for the Editors'' Summary     

Impact of Dietary Organic Mineral Supplementation on Reproductive Performance,Egg Quality Characteristics,Lipid Oxidation,Ovarian Follicular Development,and Immune Response in Laying Hens Under High Ambient Temperature

Biological Trace Element Research - The objectives of this study were to investigate the impact of dietary organic mineral mixture (manganese, zinc, and copper) supplementation on reproductive...     

Expression of novel lhmlt fusion protein using plant viral vector and study of its anticancer effect

Plant Cell, Tissue and Organ Culture (PCTOC) - Melittin peptide is the main component of honey bee venom with the cytotoxic and anti-cancer effect which can affect healthy and cancerous cells...     

Chlorogenic acid prevents hepatotoxicity in arsenic-treated mice: role of oxidative stress and apoptosis

Molecular Biology Reports - Arsenic is a potent and toxic heavy metal found in the environment that causes health problems, including liver disease, in humans and animals. Chlorogenic acid (CA) is...     

The commercially important shoemaker spinefoot,Siganus sutor,connects coral reefs to neighbouring seagrass meadows

Spatial management of fish populations can potentially be optimized by determining the area of influence of a particular species. We performed an acoustic tagging study implemented on Denis Island in the Seychelles to assess the area of influence of the heavily targeted shoemaker spinefoot, Siganus sutor. We investigated whether this species acts as a mobile link between coral patches and seagrass meadows, and whether their movements differed between day and night. The study incorporated an array of 22 acoustic stations deployed within dense coral patches, seagrass meadows and mixed habitats of both seagrass and coral. Fifteen S. sutor carrying internal acoustic tags were monitored from November 2016 until May 2017. Detection patterns revealed them to be diurnal herbivores, with only rare nocturnal movements. Home-range estimates showed that individuals differed in their spatial range extents and habitats used, covering ~15% of the total shallow subtidal coastline of the island. However, they displayed very small daily movements (<200 m), concentrated mainly around sites within mixed coral and seagrass habitats. An optimal number of detections was recorded when the coral to seagrass area ratio was approximately 1.6:1. This ratio was confirmed through statistical prediction modelling. Identification of such links of commercially important species between networked habitats may help authorities consider incorporating seagrass meadows of the Seychelles into management discussions, which are currently lacking.     

O-Heterocyclic Embeurekols from Embellisia eureka,an Endophyte of Cladanthus arabicus

Three new polyketides (-)-1 , (+)-1 , and 2 ) were isolated from the EtOAc extract of the fungus Embellisia eureka, an endophyte of the Moroccan plant Cladanthus arabicus (Asteraceae). The structures of these new compounds were determined on the basis of one- and two-dimensional NMR spectroscopy as well as by high-resolution mass spectrometry. The absolute configurations of (-)-1 , (+)-1 , and 2 were determined by TDDFT ECD calculations of solution conformers, online HPLC-ECD analysis, and the modified Mosher method. Chirality 25:250–256, 2013. © 2013 Wiley Periodicals, Inc.     

Molecular and morphological characterization of Pristionchus pacificus (Nematoda: Rhabditida: Neodiplogastridae), a new record of an entomophilic nematode from Iran

During a survey of entomopathogenic nematodes from the Mashhad region, in northeastern Iran, an entomophilic nematode was isolated using the Galleria trap method. Morphological characterization showed that this isolate belongs to the family Neodiplogastridae. Detailed morphological and morphometric characterization including SEM data fit with Pristionchus pacificus Sommer, Carta, Kim et Sternberg, 1996, representing the first record of this genus and species from Iran. Iranian specimens of P. pacificus FUM 5 are characterized by the body length (0.69–0.83 mm), the stoma (6–10 μm) bearing a dorsal tooth and a conical elongated tail (146–220 μm). Molecular analyses using 18S and ITS rDNA genes further support this identification. Measurements, illustrations, and SEM photographs of the Iranian isolate are provided and the phylogenetic position of the species is discussed.     

Development of an in vivo active,dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere

Recent preclinical studies demonstrate a role for the prostaglandin E₂ (PGE₂) subtype 1 (EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and diabetes mellitus. A series of amide and N-acylsulfonamide analogs of a previously described picolinic acid-based human EP1 receptor antagonist (7) were prepared. Each analog had improved selectivity at the mouse EP1 receptor over the mouse thromboxane receptor (TP). A subset of analogs gained affinity for the mouse PGE₂ subtype 3 (EP3) receptor, another potential therapeutic target. One analog (17) possessed equal selectivity for EP1 and EP3, displayed a sufficient in vivo residence time in mice, and lacked the potential for acyl glucuronide formation common to compound 7. Treatment of mice with 17 significantly attenuated the vasopressor activity resulting from an acute infusion of EP1 and EP3 receptor agonists. Compound 17 represents a potentially novel therapeutic in the treatment of hypertension and diabetes mellitus.