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Synthesis, Aromatase Inhibition, Cytotoxicity and Molecular Docking Studies of New Fluorinated and Non-Fluorinated Thiourea Derivatives of Desloratadine
Get PDFAromatase inhibitors are among the most effective treatment of the breast cancer. Aromatase catalyzes estrogen biosynthesis, which is a long-term cause of breast cancer. Current study describes the synthesis, purification of 26 new fluorinated and non-fluorinated thiourea derivatives of desloratadine (5), and their aromatase inhibition activity, cytotoxicity against cancer cell line (MDA-MB-231). Compounds 7 v and 7 l exhibited a significant anti-aromatase activity, while compounds 7 a, 7 g–h, 7 m and 7 u were also significant active against MDA-MB-231 cell line. Furthermore, the molecular docking studies revealed that active compounds form key interactions with the crucial amino acid of aromatase active site including TRP224, LEU477, CYS437, ALA438, MET374, ARG115, ILE305, and PHE221, which are responsible for the binding interactions of aromatase. All analogues were new, except 7 b and 7 k and also lacked cytotoxicity against BJ human fibroblasts, with the exception of 5 and 7 x. This selectivity makes this series particularly interesting for further studies.</p
Genetic Mapping of the Powdery Mildew Resistance Gene Pm13 on Oat (Avena sativa) Chromosome 1D
Get PDFPowdery mildew, caused by the biotrophic fungus Blumeria graminis DC. f. sp. avenae, is a widespread disease of oats, especially in the temperate regions of Western and Central Europe, and the use of resistant varieties is the most sustainable way to ensure stable yields. Therefore, the identification of robust and effective resistance to powdery mildew is of great interest for oat breedinpg. In contrast to race-specific resistance genes, adult plant resistance (APR) is generally considered to be more durable. The oat variety ‘Firth’, as well as related varieties such as ‘Husky’ or ‘Flämingstip’, contains an unknown APR gene, which was previously located on chromosome 1D using DArT markers. The aim of this study was to confirm and refine the chromosomal location of this resistance gene, tentatively named Pm13. To this end, two independent experiments were carried out using different genetic material under natural infection conditions in the field: genome-wide association mapping (GWAS) in a diverse set of 250 oat lines grown in 10 environments and QTL mapping in a HuskyxAVE1284 biparental population grown in three environments. Both approaches identified a QTL for powdery mildew resistance on the distal end of chromosome 1D in the hexaploid Sang oat genome. The locus explained up to 15% of the phenotypic variance in GWAS and 64% of the phenotypic variance in QTL mapping. Comparison of field data with results from laboratory leaf segment tests confirmed that Pm13 does indeed confer APR. The sequence information of the identified linked markers may allow the development of molecular markers useful for early selection of oat lines with high levels of APR.</p
Insect visual perception and pest control:Opportunities and challenges
Get PDFHumans and insects inhabit very different perceptual worlds, so human experimenters need to be aware of their perceptual biases when investigating insect behaviour. In applied entomology, human perceptual biases have been a barrier to the rational design, manufacture, and improvement of pest control devices that effectively exploit insect visual behaviour. This review describes how the influence of human perceptual bias on this area of applied entomology is being reduced by our expanding understanding of insect visual perception and use of visual modelling methods and highlights several important challenges that are yet to be overcome. [Abstract copyright: Copyright © 2025 The Author(s). Published by Elsevier Inc. All rights reserved.
Planning, transport, and healthy ageing in Asia
Get PDFHigh-density built environments in Asian cities and regions such as Hong Kong and Tokyo have significantly influenced the travel behaviours and health outcomes of older adults. Rapid urban development has led to substantial changes in transport systems, often making travel behaviour complex and, at times, overwhelming for older populations. The rapid growth of ageing populations in these cities presents major public health challenges that demand in-depth research and evidence-based solutions. This special issue brings together studies that explore how transport and urban planning and design in Asian cities can promote healthy ageing. These studies aim to enhance scientific understanding of the health impacts of transport infrastructure in the region. We discussed planning and design contexts, the provision and modification of transport infrastructure, public transport usage behaviours, and their broader implications for health outcomes and well-being among older adults. This paper addresses the unique opportunities and challenges, including large-scale transport infrastructure interventions, health impact assessments, causal inference, and planning and policy recommendations, to support sustainable urban development and improve transport planning for the health and well-being of ageing populations in Asia and beyond.</p
Understanding the Impact of COPD and Self-Management Interventions:A Self-Determination Theory Perspective
Get PDFPeople with COPD (pwCOPD) experience a range of daily living limitations caused by breathlessness, which can affect their quality of life and physical and mental health. There are approximately 1.2 million pwCOPD in the UK. Two common behavioural interventions are self-management support and pulmonary rehabilitation, which support pwCOPD to exercise and adopt techniques to decrease their symptoms; however, adherence to these can be poor. This study aimed to understand whether these two different interventions can affect motivational concepts and explore how pwCOPD experience their condition and these interventions. This study used a mixed-method design. Participants were allocated to receive either: pulmonary rehabilitation and PocketMedic (a self-management intervention), only PocketMedic, or only pulmonary rehabilitation. Questionnaires measuring self-determination theory motivational concepts were completed at baseline and seven weeks. Semi-structured interviews were conducted and analysed using Reflexive Thematic Analysis. 53 participants were recruited to the three conditions. An ANOVA found no statistically significant differences between the groups for any of the questionnaires, which may be related to the low sample size. However, when the research condition was held constant, significant improvements were identified for competence satisfaction (p < 0.001) and relatedness satisfaction (p < 0.05) and autonomy frustration (p < 0.001) and competence frustration (p < 0.05). Seven participants from the PocketMedic conditions were interviewed. Overarching themes described the participants’ experiences and adaptations to psychological need frustration, and how the interventions facilitated basic psychological need satisfaction. This study suggests that pulmonary rehabilitation and PocketMedic can improve basic psychological need satisfaction and frustration; however, there were no cumulative affects when the interventions were combined. Need frustration is important to consider in research on long-term conditions. The qualitative analysis provides greater knowledge on mechanisms by which healthcare interventions have been shown to be effective. Further research is needed including larger and more diverse samples to enable complete generalisability.</p
Characterisation of components of an extract of hemp and preliminary assessment of anti-inflammatory activity in an ex vivo model of bovine endometritis
Get PDFHemp products are currently enjoying much commercial interest as potential anti-inflammatory preparations. However, evidence for efficacy is lacking for some clinical conditions and for crude extracts and mixtures of cannabinoids. Uterine inflammation (endometritis) is a major cause of subfertility in livestock. The aim was to assess whether a commercially important crude hemp extract (extracted with supercritical CO2) and a commercial CBG:CBD (cannabigerol:cannabidiol) cannabinoid mixture have anti-inflammatory properties, using an ex vivo bovine tissue culture model of endometritis. LC-MS2 (liquid chromatography-tandem mass spectrometry) analysis of the crude extract allowed identification of twelve cannabinoids (cannabidiolic acid (CBDA), cannabidiol (CBD), cannabidivarinic acid (CBDVA), cannabidivarin (CBDV), cannabielsoic acid A (CBEA-A), cannabielsoic acid B (CBEA-B), cannabichromene (CBC), cannabinoloic acid (CBNA), cannabinol (CBN), cannabiripsol (CBR), cannabicoumarononic acid (CBCONA), cannabicoumaronone (CBCON)) in the extract, along with isomers, an alkaloid and three polyunsaturated fatty acids. Fragmentation pathways, some including 6-π-electron pericyclic processes, are proposed. Tissue explants, from uteri from heifers at stage I or IV of the oestrous cycle, were treated with control, LPS (lipopolysaccharide), crude hemp extract, or with LPS + crude hemp extract for 24 h. The CBG:CBD mixture was assessed similarly. Inflammatory responses were measured as concentrations of PGF2α, PGE2 and IL-6 in culture supernatants. Secretion of IL-6 from tissue explants was abrogated by the hemp extract (50 μg mL-1), compared to LPS alone, but it had no effect on secretion of PGF2α. The CBG:CBD mixture had no effect on any of the markers. The crude hemp extract was not cytotoxic towards MDBK bovine kidney cells whereas the CBG:CBD mixture (50 μg mL−1) caused cell death. The hemp extract warrants further investigation for anti-inflammatory effects using a broader range of inflammatory markers, whereas the CBG:CBD mixture is not recommended for further study in the context of bovine endometritis.<br/
Integrative phenomics, metabolomics and genomics analysis provides new insights for deciphering the genetic basis of metabolism in polished rice
Get PDFBackground: Metabolomics is one of the most widely used omics tools for deciphering the functional networks of the metabolites for crop improvement. However, it is technically demanding and costly.Results: We propose a relatively inexpensive approach for metabolomics analysis in which metabolomics is combined with hyperspectral imaging via machine learning. This approach can be used to target important steps in flavonoid and lipid biosynthesis in rice. We extract 1848 hyperspectral indices and 887 metabolites from polished grains of 533 Oryza sativa accessions. Hyperspectral indices are then linked to metabolites through correlation analysis and modelling. Based on this, a total of 554 metabolites and 1313 hyperspectral indices are identified for further genome-wide association study (GWAS). By GWAS, we detect 17,509 significant locus-trait associations with 2882 single nucleotide polymorphisms (SNPs). Colocalization analysis links these SNPs to the corresponding metabolites and hyperspectral indices. We detect 6415 pairs of metabolites and hyperspectral indices within a linkage disequilibrium of 300 kb in the Oryza sativa genome. We then characterize 1761 candidate genes colocalized to these loci by transcriptomic analysis. We further verify novel candidate genes encoding a novel flavonoid (LOC_Os09g18450) and a flavonoid/lipid (LOC_Os07g11020) respectively by gene editing and overexpression in rice.Conclusion: Our findings indicate that hyperspectral imaging combined with machine learning methods could serve as a powerful tool for quickly and inexpensively assessing crop metabolites.</p
Incorporating Genetic Diversity to Optimize the Plant Conservation Network in the Third Pole
Get PDFClimate change poses a significant threat to the survival of many species. Although protected areas can slow down biodiversity loss, they often lack systematic planning and do not integrate genetic diversity. Genetic diversity is a key prerequisite for species survival and the ability to tolerate new conditions. Using population genetic and distribution data from 96 plant species in the Third Pole (encompassing the Tibetan Plateau and adjacent mountains), we mapped patterns of genetic diversity, projected climate-driven range dynamics and future genetic erosion, and designed an optimal conservation framework for the region. We identified several patches of high haplotype diversity (H D), with a relatively high number of haplotypes in southeastern Third Pole. Regression models revealed that climate and topography have interacted to shape patterns of genetic diversity, with latitude and precipitation being the best predictors for H D of cpDNA and nrDNA, respectively. Ecological niche modeling predicted an approximate 43 km northwestward and 86 m upward shift in suitable habitats under future climate scenarios, likely leading to a significant loss of up to 13.19% and 15.49% of cpDNA and nrDNA genetic diversity, respectively. Alarmingly, 71.20% of the newly identified conservation priority areas fall outside of the existing protected areas and planned National Park Clusters. Therefore, we recommend expanding the network by 2.02 × 10 5 km 2 (5.91%) in the Third Pole, increasing the total conserved area to 1.36 × 10 6 km 2 (39.93%) to effectively preserve the evolutionary potential of plants. This study represents an innovative attempt to incorporate genetic diversity into biodiversity conservation efforts.</p
Lineage-specific microbial protein prediction enables large-scale exploration of protein ecology within the human gut
Get PDFMicrobes use a range of genetic codes and gene structures, yet these are often ignored during metagenomic analysis. This causes spurious protein predictions, preventing functional assignment which limits our understanding of ecosystems. To resolve this, we developed a lineage-specific gene prediction approach that uses the correct genetic code based on the taxonomic assignment of genetic fragments, removes incomplete protein predictions, and optimises prediction of small proteins. Applied to 9634 metagenomes and 3594 genomes from the human gut, this approach increased the landscape of captured expressed microbial proteins by 78.9 including previously hidden functional groups. Optimised small protein prediction captured 3,772,658 small protein clusters, which form an improved microbial protein catalogue of the human gut (MiProGut). To enable the ecological study of a protein's prevalence and association with host parameters, we developed InvestiGUT, a tool which integrates both the protein sequences and sample metadata. Accurate prediction of proteins is critical to providing a functional understanding of microbiomes, enhancing our ability to study interactions between microbes and hosts
The view from the Welsh mountains:On the rise and proliferation of small basin studies in the UK and their legacy
No full textThe 1960s and 1970s saw a blossoming of interest in hydrological processes and the establishment of a range of small catchment research programmes in the UK. Most of these studies were funded by the Natural Environment Research Council (NERC), through university grants and through its Institute of Hydrology. The university projects were mostly intentionally short-term. The Institute has suffered from funding issues and is now merged with other NERC units. It is therefore appropriate to assess what has been learnt from this research; whether the knowledge gained is of practical value to hydrology, to other disciplines or to society, or is purely academic. The paper discusses these issues with reference to a selection of small research catchments in the UK operating between the 1960s and the present day. It analyses the current situation and discusses possible ways forward for funding and research.</p