To develop new compounds with high activity, broad spectrum and low-toxicity, 17 benzamides substituted with quinoline-linked 1,2,4-oxadiazole were designed using the splicing principle of active ...substructures and were synthesized. The biological activities were evaluated against 10 fungi, indicating that some of the synthetic compounds showed excellent fungicidal activities. For example, at 50 mg/L, the inhibitory activity of 13p (3-Cl-4-Cl substituted, 86.1%) against Sclerotinia sclerotiorum was superior to that of quinoxyfen (77.8%), and the inhibitory activity of 13f (3-CF3 substituted, 77.8%) was comparable to that of quinoxyfen. The fungicidal activities of 13f and 13p to Sclerotinia sclerotiorum were better than that of quinoxyfen (14.19 mg/L), with EC50 of 6.67 mg/L and 5.17 mg/L, respectively. Furthermore, the acute toxicity of 13p was 19.42 mg/L, classifying it as a low-toxic compound.
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In order to discover pesticidal lead compounds with high activity and low toxicity, a series of novel benzamides substituted with pyrazole-linked 1,2,4-oxadiazole were designed via bioisosterism. The ...chemical structures of the target compounds were confirmed via 1H NMR, 13C NMR and HRMS analysis. The preliminary bioassay showed that most compounds exhibited good lethal activities against Mythimna separate, Helicoverpa armigera, Ostrinia nubilalis and Spodoptera frugiperda at 500 mg/L. Particularly in the case of Mythimna separate, compound 14q (70%) exhibited obvious insecticidal activity. In addition, compound 14h demonstrated good fungicidal activity against Pyricularia oryae with an inhibition rate of 77.8%, and compounds 14e, 14k, 14n and 14r also showed certain antifungal activities (55.6–66.7%). The zebrafish toxicity test showed that the LC50 of compound 14h was 14.01 mg/L, which indicated that it may be used as a potential leading compound for further structural optimization.
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“Learning by design” is a widely used approach for developing teachers' technological pedagogical content knowledge (TPACK) in the context of designing technology-enhanced instruction. This approach ...offers teachers the opportunity to learn from colleagues with different areas of expertise. Despite the critical importance of teachers' collaborative discourse in mediating teacher learning in the design process, there has not yet been a TPACK review to analyze how researchers investigate this discourse. After a systematic literature search, we identified eleven TPACK studies from seven geographical regions that investigated teachers' collaborative discourse, and then examined how the researchers had structured and analyzed this discourse and integrated their findings. Our analysis identified four strategies used by the researchers to structure and promote teachers' collaborative discourse. We found that most studies relied on the “coding and counting” data analysis method to reveal the distribution of TPACK (sub)sets expressed in the collaborative discourse but not the dynamics of the knowledge construction process or the progression of the discourse. Although the studies generally provided initial evidence for the efficacy of the design process, this evidence was rarely based on changes in teachers' TPACK as enacted during classroom instruction or on the quality of the design outcomes. We thus propose a new conceptual framework that emphasizes the reciprocal knowledge exchange process between the TPACK of individual teachers and the knowledge shared by teachers through collaboration. This framework refocuses the attention of researchers on investigating and connecting teachers’ individual and collective TPACK and their development during the learning by design process.
•Eleven TPACK studies were identified that investigated teachers' collaborative discourse.•How TPACK researchers investigated teacher collaborative discourse was analyzed.•Research designs and related findings in the field were synthesized and appraised.•Strategies to promote productive teacher collaborative discourse were identified.•A TPACK framework connecting personal, collective and enacted TPACK was proposed.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
N-N axially chiral skeletons are significant structural motifs in natural products, pharmaceuticals, and functional materials. Herein we disclose a method for the asymmetric synthesis of N-N axially ...chiral compounds by phase-transfer catalysis. A wide range of N-N axially chiral quinazolinone derivatives were prepared in high yields with excellent stereoselectivities. Furthermore, the synthetic utility of the protocol was proved by large-scale reaction and transformation of the product. Density functional theory calculations provide insight into the mechanism.
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IJS, KILJ, NUK, PNG, UL, UM
The advancements in wireless communication impose a growing range of demands on the antennas performance, requiring multiple functionalities to be present in a single device. To satisfy these ...different application needs within a limited space, reconfigurable antennas are often used which are able to switch between a number of states, providing multiple functions using a single antenna. Electronic switching components, such as PIN diodes, radio-frequency micromechanical systems (RF-MEMS), and varactors, are typically used to achieve antenna reconfiguration. However, some of these approaches have certain limitations, such as narrow bandwidth, complex biasing circuitry, and high activation voltages. In recent years, an alternative approach using liquid dielectric materials for antenna reconfiguration has drawn significant attention. The intrinsic conformability of liquid dielectric materials allows us to realize antennas with desired reconfigurations with different physical constraints while maintaining high radiation efficiency. The purpose of this review is to summarize different approaches proposed in the literature for the liquid dielectric reconfigurable antennas. It facilitates the understanding of the advantages and limitations of this technology, and it helps to draw general design principals for the development of reconfigurable antennas in this category.
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Pharmaceuticals in surface waters have raised significant concern in recent years for their potential environmental effects. This study identified that at present a total of 477 substances (including ...66 metabolites and transformation products) have been analyzed in European surface waters. Around 60% (284) of these compounds belonging to 16 different therapeutic groups were positively detected in one or more of 33 European countries. To conveniently and effectively prioritize potential high-risk compounds, an optimized method that considers the frequency of concentrations above predicted no effects levels was developed on the basis of the traditional method, and it was then used to identify and screen candidate priority pollutants in European surface waters. The results proved the feasibility and advantages of the optimized method. Pharmaceuticals detected in European surface waters were classified into 5 categories (high, moderate, endurable, negligible and safe) depending on their potential environmental effects and the distribution of pharmaceuticals. Circa 9% (45 out of 477) analyzed compounds showed a potential environmental risk to aquatic ecosystems. Among these 45 compounds, 12 compounds were indicated to have high environmental risk in aquatic environments, while 17 and 7 compounds showed moderate and small-scale environmental risks, respectively.
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•An optimized method was developed to identify and screen candidate priority pollutants in surface waters.•Different therapeutic groups were positively detected in many European countries.•45 compounds showed potential environmental risks in European surface waters.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Diffuse gliomas are the most common type of primary brain and central nervous system (CNS) tumors. Protein disulfide isomerases (PDIs) such as P4HB and PDIA3 act as molecular chaperones for ...reconstructing misfolded proteins, and are involved in endoplasmic reticulum stress and the unfolded protein response. The present study focused on the role of P4HB and PDIA3 in diffuse gliomas. Analysis of GEO and HPA data revealed that the expression levels of P4HB and PDIA3 were upregulated in glioma datasets. their increased expression was then validated in 99 glioma specimens compared with 11 non-tumor tissues. High expression of P4HB and PDIA3 was significantly correlated with high Ki-67 and a high frequency of the TP53 mutation. Kaplan-Meier survival curve and Cox regression analyses showed that glioma patients with high P4HB and PDIA3 expression had a poor survival outcome, P4HB and PDIA3 could be independent prognostic biomarkers for diffuse gliomas. In vitro, knockdown of PDIA3 suppressed cell proliferation, induced cell apoptosis, and decreased the migration of glioma cells. Furthermore, downregulation of P4HB and PDIA3 may contribute to improve the survival of patients who receive chemotherapy and radiotherapy. The data suggest that high expression of P4HB and PDIA3 plays an important role in glioma progression, and could predict the survival outcome and therapeutic response of glioma patients. Therefore, protein disulfide isomerases may be explored as prognostic biomarkers and therapeutic targets for diffuse gliomas.
Aim
The aim of this study was to conduct comprehensive phylogeographic and demographic analyses to examine the degree to which topographic and climatic conditions have affected the patterns of ...diversification and migration in a strictly montane inhabitant, the montane long‐tailed mole (Scaptonyx fusicaudus).
Location
The mountains of south‐western China and adjacent mountains including Mts. Bashan, Dalou and Qinling also known as the sky islands in south‐western China.
Taxon
The long‐tailed mole (S. fusicaudus), a semi‐fossorial mammal distributed in the sky islands of south‐western China, is a relict species and the sole representative of the tribe Scaptonychini.
Methods
We sequenced one mitochondrial and six nuclear genes from 113 samples across the species’ range. We estimated phylogenetic relationships and divergence times, conducted genetic structuring and species delimitation using multiple approaches and used Approximate Bayesian Computation to test potential gene flow. We conducted ecological niche modelling to predict the species’ potential distribution in the present, the last glacial maximum and the last interglacial (LIG).
Results
The species comprises a minimum of 17 operational taxonomic units which are isolated in different mountain ranges. The lowlands and large rivers act as barriers to dispersal, and have isolated evolutionary lineages for up to 11 million years. Long‐distance dispersal is evident among a few discrete montane archipelagos. Suitable climatic conditions during the LIG are limited to only a few sites, thus geographically restricting climatic stable areas across geological periods (from the LIG to the present).
Main conclusions
For low‐vagility species, the complex topography of the sky islands has promoted exceptional diversification through a combination of eco‐environmental stability as well as geographic fragmentation. The mountains have acted as a buffer against climate change, and have provided continuously suitable habitats for S. fusicaudus since the early Late Miocene, supporting the hypothesis that the sky islands constitute “museums” of ancient lineages. Lowlands and river valleys have acted as barriers preventing gene flow, while the montane archipelagos could have provided stepping stones to facilitate dispersal.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
Background
As one of the gamification elements, leaderboard, especially absolute leaderboard, is widely used in educational gamification systems. However, empirical studies on the optimal use ...condition of the leaderboard and underlying influence mechanisms are deficient.
Objectives
This study explored which difficulty was more conducive to learning performance in leaderboard context, and when and how it played a role.
Methods
To address these questions, this study conducted a 2 (dominant goal orientation: learning/performance) × 2 (difficulty: high/low) between‐subjects design. Seventy‐eight dominant learning‐oriented and 78 dominant performance‐oriented participants were recruited and randomly assigned to the high or low difficulty group respectively.
Results and Conclusions
Participants in the low difficulty group experienced more positive emotions, less negative emotions, and higher learning motivation than those in the high difficulty group, but the effect of difficulty on performance was not significant. Moreover, goal orientation did not moderate the effects of difficulty, dominant learning‐oriented and performance‐oriented learners were equally affected by difficulty. Further mediating analysis showed that negative emotions and learning motivation rather than positive emotions mediated the relationship between difficulty and learning performance.
Implications
These results confirmed the positive effect of low difficulty in leaderboard context, as well as the mediating roles of emotions and motivation involved in the relationship between difficulty and learning performance. These findings enlighten us that it is necessary to equip leaderboards in educational gamification with achievable difficulty.
Lay Description
What is already known about this topic
As one of the gamification elements, leaderboard was widely used in educational gamification.
The effect of the leaderboard was not always consistent among various educational situations.
Empirical studies on the optimal use condition of the leaderboard were deficient.
The mechanisms by difficulty within leaderboards affected the learning performance were not clear.
What this paper adds
Lower difficulty within leaderboards could induce more positive emotions, less negative emotions and higher learning motivation.
Difficulty within leaderboards did not directly affect learning performance.
Negative emotions and learning motivation mediated the relationship between difficulty and performance.
Dominant goal orientation did not moderate the effect of difficulty on learning.
The implications of study findings for practitioners
We could improve learners' emotional and motivational states by reducing difficulty within leaderboards.
We could promote learning performance through appropriate emotional and motivational designs using gamification.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
Triple-negative breast cancer (TNBC) is the most fatal subtype of breast cancer; however, effective treatment strategies for TNBC are lacking. Therefore, it is important to explore the mechanism of ...TNBC metastasis and identify its therapeutic targets. Dysregulation of ETHE1 leads to ethylmalonic encephalopathy in humans; however, the role of ETHE1 in TNBC remains elusive. Stable cell lines with ETHE1 overexpression or knockdown were constructed to explore the biological functions of ETHE1 during TNBC progression in vitro and in vivo. Mass spectrometry was used to analyze the molecular mechanism through which ETHE1 functions in TNBC progression. ETHE1 had no impact on TNBC cell proliferation and xenograft tumor growth but promoted TNBC cell migration and invasion in vitro and lung metastasis in vivo. The effect of ETHE1 on TNBC cell migratory potential was independent of its enzymatic activity. Mechanistic investigations revealed that ETHE1 interacted with eIF2α and enhanced its phosphorylation by promoting the interaction between eIF2α and GCN2. Phosphorylated eIF2α in turn upregulated the expression of ATF4, a transcriptional activator of genes involved in cell migration and tumor metastasis. Notably, inhibition of eIF2α phosphorylation through ISRIB or ATF4 knockdown partially abolished the tumor-promoting effect of ETHE1 overexpression. ETHE1 has a functional and mechanistic role in TNBC metastasis and offers a new therapeutic strategy for targeting ETHE1-propelled TNBC using ISRIB.
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