Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical structures that confer them with a broad spectrum of pharmacological activities. They have been extensively ...explored for designing potent and selective anticancer agents. In recent years, numerous pyrazole derivatives have been synthesized and evaluated for their anticancer potential against various cancer cell lines. Structure–activity relationship studies have shown that appropriate substitution on different positions of the pyrazole ring can significantly enhance anticancer efficacy and tumor selectivity. It is noteworthy that many pyrazole derivatives have demonstrated multiple mechanisms of anticancer action by interacting with various targets including tubulin, EGFR, CDK, BTK, and DNA. Therefore, this review summarizes the current understanding on the structural features of pyrazole derivatives and their structure-activity relationships with different targets, aiming to facilitate the development of potential pyrazole-based anticancer drugs. We focus on the latest research advances in anticancer activities of pyrazole compounds reported from 2018 to present.
As an essential component of modern drug discovery, the role of drug-target identification is growing increasingly prominent. Additionally, single-omics technologies have been widely utilized in the ...process of discovering drug targets. However, it is difficult for any single-omics level to clearly expound the causal connection between drugs and how they give rise to the emergence of complex phenotypes. With the progress of large-scale sequencing and the development of high-throughput technologies, the tendency in drug-target identification has shifted towards integrated multi-omics techniques, gradually replacing traditional single-omics techniques. Herein, this review centers on the recent advancements in the domain of integrated multi-omics techniques for target identification, highlights the common multi-omics analysis strategies, briefly summarizes the selection of multi-omics analysis tools, and explores the challenges of existing multi-omics analyses, as well as the applications of multi-omics technology in drug-target identification.
Soil protists are essential but often overlooked in soils, although they play crucial functional roles in the terrestrial ecosystem. While soil protists have drawn increased attention to their ...functional role in soils, their interaction with soil pollutants remains unresolved. This review provides a first overview of the current understanding of interactions between soil protists and major pollutants (heavy metals, organic pollutants, nanoparticles, and soil pathogens). We summarize how soil pollutants affect protists and vice versa, showing that we are just beginning to understand their complex interactions. In addition, we identify five research gaps, including hidden diversity, adaptive mechanisms, species interactions, soil bioindicators and environmental applications, and we hope that our review will help promote and build research guidelines for the future. In conclusion, a better understanding of soil pollutant-protist interactions will significantly increase our knowledge of the pollution ecology in the soil and how soil organisms respond and adapt to environmental pollution, which will contribute to the bioremediation and environmental applications of protists in soil.
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•Soil protists are essential in soil, but their interaction with soil pollutants remains unresolved.•Pollutants can negatively impact soil protists at different levels, and their sensitivity is different from bacteria.•Soil protists interact with pollutants through absorption, transformation, and predation.•High-throughput sequencing and culturing techniques are needed to understand their interactions better.•Soil protists have great potential for applications of bioindicators and soil health.
Inadequate drying and overdrying of grains due to the absence of timely and reliable information on moisture content (MC) aggravates grain postharvest loss. In this study, we investigate the ...real-time acquisition of MC using microwave free-space transmission measurements. A multifrequency swept signal is used to acquire the attenuation and phase-shift spectrum (2.00-10.00 GHz) of the paddy samples (9.553%-29.633% w.b.) for six thicknesses (1-6 cm). Based on the four rules that are followed in the phase-shift measurement, a phase-shift correction algorithm without any restrictions on the sample thickness is proposed to solve the phase-shift ambiguity that occurs when the sample thickness exceeds the wavelength. To choose the most effective frequencies, 17 candidate frequency subsets are generated by the recursive feature elimination algorithm, and the optimal frequency set, containing eight individual frequencies, is selected by using the Friedman and Nemenyi post hoc tests. The sample thickness and microwave characteristics are used as the input variables to establish the prediction models to achieve a thickness-independent measurement of the MC, and the support vector machine model yielded the best performance (<inline-formula><tex-math notation="LaTeX">R^2</tex-math></inline-formula> = 0.992, RMSE = 0.555%, and MAE = 0.398%). The results of this study should encourage future research on the real-time acquisition of reliable MC information in food processing and agriculture-related industries.
Amoebae are protists that have complicated relationships with bacteria, covering the whole spectrum of symbiosis. Amoeba-bacterium interactions contribute to the study of predation, symbiosis, ...pathogenesis, and human health. Given the complexity of their relationships, it is necessary to understand the ecology and evolution of their interactions. In this paper, we provide an updated review of the current understanding of amoeba-bacterium interactions. We start by discussing the diversity of amoebae and their bacterial partners. We also define three types of ecological interactions between amoebae and bacteria and discuss their different outcomes. Finally, we focus on the implications of amoeba-bacterium interactions on human health, horizontal gene transfer, drinking water safety, and the evolution of symbiosis. In conclusion, amoeba-bacterium interactions are excellent model systems to investigate a wide range of scientific questions. Future studies should utilize advanced techniques to address research gaps, such as detecting hidden diversity, lack of amoeba genomes, and the impacts of amoeba predation on the microbiome.
A novel quinoline-fused Rhodamine dye is designed and synthesized to achieve near-infrared fluorescent emission by expanding the π-conjugated system. Ratiometric fluorescent probe (RhQ) is further ...constructed by introducing the 3,5-ditrifluormethylthiophenol moiety into dye through a thioester bond to take advantage of spirocyclization open-ring states of Rhodamine platform. The probe exhibits remarkable dual-channel fluorescence response toward Cys/Hcy in aqueous solutions between near-infrared and visible emission, arising from the formation of closed spirolactam configuration disrupting molecular π-conjugation system. RhQ is highly selective and sensitive to Cys/Hcy with detection limits of 0.12 μM and 0.25 μM for Cys and Hcy, respectively. Moreover, imaging in cellular experiment indicates that probe displays excellent mitochondrial targeting ability, lower cytotoxicity and ratiometric responses with two well-defined emissions to ensure exactly comparison and quantitative analysis of Cys/Hcy changes in the cell.
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•A novel quinoline-fused rhodamine dye is designed and applied to construct the ratiometric fluorescent probe (RhQ).•Probe RhQ displays remarkable ratiometric fluorescent change with high selectivity and sensitivity toward Cys/Hcy.•Probe RhQ can be used to visualize monitor Cys concentration changes in mitochondria.
Breast cancer incidence rates more than double in Chinese women as they migrate from China to Hong Kong to the United States, suggesting that environmental factors contribute to the international ...variation in breast cancer incidence. Several dietary factors, which differ between the United States and the Chinese population, including intake of soy, meat, and fruits and vegetables, have been suggested to affect breast cancer risk. This report describes results from a case-control study of diet and risk of breast cancer nested in a randomized trial of breast self exam in Shanghai, China. Participating breast cancer cases (n = 378) and frequency age-matched controls (n = 1,070) completed a comprehensive food frequency questionnaire and a risk factor questionnaire. After adjustment for age, total energy intake, and total years of breast-feeding, women in the highest quartile of fruit and vegetable intake (> or =3.8 servings/d) were significantly less likely to have breast cancer (odds ratio, 0.48; 95% confidence interval, 0.29-0.78) as compared with women in the lowest quartile of intake (< or =2.3 servings/d). Egg consumption was also significantly inversely associated with risk of breast cancer (odds ratio for > or =6.0 eggs/wk versus < or =2.0 eggs/wk is 0.56; 95% confidence interval, 0.35-0.91). There was no difference in soy consumption between cases and controls. None of the associations with a single botanical family explained the strong inverse relationship between fruits and vegetables and breast cancer risk. These results provide additional evidence in support of the important role of fruits and vegetables in breast cancer prevention.
The rapid and accurate moisture content (MC) measuring of withering tea leaves faces multiple challenges. In this study, a self-developed microwave sensing system equipped with multifrequency-swept ...signals (2.00–10.00 GHz, an interval of 10.00 MHz) was used to measure the MC of withering tea leaves (16.25%–77.65%). Four kinds of hybrid-based ant colony optimizations were advanced to optimize microwave frequency signals, and the attenuation features at six frequencies (2.16, 3.42, 3.88, 4.48, 5.32 and 7.70 GHz) and phase shift features at four frequencies (2.84, 4.04, 7.88 and 8.43 GHz) were selected. Based on those optimized features, three primary models (support vector regression, extreme gradient boosting, and multi-layer perception) and one secondary model (decision tree) presented the best MC values (the average of mean absolute error was 0.349). The results showed the potential application of microwave technology in the MC monitoring in tea processing industry.
•A microwave sensing system was developed for moisture detection in tea withering.•A hybrid-based ACO algorithm was designed to optimize the frequency features.•Attenuation and phase shift features correlated with MC were selected by MRACO.•The best MC detection was achieved by the stacking model of SVR, LGBM, and MLP.
Nano- and microplastics have become a serious global concern, threatening our living environments. Previous studies have shown that many organisms, including bacteria, animals, and plants, can be ...affected by microplastics. However, little is known about one ecologically important group of soil organisms, the protists. In this study, we investigated how polystyrene micro- and nanoplastics interacted with a soil amoeba
. The results showed that environmental concentrations of nano- and microplastics could negatively affect the soil amoeba's fitness and development.
ingested both nano- and microplastics through phagocytosis but packed and excreted them during slug migration, which also promoted their biodegradation. Fourier transform infrared spectroscopy analyses revealed the formation of new oxygen-containing functional groups and the sign of possible oxidation of polystyrene. Also, nano- and microplastic exposure disrupted the nutrient and energy metabolisms of
and affected the expression of key genes (e.g.,
,
,
,
, and
) related to morphogenesis and phagocytosis. In conclusion, our results show that nano- and microplastics have complex bilateral interactions with the soil amoeba, affecting each other's fate in the soil environment. This study provides new insights into how soil protists interact with nano- and microplastics in the soil ecosystem.
We propose NetSpec, a tool that synthesizes network specifications in a declarative logic programming language from input-output examples. NetSpec aims to accelerate the adoption of formal ...verification in networking practice, by reducing the effort and expertise required to specify network models or properties. NetSpec aims to be i) highly expressive, capable of synthesizing network specifications with complex semantics; ii) scalable, by virtue of using a novel best-first search algorithm to efficiently explore an unbounded solution space, and iii) robust, avoiding the need for exhaustive input-output examples by actively generating new examples. Our experiments demonstrate that NetSpec can synthesize a wide range of specifications used in network verification, analysis, and implementations. Furthermore, NetSpec improves upon existing approaches in terms of expressiveness, robustness to examples, and the quality of synthesized programs.
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