A new series of N–substituted 2–pyrazolines 9a–f, 10a–f, 11a–f, 12a–f and 13a–f were obtained from the cyclocondensation reaction of (7–chloroquinolin–4–yl)aminochalcones 8a–f with hydrazine hydrate ...and its derivatives. Fourteen of the synthesized compounds including the starting chalcones were selected by US National Cancer Institute (NCI) for testing their anticancer activity against 60 different human cancer cell lines, with the most important GI50 values ranging from 0.28 to 11.7 μM (0.13–6.05 μg/mL) and LC50 values ranging from 2.6 to > 100 μM (1.2 to > 51.7 μg/mL), for chalcones 8a,d and pyrazolines 10c,d. All compounds were assessed for antibacterial activity against wild type and multidrug resistant gram negative and gram positive bacteria, with MIC values ranging from 31.25 to 500 μg/mL. Additionally, the novel compounds were tested for antifungal and antiparasitic properties. Although these compounds showed mild activity against Candida albicans, chalcones 8a and 8e showed high activity against Cryptococcus neoformans with MIC50 = 7.8 μg/mL. For anti–Plasmodium falciparum activity the 2–pyrazoline 11b was the most active with EC50 = 5.54 μg/mL. Regarding the activity against Trypanosoma cruzi, compound 10a was highly active with EC50 = 0.70 μg/mL. Chalcone 8a had good activity against Leishmania panamensis amastigotes with EC50 = 0.79 μg/mL.
Display omitted
•New series of 4,5–dihydro–1H–pyrazoles were synthesized from quinoline–chalcones.•Compounds 8c,d and 10a,c showed important anticancer activity with GI50 0.28–11.7 μM.•Chalcones 8a and 8e showed excellent anti–C. neoformans activity with MIC50 = 7.8 μg/mL.•Pyrazoline 9d selectively inhibited N. gonorrhoeae growth.•Compounds 8a, 10a and 11b were active to Leishmania, Trypanosoma and Plasmodium, respectively.
The physiologic mechanisms by which the four activities of sleep, sedentary behavior, light-intensity physical activity, and moderate-to-vigorous physical activity (MVPA) affect health are related, ...but these relationships have not been well explored in adults. Research studies have commonly evaluated how time spent in one activity affects health. Because one can only increase time in one activity by decreasing time in another, such studies cannot determine the extent that a health benefit is due to one activity versus due to reallocating time among the other activities. For example, interventions to improve sleep possibly also increase time spent in MVPA. If so, the overall effect of such interventions on risk of premature mortality is due to both more MVPA and better sleep. Further, the potential for interaction between activities to affect health outcomes is largely unexplored. For example, is there a threshold of MVPA minutes per day, above which adverse health effects of sedentary behavior are eliminated? This article considers the 24-h Activity Cycle (24-HAC) model as a paradigm for exploring inter-relatedness of health effects of the four activities. It discusses how to measure time spent in each of the four activities, as well as the analytical and statistical challenges in analyzing data based on the model, including the inevitable challenge of confounding among activities. The potential usefulness of this model is described by reviewing selected research findings that aided in the creation of the model and discussing future applications of the 24-HAC model.
The research area of ambient assisted living has led to the development of activity recognition systems (ARS) based on human activity recognition (HAR). These systems improve the quality of life and ...the health care of the elderly and dependent people. However, before making them available to end users, it is necessary to evaluate their performance in recognizing activities of daily living, using data set benchmarks in experimental scenarios. For that reason, the scientific community has developed and provided a huge amount of data sets for HAR. Therefore, identifying which ones to use in the evaluation process and which techniques are the most appropriate for prediction of HAR in a specific context is not a trivial task and is key to further progress in this area of research. This work presents a systematic review of the literature of the sensor-based data sets used to evaluate ARS. On the one hand, an analysis of different variables taken from indexed publications related to this field was performed. The sources of information are journals, proceedings, and books located in specialized databases. The analyzed variables characterize publications by year, database, type, quartile, country of origin, and destination, using scientometrics, which allowed identification of the data set most used by researchers. On the other hand, the descriptive and functional variables were analyzed for each of the identified data sets: occupation, annotation, approach, segmentation, representation, feature selection, balancing and addition of instances, and classifier used for recognition. This paper provides an analysis of the sensor-based data sets used in HAR to date, identifying the most appropriate dataset to evaluate ARS and the classification techniques that generate better results.
Enzyme activity as a method for soil biochemistry and microbiology research has a long history of more than 100 years that is not widely acknowledged in terms of adherence to strict assay protocols ...and the interpretation of results. However, in the recent past, there is a growing lack of recognition of the historic advancements among researchers that use soil enzymology. Today, many papers are being published that use methods that either do not follow exact protocols as originally vetted in the research literature or individual labs use their own method that has not been optimized for pH, co-factors, substrate concentrations, or other conditions. This is of particular concern for fluorogenic substrates and microplate methods. Furthermore, there is a lack of understanding of the origin and location of a given enzyme being studied. Notably, regardless of the enzyme, it is too often assumed that enzyme activity equals microbial activity—which is not the case for most hydrolytic enzyme assays. Because as established by Douglas McLaren in the 1950s, a considerable amount of activity can come from catalytic enzymes stabilized in the soil matrix but that are no longer associated with viable cells (known as abiontic enzymes). In summary, today, many papers are using imperfect methods and/or misinterpret enzyme activity data that at a minimum confounds cross paper studies and meta-analysis. However, most importantly, lack of historical perspectives and ignoring strict protocols cause redundancy and fundamentally undermine the discipline and understanding of soil microbiology/biochemistry when enzymology methods are used.
Hydrazide–hydrazones possess a wide spectrum of bioactivity, including antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antidepressant, antiviral, and ...antiprotozoal properties. This review is focused on the latest scientific reports regarding antibacterial, antimycobacterial, and antifungal activities of hydrazide–hydrazones published between 2017 and 2021. The molecules and their chemical structures presented in this article are the most active derivatives, with discussed activities having a hydrazide–hydrazone moiety as the main scaffold or as a side chain. Presented information constitute a concise summary, which may be used as a practical guide for further design of new molecules with antimicrobial activity.
How can the poor and weak 'work' a political system to their advantage? Drawing mainly on interviews and surveys in rural China, Kevin O'Brien and Lianjiang Li show that popular action often hinges ...on locating and exploiting divisions within the state. Otherwise powerless people use the rhetoric and commitments of the central government to try to fight misconduct by local officials, open up clogged channels of participation, and push back the frontiers of the permissible. This 'rightful resistance' has far-reaching implications for our understanding of contentious politics. As O'Brien and Li explore the origins, dynamics, and consequences of rightful resistance, they highlight similarities between collective action in places as varied as China, the former East Germany, and the United States, while suggesting how Chinese experiences speak to issues such as opportunities to protest, claims radicalization, tactical innovation, and the outcomes of contention.
Display omitted
•AgGO with enhanced absorption in the visible spectrum through a single-step surfactant-free facile method was prepared.•WO3-x/AgrGO composite with better photocatalytic activity was ...prepared by doping WO3-x by AgGO via a hydrothermal process.•Better carrier separation and reduced impedance leading to RhB degradation and bacterial inactivation.•It exhibits versatilities for photocatalytic activities in visible regions.•Stability tests suggest its excellent reusability.
Suppressing charge recombination in semiconductors via triggering interfacial polarization and synergism provides an effective way to redeem multifunctionality and achieve environmental sustainability. Herein, we anchor a single-step facile synthesis of AgGO, providing bandgap control through varying oxidation time and subsequent simultaneous incorporation of Ag and rGO via the in situ hydrothermal method in WO3-x. The resulting WO3-x/AgrGO composite demonstrated a broadening of optical absorption and excellent suppression of carrier recombination, thereby improving the catalytic properties. The synergism and excellent conductivity of AgrGO enhance the interfacial polarization to store the carriers for longer times and help carriers carry most of their energy to the catalyst’s surface. When WO3-x/AgrGO was tested against RhB under visible light irradiation, its degradation constant reached 0.034/min, 7.4 times faster than pure WO3-x. It has left no viable bacteria during the photoinactivation of gram-negative E. coli bacteria, and even its inactivation rate is 1.07 times faster than AgGO. So, this study provides a direct method of metal-GO composite synthesis and subsequent introduction into WO3-x to broaden the versatility of environmental semiconductors.
The Achillea genus belongs to the Asteraceae family, which is mostly found in the northern hemisphere and is comprised of 115 species in the world. In Turkish flora, there are 52 species and 58 taxa, ...among them half of which are recorded as endemic. To the best of our knowledge, there has been no biological activity studied in this species until now, with the exception of one study of the antimicrobial activity of certain essential oils. This study focused primarily on the determination of antioxidant, antimicrobial, and enzyme-inhibition activity of aqueous ethanol extract of Turkish endemic Achillea cucullata by in vitro methods. The extract exhibited DPPH radical scavenging activity with an IC50 value of 132.55±0.026μg/mL, the total phenol content was 53.807±0.059 (mgGAE/g), and the total flavonoid content was 21.372±0.026 (mgQE/g), on the dry-weight basis. Antimicrobial activity was evaluated by a micro-dilution method focused on five microorganisms; two Gram-positive Staphylococcus aureus (ATCC 29213) and Enterococcus faecalis (ATCC 29212), two Gram-negative Pseudomonas aeruginosa (ATCC 27853) and Escherichia coli (ATCC 25922), and one fungal strain Candida albicans (ATCC 10231). Results show that the MIC value for the tested microorganism was higher than 5mg/mL. In this work, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glucosidase enzymes were strongly inhibited by the A. cucullata extract, and the IC50 values for these enzymes were 2.4μg/mL, 0.26μg/mL, and 24.75μg/mL, respectively. Certain acetylcholinesterase inhibitors have been used for treatment of Alzheimer's disease in the past. α-Glucosidase inhibitors are strong drug candidates, as well as potential functional food agents, for deferring the postprandial absorbency of glucose.
•Ethanol extract was prepared from endemic plant - Achillea cucullata•In vitro antioxidant was evaluated by DPPH, TPC and TFC assay•Antimicrobial activity was determined by microdilution method against five microorganisms•Acetylcholinesterase, butyrylcholinesterase, α-glucosidase enzymes were impressively inhibited by the A. cucullata ethanol extract
The occurrence of mental fatigue during tasks like driving a vehicle increases risk of injury or death. Changes in electroencephalographic (EEG) activity associated with mental fatigue has been ...frequently studied and considered a promising biomarker of mental fatigue. This is despite differences in methodologies and outcomes in prior research. A systematic review with meta‐analyses was conducted to establish the influence of mental fatigue on EEG activity spectral bands, and to determine in which regions fatigue‐related EEG spectral changes are likely to occur. A high‐yield search strategy identified 21 studies meeting inclusion criteria for investigating the change in EEG spectral activity in non‐diseased adults engaged in mentally fatiguing tasks. A medium effect size (using Cohen's g) of 0.68 (95%CI: 0.24–1.13) was found for increase in overall EEG activity following mental fatigue. Further examination of individual EEG spectral bands and regions using network meta‐analyses indicated large increases in theta (g = 1.03; 95%CI: 0.79–1.60) and alpha bands (g = 0.85; 95%CI: 0.47–1.43), with small to moderate changes found in delta and beta bands. Central regions of the scalp showed largest change (g = 0.80; 95%CI: 0.46–1.21). Sub‐group analyses indicated large increases in theta activity in frontal, central and posterior sites (all g > 1), with moderate changes in alpha activity in central and posterior sites. Findings have implications for fatigue monitoring and countermeasures with support for change in theta activity in frontal, central and posterior sites as a robust biomarker of mental fatigue and change in alpha wave activity considered a second line biomarker to account for individual variability.
There is significant risk of injury during tasks such as driving or operating machinery when mentally fatigued. Reliable biomarkers are needed that warn a fatigued person so they can take preventive action. This review uses meta‐analytic methods to synthesise the results from 21 studies. Results highlight the spectral bands and regions most promising for an EEG biomarker.
Monoterpenes, comprising hydrocarbons, are the largest class of plant secondary metabolites and are commonly found in essential oils. Monoterpenes and their derivatives are key ingredients in the ...design and production of new biologically active compounds. This review focuses on selected aliphatic, monocyclic, and bicyclic monoterpenes like geraniol, thymol, myrtenal, pinene, camphor, borneol, and their modified structures. The compounds in question play a pivotal role in biological and medical applications. The review also discusses anti-inflammatory, antimicrobial, anticonvulsant, analgesic, antiviral, anticancer, antituberculosis, and antioxidant biological activities exhibited by monoterpenes and their derivatives. Particular attention is paid to the link between biological activity and the effect of structural modification of monoterpenes and monoterpenoids, as well as the introduction of various functionalized moieties into the molecules in question.
PDF
